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Special Issue "Bioactive Compounds and Antioxidant Activity of Extracts from Different Natural Plants"

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Natural Products Chemistry".

Deadline for manuscript submissions: 15 March 2022.

Special Issue Editor

Dr. Maria Atanassova
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Guest Editor
Department of Chemical Engineering, Scientific consulting, UCTM–Sofia, Bulgaria
Interests: natural plants and products; methods of determination of bioactive compounds and antioxidant activity; different methods of extraction; total phenolic and total flavonoid compounds and vitamins and macro- and micro elements

Special Issue Information

Dear Colleagues,

“Health is priceless”—this is the maxim that we heard as children but whose truth we appreciate only when we do not feel well. In our everyday life, in the high-tech twenty-first century, we imperceptibly move away from the principles underlying a healthy lifestyle—active movement and a balanced diet. The power of food for the growth and development of the human organism has been known and applied in practice since ancient times. As early as in the fourth century BC, the father of modern medicine, Hippocrates said, “Let your food be your medicine and your medicine be your food”. A vast amount of historical evidence—old manuscripts, papyri, archaeological findings—proves that long before the birth of Christ, the ancient Chinese, Indians, Egyptians, Japanese, Greeks, and Romans cherished herbs, garlic, onion, honey, and honey products not only as food or spice but also as a medicine. In Hippocrates’ time, as well as during the Roman Empire, the dark years of the Middle Ages, and all the way up to now, wine has been recommended as a therapeutic means. We often forget that in addition to pleasure, food can mean health. Of course, this is only true if you know how to use, combine, and dose it.

Biologically active substances in foods are compounds which help people to maintain their vital functions, prevent multiple diseases, and ensure their effective treatment. There are different classifications of biologically active compounds depending on their origin, their chemical composition, and their structure, as well as on their biological activity, and last but not least, the effect of their influence on human health. Antioxidants and free radicals are popular terms used by both health professionals and specialists in other fields of science.

Over the past few years, an unprecedented explosion of information around the role of oxidative stress on a number of serious diseases such as cancer, diseases of the cardiovascular system, and some degenerative changes as well as diseases of the human organism associated with aging has been registered. Many diseases are associated with the action of the oxidants, which include active forms of oxygen, nitrogen, sulphur-centered radicals, and various other active radical forms. They are generated constantly in the body by means of the normal metabolism, environmental pollutants, and tension and stress that accompany our existence. Food as a source of antioxidants occupies a central role in the battle against the harmful effects of the free radicals, protecting the human body from many diseases, and confirming the dictum of Norman Kretschmer that “Food is the secret key to prevention”.

The main aims of this Special Issue on “Bioactive Compounds and Antioxidant Activity of Extracts from different Natural Plants” is to be an open forum where researchers may share their investigations and findings in this promising field and, thanks to the open access platform, increase their visibility and the chances to interact with industries and the production systems. Contributions to this issue, both in the form of original research or review articles, may cover all aspects of dietary and non-dietary bioactive compounds, nature plants and products, and different type of extractions; studies with a multidisciplinary input, offering new methodologies or insights, are particularly welcome.

Dr. Maria Atanassova
Guest Editor

Manuscript Submission Information

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Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2300 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • Natural plants and products
  • Methods of determination of bioactive compounds
  • Different methods of extraction
  • Methods of determination of antioxidant activity
  • Total phenolic and total flavonoid compounds
  • Vitamins and macro- and micro elements

Published Papers (59 papers)

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Research

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Article
Antioxidant, Antimicrobial Activities and Characterization of Polyphenol-Enriched Extract of Egyptian Celery (Apium graveolens L., Apiaceae) Aerial Parts via UPLC/ESI/TOF-MS
Molecules 2022, 27(3), 698; https://doi.org/10.3390/molecules27030698 - 21 Jan 2022
Viewed by 190
Abstract
Medicinal plant extracts are increasingly considered a major source of innovative medications and healthcare products. This study focused on preparing a polyphenol enriched water extract of Egyptian celery “Apium graveolens L., Apiaceae” aerial parts (TAE) in an endeavor to accentuate its antioxidant [...] Read more.
Medicinal plant extracts are increasingly considered a major source of innovative medications and healthcare products. This study focused on preparing a polyphenol enriched water extract of Egyptian celery “Apium graveolens L., Apiaceae” aerial parts (TAE) in an endeavor to accentuate its antioxidant capacity as well as its antimicrobial activity. (TAE) of celery was partitioned against different organic solvents to yield dichloromethane (DCM), ethyl acetate (EAC), and butanol (BUOH) fractions. (TAE) and the organic fractions thereof besides the remaining mother liquor (ML) were all screened for their antioxidant capacity using various protocols viz. monitoring the reducing amplitudes for ferric ions (FRAP), and radical scavenging potentials of oxygen (ORAC), 2,2’-azino-bis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS), 2,2-diphenyl-1-picrylhydrazyl (DPPH), and metal chelation assays. The examination procedure revealed both (TAE) extract and (DCM) fraction, to pertain the highest antioxidant potentials, where the IC50 of the (TAE) using ABTS and metal chelation assays were ca. 34.52 ± 3.25 and 246.6 ± 5.78 µg/mL, respectively. The (DCM) fraction recorded effective results using the FRAP, ORAC, and DPPH assays ca. 233.47 ± 15.14 and 1076 ± 25.73 μM Trolox equivalents/mg sample and an IC50 474.4 ± 19.8 µg/mL, respectively. Additionally, both (TAE) and (DCM) fraction exerted antimicrobial activities recording inhibition zones (mm) (13.4 ± 1.5) and (12.0 ± 1.0) against Staphylococcus aureus and (11.0 ± 1.2) and (10.0 ± 1.3) against Escherichia coli, respectively, with no anti-fungal activity. Minimum inhibitory concentration (MIC) of (TAE) and (DCM) fraction were 1250 and 2500 µg/mL, respectively. UPLC/ESI/TOF-MS unveiled the chemical profile of both (TAE) and (DCM) fraction to encompass a myriad of active polyphenolic constituents including phenylpropanoids, coumarins, apigenin, luteolin, and chrysoeriol conjugates. Full article
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Article
Comparative Assessment of Phytochemical Compounds and Antioxidant Properties of Kernel Oil from Eight Sour Cherry (Prunus cerasus L.) Cultivars
Molecules 2022, 27(3), 696; https://doi.org/10.3390/molecules27030696 - 21 Jan 2022
Viewed by 136
Abstract
New plant oils as a potential natural source of nutraceutical compounds are still being sought. The main components of eight cultivars (‘Koral’, ‘Lucyna’, ‘Montmorency’, ‘Naumburger’, ‘Wanda’, ‘Wigor’, ‘Wołyńska’, and ‘Wróble’) of sour cherry (Prunus cerasus L.) grown in Poland, including crude fat, [...] Read more.
New plant oils as a potential natural source of nutraceutical compounds are still being sought. The main components of eight cultivars (‘Koral’, ‘Lucyna’, ‘Montmorency’, ‘Naumburger’, ‘Wanda’, ‘Wigor’, ‘Wołyńska’, and ‘Wróble’) of sour cherry (Prunus cerasus L.) grown in Poland, including crude fat, protein, and oil content, were evaluated. The extracted oils were analysed for chemical and biological activity. The oils had an average peroxide value of 1.49 mEq O2/kg, acid value of 1.20 mg KOH/g, a saponification value of 184 mg of KOH/g, and iodine value of 120 g I2/100 g of oil. The sour cherry oil contained linoleic (39.1–46.2%) and oleic (25.4–41.0%) acids as the major components with smaller concentrations of α-eleostearic acid (8.00–15.62%), palmitic acid (5.45–7.41%), and stearic acid (2.49–3.17%). The content of sterols and squalene varied significantly in all the studied cultivars and ranged between 336–973 mg/100 g and 66–102 mg/100 g of oil. The contents of total tocochromanols, polyphenols, and carotenoids were 119–164, 19.6–29.5, and 0.56–1.61 mg/100 g oil, respectively. The cultivar providing the highest amounts of oil and characterised by the highest content of PUFA (including linoleic acid), plant sterols, α-and β-tocopherol, as well as the highest total polyphenol and total carotenoids content was been found to be ‘Naumburger’. The antioxidant capacity of sour cherry kernel oils, measured using the DPPH and ABTS•+ methods, ranged from 57.7 to 63.5 and from 38.2 to 43.2 mg trolox/100 g oil, respectively. The results of the present study provide important information about potential possibilities of application of Prunus cerasus kernel oils in cosmetic products and pharmaceuticals offering health benefits. Full article
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Article
Optimization of Bioactive Phenolics Extraction and Cosmeceutical Activity of Eco-Friendly Polypropylene-Glycol–Lactic-Acid-Based Extracts of Olive Leaf
Molecules 2022, 27(2), 529; https://doi.org/10.3390/molecules27020529 - 14 Jan 2022
Viewed by 152
Abstract
Olive leaf is a rich source of phenolic compounds with numerous activities related to skin health and appearance. In this study, a green extraction method was developed using eco-friendly solvents: polypropylene glycol (PPG), lactic acid (LA), and water. The optimal extraction conditions were [...] Read more.
Olive leaf is a rich source of phenolic compounds with numerous activities related to skin health and appearance. In this study, a green extraction method was developed using eco-friendly solvents: polypropylene glycol (PPG), lactic acid (LA), and water. The optimal extraction conditions were established, including solvent, extraction time, technique (magnetic stirrer vs. ultrasound-assisted extraction), and herbal material/solvent ratio. The composition of the solvent mixture was optimized using a mixture design. The content of phenolic compounds, including oleuropein and verbascoside, was determined using high-performance liquid chromatography (HPLC) and spectrophotometric methods. Using different extraction conditions, three extracts were prepared and their phytochemical compositions and antioxidant and skin-related bioactivities were investigated. The extracts were excellent inhibitors of elastase, collagenase, tyrosinase, and lipoxygenase. The best activity was shown by the extract richest in phenolics and prepared using magnetic-stirrer-assisted extraction for 20 min, with 0.8 g of herbal material extracted in 10 mL of PPG/LA/water mixture (28.6/63.6/7.8, w/w/w), closely followed by the extract prepared using the same extraction conditions but with 0.42 g of herbal material. The investigated PPG/LA/water mixtures contributed to the overall enzyme-inhibitory activity of the extracts. The prepared extracts were appropriate for direct use in cosmetic products, thus saving the time and energy consumption necessary for the evaporation of conventional solvents. Full article
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Article
Chemical Profile, Antimicrobial and Antioxidant Activity Assessment of the Crude Extract and Its Main Flavonoids from Tartary Buckwheat Sprouts
Molecules 2022, 27(2), 374; https://doi.org/10.3390/molecules27020374 - 07 Jan 2022
Viewed by 132
Abstract
The purpose of this study was to investigate the major flavonoids content and bioactivities of Tartary buckwheat sprouts. The crude methanol extract (ME) of Tartary buckwheat sprouts was abundant in flavonoids, and six major flavonoids, including isoorientin, vitexin, isovitexin, rutin, quercetin, and kaemferol [...] Read more.
The purpose of this study was to investigate the major flavonoids content and bioactivities of Tartary buckwheat sprouts. The crude methanol extract (ME) of Tartary buckwheat sprouts was abundant in flavonoids, and six major flavonoids, including isoorientin, vitexin, isovitexin, rutin, quercetin, and kaemferol were successfully determined from the sprouts by the high-performance liquid chromatography (HPLC) method. Generally, the flavonoid content of buckwheat sprouts was in the order of rutin > quercetin > isovitexin > vitexin> isoorientin > kaemferol. The highest rutin content of the ME and sprout cultures was 89.81 mg/g and 31.50 mg/g, respectively. Antibacterial activity results indicated the ME displayed notable inhibitory activity against the five tested bacteria, and its minimum inhibitory concentration (MIC) values ranged from 0.8 mg/mL to 3.2 mg/mL. Among the six flavonoids, quercetin was the most active compound, which exhibited strong activity against all tested bacteria except for E. coli and S. epidermidis, with its MIC values ranging from 0.2 mg/mL to 0.4 mg/mL. For the antifungal activity assay, the ME of Tartary buckwheat sprouts and four flavonoids could significantly inhibit the spore germination of two pathogenic fungi, and their inhibitory efficiency was concentration dependent. Quercetin was the most active one, which significantly inhibited the spore germination of F. oxysporum f. sp. vasinfectum and F. oxysporum f. sp. cucumerinum, and its median effective inhibitory concentration (IC50) value was 42.36 and 32.85 µg/mL, respectively. The antioxidant activity results showed that quercetin, kaemferol, and rutin displayed excellent antioxidant activity in the DPPH radical scavenging test, and their IC50 value was calculated as 5.60, 16.23, and 27.95 µg/mL, respectively. This is the first report on the antimicrobial activity of the crude extract of Tartary buckwheat sprouts. These results indicated that the methanol extract of Tartary buckwheat sprouts could be used as a potential antimicrobial or antioxidant agent in the future. Full article
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Article
Potential Associations among Bioactive Molecules, Antioxidant Activity and Resveratrol Production in Vitis vinifera Fruits of North America
Molecules 2022, 27(2), 336; https://doi.org/10.3390/molecules27020336 - 06 Jan 2022
Viewed by 138
Abstract
Grapes (Vitis vinifera L.) are rich in bioactive molecules contributing to health benefits. Consumption of grapes is linked to reduced incidence of cardiovascular diseases. Studies on table grape cultivars are limited although much attention in research was focused on the wine industry. [...] Read more.
Grapes (Vitis vinifera L.) are rich in bioactive molecules contributing to health benefits. Consumption of grapes is linked to reduced incidence of cardiovascular diseases. Studies on table grape cultivars are limited although much attention in research was focused on the wine industry. Bioactive effects of grapes as anti-inflammatory, anticarcinogenic, cardioprotective, vasorelaxant, phytoestrogenic and neuroprotective have also been reported. For example, resveratrol is a natural food ingredient present in grapes, with high antioxidant potential. Here we conducted an exploratory study to investigate bioactive molecules, antioxidant activity and the association between constitutive stilbene synthase (STS) gene expression and the resveratrol biosynthesis in selected table grape varieties in North America. The phenolic compounds, fatty acid composition and antioxidant activity of four grape varieties were compared. Red Globe variety was rich in unsaturated fatty acids as well as phenolic compounds such as caffeic acid, quercetin and resveratrol. Meanwhile, the constitutive expression of grape stilbene synthase gene was higher in Flame and Autumn Royal where resveratrol content of these cultivars was relatively low compared to the Red Globe variety. This study shows the potential links in grape antioxidant activity and resveratrol production, but more studies are necessary to show the association. Full article
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Article
Isolation of Anti-Diabetic Active Compounds from Benincasae Exocarpium and Development of Simultaneous Analysis by HPLC-PDA
Molecules 2022, 27(1), 9; https://doi.org/10.3390/molecules27010009 - 21 Dec 2021
Viewed by 397
Abstract
Diabetes is a chronic metabolic disease that is a constant problem. Previous studies have reported that Benincasa cerifera Savi. extracts are effective in treating diabetes and its complications. Benincasae Exocarpium (BE) is a fruit peel of B. cerifera that has been reported to [...] Read more.
Diabetes is a chronic metabolic disease that is a constant problem. Previous studies have reported that Benincasa cerifera Savi. extracts are effective in treating diabetes and its complications. Benincasae Exocarpium (BE) is a fruit peel of B. cerifera that has been reported to be used for the prevention and treatment of metabolic diseases such as hyperglycemia, obesity, and hyperlipidemia. However, there are not enough studies on the compounds and bioassays to support the efficacy of BE. The inhibitory activity of the BE extracts and fractions against advanced glycation end-products (AGE) formation and α-glucosidase activity was evaluated. These assays are relevant for the treatment of type 2 diabetes and its complications. Based on these results, compounds 111 were isolated through bioassay-guided isolation. In addition, we developed a high-performance liquid chromatography (HPLC) method that can simultaneously analyze these 11 compounds. Activity evaluation of the compounds was also conducted, and eight compounds exhibited significant activity. Among these, flavonoid compounds showed strong activity. A quantitative evaluation of eight bioactive compounds (2, 511) was conducted. In conclusion, this study demonstrated the potential of BE for prevention and treatment of type 2 diabetes and its complications. Full article
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Article
Effect of Extraction Methods on Polyphenols, Flavonoids, Mineral Elements, and Biological Activities of Essential Oil and Extracts of Mentha pulegium L.
Molecules 2022, 27(1), 11; https://doi.org/10.3390/molecules27010011 - 21 Dec 2021
Viewed by 1008
Abstract
Our study evaluated the in vitro antioxidant properties, antibacterial and antifungal activities, anti-inflammatory properties, and chemical composition of the essential oils (EOs), total phenol, and total flavonoid of wild Mentha pulegium L. This study also determined the mineral (nutritional and toxic) elements in [...] Read more.
Our study evaluated the in vitro antioxidant properties, antibacterial and antifungal activities, anti-inflammatory properties, and chemical composition of the essential oils (EOs), total phenol, and total flavonoid of wild Mentha pulegium L. This study also determined the mineral (nutritional and toxic) elements in the plant. The EOs were extracted using three techniques—hydro distillation (HD), steam distillation (SD), and microwave-assisted distillation (MAD)—and were analyzed using chromatography coupled with flame ionization (GC-FID) and gas chromatography attached with mass spectrometry detector (GC-MS). The antioxidant effects of the EOs were tested with 2,2-diphenyl-1-picrylhydrazyl (DPPH) and ABTS (2,2’-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid), while the antibacterial and antifungal activities of the EO and methanolic extract were tested using Staphylococcus aureus, Bacillus subtilis, Pseudomonas aeruginosa, Escherichia coli, and Candida albicans. Twenty-six compounds were identified in the essential oil, representing 97.73% of the total oil, with 0.202% yield. The major components were pulegone (74.81%), menthone (13.01%) and piperitone (3.82%). Twenty-one elements, including macro- and micro-elements (Ba, Br, Ca, Cl, Co, Cr, Cs, Eu, Fe, K, Mg, Mn, Mo, Na, Rb, Sb, Sc, Sr, Th, U and Zn), were detected using neutron activation analysis (INAA) and inductively coupled plasma optical emission spectrometry (ICP-OES), with the concentration of mineral element close to the FAO recommendation. The results show that the EOs and extracts from Mentha pulegium L. had significant antimicrobial activities against the microorganisms, including five human pathogenic bacteria, one yeast (Candida albicans), and one phytopathogenic fungi. The in vivo anti-inflammatory activities of the leaf extracts were confirmed. The results indicate that the EOs and extracts from Mentha pulegium L. have promising applications in the pharmaceutical industries, clinical applications, and in medical research. Full article
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Article
HPLC/DAD, Antibacterial and Antioxidant Activities of Plectranthus Species (Lamiaceae) Combined with the Chemometric Calculations
Molecules 2021, 26(24), 7665; https://doi.org/10.3390/molecules26247665 - 17 Dec 2021
Viewed by 506
Abstract
The increase in antibiotic resistance and the emergence of new bacterial infections have intensified the research for natural products from plants with associated therapy. This study aimed to verify the antibacterial and antioxidant activity of crude extracts of the genus Plectranthus species, being [...] Read more.
The increase in antibiotic resistance and the emergence of new bacterial infections have intensified the research for natural products from plants with associated therapy. This study aimed to verify the antibacterial and antioxidant activity of crude extracts of the genus Plectranthus species, being the first report on the modulation of aminoglycosides antibiotic activity by Plectranthus amboinicus extracts. The chemical composition was obtained by chemical prospecting and High-Performance Liquid Chromatography with diode arrangement detector (HPLC/DAD). The antibacterial activities of the extracts alone or in association with aminoglycosides were analyzed using the microdilution test. The antioxidant activity was evaluated by 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging. The phytochemical prospection allowed the flavonoids, saponins, tannins and triterpenoids to be identified. Quercetin, rutin, gallic acid, chlorogenic acid, caffeic acid, catechin, kaempferol, glycosylated kaempferol, quercitrin, and isoquercitrin were identified and quantified. The principal component analysis (PCA) observed the influence of flavonoids and phenolic acids from Plectranthus species on studied activities. Phytochemical tests with the extracts indicated, especially, the presence of flavonoids, confirmed by quantitative analysis by HPLC. The results revealed antibacterial activities, and synergistic effects combined with aminoglycosides, as well as antioxidant potential, especially for P. ornatus species, with IC50 of 32.21 µg/mL. Multivariate analyzes show that the inclusion of data from the antioxidant and antibacterial activity suggests that the antioxidant effect of these species presents a significant contribution to the synergistic effect of phytoconstituents, especially based on the flavonoid contents. The results of this study suggest the antibacterial activity of Plectranthus extracts, as well as their potential in modifying the resistance of the analyzed aminoglycosides. Full article
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Article
In Vitro Phytochemical Screening, Cytotoxicity Studies of Curcuma longa Extracts with Isolation and Characterisation of Their Isolated Compounds
Molecules 2021, 26(24), 7509; https://doi.org/10.3390/molecules26247509 - 11 Dec 2021
Cited by 1 | Viewed by 491
Abstract
The Curcuma longa plant is endowed with multiple traditional and therapeutic utilities and is here explored for its phytochemical constituents and cytotoxic potential. Turmeric rhizomes were extracted from three different solvents and screened for the presence of different phytochemical constituents, observation of which [...] Read more.
The Curcuma longa plant is endowed with multiple traditional and therapeutic utilities and is here explored for its phytochemical constituents and cytotoxic potential. Turmeric rhizomes were extracted from three different solvents and screened for the presence of different phytochemical constituents, observation of which indicated that the polar solvents favoured extraction of greater versatile phytochemical constituents. These extracts were investigated for their cytotoxic potential by MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay on three different of cell lines including SCC-29B (oral cancer cell line), DU-145 (prostate cancer cell line) and the Vero cell line (healthy cell line/non-cancerous cell line). This assay was performed by taking three extracts from isolated curcuminoids and a pure bioactive compound bisdemethoxycurcumin (BD). Bisdemethoxycurcumin was isolated from curcuminoids and purified by column and thin-layer chromatography, and its structural characterisation was performed with different spectroscopic techniques such as FTIR, NMR (1H Proton and 13C Carbon-NMR) and LC-MS. Amongst the extracts, the ethanolic extracts exhibited stronger cytotoxic potential against the oral cancer cell line (SCC-29B) with an IC50value of 11.27 μg/mL, and that this was too low of a cytotoxicity against the Vero cell line. Although, curcuminoids have also shown a comparable cytotoxic potential against SCC-29B (IC50 value 16.79 μg/mL), it was not as potent against the ethanolic extract, and it was even found to be cytotoxic against healthy cell lines at a very low dose. While considering the isolated compound, bisdemethoxycurcumin, it also possessed a cytotoxic potential against the prostate cancer cell line (DU-145) (IC50 value of 93.28 μg/mL), but was quite safe for the healthy cell line in comparison to doxorubicin. Full article
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Communication
Antioxidant Potential of Flower Extracts from Centaurea spp. Depends on Their Content of Phenolics, Flavonoids and Free Amino Acids
Molecules 2021, 26(24), 7465; https://doi.org/10.3390/molecules26247465 - 09 Dec 2021
Viewed by 573
Abstract
Scientists intensely search for new sources of antioxidants, perceived as important health-promoting agents. Some species of the large genus Centaurea provide raw materials for the pharmaceutical and cosmetic industries, as well as produce edible flowers. This is the first study that determines the [...] Read more.
Scientists intensely search for new sources of antioxidants, perceived as important health-promoting agents. Some species of the large genus Centaurea provide raw materials for the pharmaceutical and cosmetic industries, as well as produce edible flowers. This is the first study that determines the content of total polyphenols, flavonoids, reducing sugars, free amino acids and the antioxidant potential in the flower extracts of C. nigra L., C. orientalis L. and C. phrygia L. The total polyphenol and flavonoid content is the highest in the extract of C. orientalis, and the lowest in that of C. phrygia. Similarly, C. orientalis shows the greatest scavenging activity on DPPH (1,1-diphenyl-2-picryl-hydrazyl), ABTS [2,2′-azobis(3-ethylbenzothiazoline-6-sulfonate)] and Fe3+ reducing power assays, whereas the lowest activity is found for C. phrygia. The highest content of reducing sugars is found in C. nigra, while C. orientalis has the highest levels of free amino acids. We find a strong positive correlation between total phenolics and flavonoids and the antioxidant capacity of all three Centaurea species. Moreover, the content of free amino acids strongly and positively correlates with the levels of total phenolics and flavonoids, antioxidant activity assessed by DPPH and ABTS assays and Fe3+ reducing power. Summing up, C. orientalis exhibits the strongest antioxidant potential of the investigated Centaurea species. This species could potentially be a natural source of antioxidant substances for the pharmacy, cosmetics and food industries. The content of free amino acids may be used as a marker of the antioxidant status of Centaurea species. Full article
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Article
Tetrandrine Suppresses Human Brain Glioblastoma GBM 8401/luc2 Cell-Xenografted Subcutaneous Tumors in Nude Mice In Vivo
Molecules 2021, 26(23), 7105; https://doi.org/10.3390/molecules26237105 - 24 Nov 2021
Viewed by 339
Abstract
Tetrandrine (TET), a bisbenzylisoquinoline (BBI) alkaloid, is isolated from the plant Stephania tetrandra S. Moore and has a wide range of biological activity, including anticancer properties in vitro and in vivo. At first, we established a luciferase-expressing stable clone that was named GBM [...] Read more.
Tetrandrine (TET), a bisbenzylisoquinoline (BBI) alkaloid, is isolated from the plant Stephania tetrandra S. Moore and has a wide range of biological activity, including anticancer properties in vitro and in vivo. At first, we established a luciferase-expressing stable clone that was named GBM 8401/luc2 cells. Herein, the primary results indicated that TET reduced the total cell viability and induced cell apoptosis in GBM 8401/luc2 human glioblastoma cells. However, there is no available information showing that TET suppresses glioblastoma cells in vivo. Thus, we investigated the effects and mechanisms of TET on a GBM 8401/luc2 cell-generated tumor in vivo. After the tumor volume reached 100–120 mm3 in subcutaneously xenografted nude mice, all of the mice were randomly divided into three groups: Group I was treated with phosphate-buffered solution (PBS) containing 0.1% dimethyl sulfoxide, Group II with 25 mg/kg of TET, and Group III with 50 mg/kg of TET. All mice were given the oral treatment of PBS or TET by gavage for 21 days, and the body weight and tumor volumes were recorded every 5 days. After treatment, individual tumors, kidneys, livers, and spleens were isolated from each group. The results showed that TET did not affect the body weights, but it significantly decreased the tumor volumes. The TET treatment at 50 mg/kg had a two-fold decrease in tumor volumes than that at 25 mg/kg when compared to the control. TET decreased the total photon flux, and treatment with TET at 50 mg/kg had a lower total photon flux than that at 25 mg/kg, as measured by a Xenogen IVIS imaging system. Moreover, the higher TET treatment had lower tumor volumes and weights than those of the lower dose. The apoptosis-associated protein expression in the tumor section was examined by immunohistochemical analysis, and the results showed that TET treatment reduced the levels of c-FLIP, MCL-1, and XIAP but increased the signals of cleaved-caspase-3, -8, and -9. Furthermore, the hematoxylin and eosin (H & E) staining of kidney, liver, and spleen tissues showed no significant difference between the TET-treated and control groups. Overall, these observations demonstrated that TET suppressed subcutaneous tumor growth in a nude-mice model via the induction of cell apoptosis. Full article
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Article
Molecular Mechanism of Antioxidant and Anti-Inflammatory Effects of Omega-3 Fatty Acids in Perilla Seed Oil and Rosmarinic Acid Rich Fraction Extracted from Perilla Seed Meal on TNF-α Induced A549 Lung Adenocarcinoma Cells
Molecules 2021, 26(22), 6757; https://doi.org/10.3390/molecules26226757 - 09 Nov 2021
Viewed by 527
Abstract
Industrially, after the removal of oil from perilla seeds (PS) by screw-type compression, the large quantities of residual perilla seed meal (PSM) becomes non-valuable waste. Therefore, to increase the health value and price of PS and PSM, we focused on the biological effects [...] Read more.
Industrially, after the removal of oil from perilla seeds (PS) by screw-type compression, the large quantities of residual perilla seed meal (PSM) becomes non-valuable waste. Therefore, to increase the health value and price of PS and PSM, we focused on the biological effects of perilla seed oil (PSO) and rosmarinic acid-rich fraction (RA-RF) extracted from PSM for their role in preventing oxidative stress and inflammation caused by TNF-α exposure in an A549 lung adenocarcinoma culture model. The A549 cells were pretreated with PSO or RA-RF and followed by TNF-α treatment. We found that PSO and RA-RF were not toxic to TNF-α-induced A549 cells. Both extracts significantly decreased the generation of reactive oxygen species (ROS) in this cell line. The mRNA expression levels of IL-1β, IL-6, IL-8, TNF-α, and COX-2 were significantly decreased by the treatment of PSO and RA-RF. The Western blot indicated that the expression of MnSOD, FOXO1, and NF-κB and phosphorylation of JNK were also significantly diminished by PSO and RA-RF treatment. The results demonstrated that PSO and RA-RF act as antioxidants to scavenge TNF-α induced ROS levels, resulting in decreased the expression of MnSOD, FOXO1, NF-κB and JNK signaling pathway in a human lung cell culture exposed to TNF-α. Full article
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Article
Solvent Mixture Optimization in the Extraction of Bioactive Compounds and Antioxidant Activities from Garlic (Allium sativum L.)
Molecules 2021, 26(19), 6026; https://doi.org/10.3390/molecules26196026 - 04 Oct 2021
Viewed by 525
Abstract
Garlic is a health promoter that has important bioactive compounds. The bioactive extraction is an important step in the analysis of constituents present in plant preparations. The purpose of this study is to optimize the extraction with the best proportion of solvents to [...] Read more.
Garlic is a health promoter that has important bioactive compounds. The bioactive extraction is an important step in the analysis of constituents present in plant preparations. The purpose of this study is to optimize the extraction with the best proportion of solvents to obtain total phenolic compounds (TPC) and thiosulfinates (TS) from dried garlic powder, and evaluate the antioxidant activities of the optimized extracts. A statistical mixture simplex axial design was used to evaluate the effect of solvents (water, ethanol, and acetone), as well as mixtures of these solvents, after two ultrasound extraction cycles of 15 min. Results showed that solvent mixtures with a high portion of water and pure water were efficient for TPC and TS recovery through this extraction procedure. According to the regression model computed, the most significant solvent mixtures to obtain high TPC and TS recovery from dried garlic powder are, respectively, the binary mixture with 75% water and 25% acetone and pure water. These optimized extracts presented oxygen radical absorbance capacity. Pure water was better for total antioxidant capacity, and the binary mixture of water–acetone (75:25) was better for DPPH scavenging activity. These optimized extracts can be used for industrial and research applications. Full article
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Article
Topical Nano Clove/Thyme Gel against Genetically Identified Clinical Skin Isolates: In Vivo Targeting Behavioral Alteration and IGF-1/pFOXO-1/PPAR γ Cues
Molecules 2021, 26(18), 5608; https://doi.org/10.3390/molecules26185608 - 15 Sep 2021
Viewed by 976
Abstract
Antimicrobial resistance is a dramatic global threat; however, the slow progress of new antibiotic development has impeded the identification of viable alternative strategies. Natural antioxidant-based antibacterial approaches may provide potent therapeutic abilities to effectively block resistance microbes’ pathways. While essential oils (EOs) have [...] Read more.
Antimicrobial resistance is a dramatic global threat; however, the slow progress of new antibiotic development has impeded the identification of viable alternative strategies. Natural antioxidant-based antibacterial approaches may provide potent therapeutic abilities to effectively block resistance microbes’ pathways. While essential oils (EOs) have been reported as antimicrobial agents, its application is still limited ascribed to its low solubility and stability characters; additionally, the related biomolecular mechanisms are not fully understood. Hence, the study aimed to develop a nano-gel natural preparation with multiple molecular mechanisms that could combat bacterial resistance in an acne vulgaris model. A nano-emulgel of thyme/clove EOs (NEG8) was designed, standardized, and its antimicrobial activity was screened in vitro and in vivo against genetically identified skin bacterial clinical isolates (Pseudomonas stutzeri, Enterococcus faecium and Bacillus thuringiensis). As per our findings, NEG8 exhibited bacteriostatic and potent biofilm inhibition activities. An in vivo model was also established using the commercially available therapeutic, adapalene in contra genetically identified microorganism. Improvement in rat behavior was reported for the first time and NEG8 abated the dermal contents/protein expression of IGF-1, TGF-β/collagen, Wnt/β-catenin, JAK2/STAT-3, NE, 5-HT, and the inflammatory markers; p(Ser536) NF-κBp65, TLR-2, and IL-6. Moreover, the level of dopamine, protective anti-inflammatory cytokine, IL-10 and PPAR-γ protein were enhanced, also the skin histological structures were improved. Thus, NEG8 could be a future potential topical clinical alternate to synthetic agents, with dual merit mechanism as bacteriostatic antibiotic action and non-antibiotic microbial pathway inhibitor. Full article
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Article
Antinociceptive Synergism of Pomegranate Peel Extract and Acetylsalicylic Acid in an Animal Pain Model
Molecules 2021, 26(18), 5434; https://doi.org/10.3390/molecules26185434 - 07 Sep 2021
Viewed by 566
Abstract
Several modern drugs, which are derived from traditional herbal medicine are used in contemporary pharmacotherapy. Currently, the study of drug–plant interactions in pain has increased in recent years, looking for greater efficacy of the drug and reduce side effects. The antinociception induced by [...] Read more.
Several modern drugs, which are derived from traditional herbal medicine are used in contemporary pharmacotherapy. Currently, the study of drug–plant interactions in pain has increased in recent years, looking for greater efficacy of the drug and reduce side effects. The antinociception induced by intragastric co-administration of the combination of pomegranate peel extract (PoPEx) and acetylsalicylic acid (ASA) was assessed using the isobolographic analysis in formalin test (nociceptive and inflammatory pain). The effective dose that produced 30% of antinociception (ED30) was calculated for both drugs from the logarithmic dose–response curves, subsequently generating a curve with the combination on fixed proportions (1:1) of PoPEx and ASA. Through isobolographic analysis, this experimental ED30 was compared with the calculated theoretical additive ED30. The result was a synergistic interaction, the experimental ED30 was significantly smaller (p < 0.05) than the theoretical ED30. The antinociceptive mechanism of the PoPEx-ASA combination involves the l-Arginine/NO/cGMP pathway, antioxidant capacity, and high content of total phenols. These findings suggest that an interaction between PoPEx and ASA could be a novel treatment for inflammatory and nociceptive pain, also diminish the secondary reactions of ASA. Full article
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Article
Insight into the Way the Content of Biologically Active Compounds in Meadowsweet Inflorescences (Filipendula ulmaria (L.) Maxim.) Is Shaped by Phytosociological Habitats
Molecules 2021, 26(17), 5172; https://doi.org/10.3390/molecules26175172 - 26 Aug 2021
Viewed by 523
Abstract
A collection of herbs from the natural environment remains not only a source of raw material but also provides evidence of chemical differentiation of the local populations. This work aimed at performing a phytosociological analysis of seven different stands of meadowsweet (Filipendula [...] Read more.
A collection of herbs from the natural environment remains not only a source of raw material but also provides evidence of chemical differentiation of the local populations. This work aimed at performing a phytosociological analysis of seven different stands of meadowsweet (Filipendula ulmaria (L.) Maxim.) occurrence. A determination of total phenolic compounds and salicylates and the antioxidant activity of dried meadowsweet inflorescences (Flos ulmariae) was also performed. Active chemical compounds in F. ulmaria inflorescences were related to chemotype and diversified between investigated populations. Geographical distance and variation in phytosociological locations affected chemical composition in different ways, shaping the content of biochemical compounds crucial for herbal material quality. The obtained results can be a valuable indicator for Nexo and Baligród populations, which are good genetic material for research, breeding, and cultivation due to their biochemical composition, especially with respect to salicylates, as major compounds of determining market quality of Flos ulmariae. Full article
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Article
Bioactive Betalain Extracts from Cactus Pear Fruit Pulp, Beetroot Tubers, and Amaranth Leaves
Molecules 2021, 26(16), 5012; https://doi.org/10.3390/molecules26165012 - 18 Aug 2021
Viewed by 816
Abstract
Natural food items and the additional benefits they provide have received considerable attention in recent years. Betalains are nutritious pigments which have valuable biological properties, e.g., antioxidant and free radical scavenging activity. In this study, aqueous betalain extracts were obtained from different coloured [...] Read more.
Natural food items and the additional benefits they provide have received considerable attention in recent years. Betalains are nutritious pigments which have valuable biological properties, e.g., antioxidant and free radical scavenging activity. In this study, aqueous betalain extracts were obtained from different coloured cactus pears (purple, red/pink, and orange), amaranth, and beetroot, with and without the addition of ascorbic acid, microwave-heated, and freeze-dried and subsequently analysed by thin layer chromatography (TLC). Beetroot samples without the addition of ascorbic acid (AA) had lower phenols, flavonoids, and ascorbic acid content than beetroot samples extracted with the addition of AA. Amaranth had significantly higher contents of antioxidants than all the other plants. Results for phenolic compounds showed that there were no significant differences between cactus pear cultivars, however, significant differences were seen between the two beetroot samples (microwave-heated with and without AA) as well as amaranth. For flavonoid compounds, amaranth had significantly higher values than all other samples. The lowest flavonoid content was found in beetroot without AA (0.49 mgCE/g). For ascorbic acid, significant differences were noticed between amaranth (71.71 mg/100 g) and samples from cactus pear and beetroot. TLC results showed that purple and red cactus pear samples had the most vivid colours, a reflection of the high betacyanin and betaxanthin contents in the cultivars. Moreover, extracts from cactus pear, beetroot, and amaranth were classified according to a decision tree which was designed by the Code of Federal Regulations/Food Additives Regulation of the EU. The classification of betalain pigment extracts as colouring foods was achieved through enrichment factor calculations and the colourant decision tree. The results showed that the betalain pigment extraction method used is inexpensive, time-saving, energy-saving, non-toxic, and chemical solvent free and yields high concentrations of betalains. Full article
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Article
Combination of Selenium and UVA Radiation Affects Growth and Phytochemicals of Broccoli Microgreens
Molecules 2021, 26(15), 4646; https://doi.org/10.3390/molecules26154646 - 31 Jul 2021
Cited by 1 | Viewed by 623
Abstract
Addition of selenium or application of ultraviolet A (UVA) radiation for crop production could be an effective way of producing phytochemical-rich food. This study was conducted to investigate the effects of selenium and UVA radiation, as well as their combination on growth and [...] Read more.
Addition of selenium or application of ultraviolet A (UVA) radiation for crop production could be an effective way of producing phytochemical-rich food. This study was conducted to investigate the effects of selenium and UVA radiation, as well as their combination on growth and phytochemical contents in broccoli microgreens. There were three treatments: Se (100 μmol/L Na2SeO3), UVA (40 μmol/m2/s) and Se + UVA (with application of Se and UVA). The control (CK) was Se spraying-free and UVA radiation-free. Although treatment with Se or/and UVA inhibited plant growth of broccoli microgreens, results showed that phytochemical contents increased. Broccoli microgreens under the Se treatment had higher contents of total soluble sugars, total phenolic compounds, total flavonoids, ascorbic acid, Fe, and organic Se and had lower Zn content. The UVA treatment increased the contents of total chlorophylls, total soluble proteins, total phenolic compounds, and FRAP. However, the Se + UVA treatment displayed the most remarkable effect on the contents of total anthocyanins, glucoraphanin, total aliphatic glucosinolates, and total glucosinolates; here, significant interactions between Se and UVA were observed. This study provides valuable insights into the combinational selenium and UVA for improving the phytochemicals of microgreens grown in an artificial lighting plant factory. Full article
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Article
Employment of Phenolic Compounds from Olive Vegetation Water in Broiler Chickens: Effects on Gut Microbiota and on the Shelf Life of Breast Fillets
Molecules 2021, 26(14), 4307; https://doi.org/10.3390/molecules26144307 - 16 Jul 2021
Viewed by 655
Abstract
Olive vegetation water (OVW) is a by-product with a noticeable environmental impact; however, its polyphenols may be reused food and feed manufacture as high-value ingredients with antioxidant/antimicrobial activities. The effect of dietary supplementation with OVW polyphenols on the gut microbiota, carcass and breast [...] Read more.
Olive vegetation water (OVW) is a by-product with a noticeable environmental impact; however, its polyphenols may be reused food and feed manufacture as high-value ingredients with antioxidant/antimicrobial activities. The effect of dietary supplementation with OVW polyphenols on the gut microbiota, carcass and breast quality, shelf life, and lipid oxidation in broiler chickens has been studied. Chicks were fed diets supplemented with crude phenolic concentrate (CPC) obtained from OVW (220 and 440 mg/kg phenols equivalent) until reaching commercial size. Cloacal microbial community (rRNA16S sequencing) was monitored during the growth period. Breasts were submitted to culture-dependent and -independent microbiological analyses during their shelf-life. Composition, fatty acid concentration, and lipid oxidation of raw and cooked thawed breasts were measured. Growth performance and gut microbiota were only slightly affected by the dietary treatments, while animal age influenced the cloacal microbiota. The supplementation was found to reduce the shelf life of breasts due to the growth of spoilers. Chemical composition and lipid oxidation were not affected. The hydroxytyrosol (HT) concentration varied from 178.6 to 292.4 ug/kg in breast muscle at the beginning of the shelf-life period. The identification of HT in meat demonstrates that the absorption and metabolism of these compounds was occurring efficiently in the chickens. Full article
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Article
Impact of Peels Extracts from an Italian Ancient Tomato Variety Grown under Drought Stress Conditions on Vascular Related Dysfunction
Molecules 2021, 26(14), 4289; https://doi.org/10.3390/molecules26144289 - 15 Jul 2021
Cited by 2 | Viewed by 936
Abstract
Background: Tomato by-products contain a great variety of biologically active substances and represent a significant source of natural antioxidant supplements of the human diet. The aim of the work was to compare the antioxidant properties of a by-product from an ancient Tuscan tomato [...] Read more.
Background: Tomato by-products contain a great variety of biologically active substances and represent a significant source of natural antioxidant supplements of the human diet. The aim of the work was to compare the antioxidant properties of a by-product from an ancient Tuscan tomato variety, Rosso di Pitigliano (RED), obtained by growing plants in normal conditions (-Ctr) or in drought stress conditions (-Ds) for their beneficial effects on vascular related dysfunction. Methods: The antioxidant activity and total polyphenol content (TPC) were measured. The identification of bioactive compounds of tomato peel was performed by HPLC. HUVEC were pre-treated with different TPC of RED-Ctr or RED-Ds, then stressed with H2O2. Cell viability, ROS production and CAT, SOD and GPx activities were evaluated. Permeation of antioxidant molecules contained in RED across excised rat intestine was also studied. Results: RED-Ds tomato peel extract possessed higher TPC than compared to RED-Ctr (361.32 ± 7.204 mg vs. 152.46 ± 1.568 mg GAE/100 g fresh weight). All extracts were non-cytotoxic. Two hour pre-treatment with 5 µg GAE/mL from RED-Ctr or RED-Ds showed protection from H2O2-induced oxidative stress and significantly reduced ROS production raising SOD and CAT activity (* p < 0.05 and ** p < 0.005 vs. H2O2, respectively). The permeation of antioxidant molecules contained in RED-Ctr or RED-Ds across excised rat intestine was high with non-significant difference between the two RED types (41.9 ± 9.6% vs. 26.6 ± 7.8%). Conclusions: RED-Ds tomato peel extract represents a good source of bioactive molecules, which protects HUVECs from oxidative stress at low concentration. Full article
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Article
Compound A Increases Cell Infiltration in Target Organs of Acute Graft-versus-Host Disease (aGVHD) in a Mouse Model
Molecules 2021, 26(14), 4237; https://doi.org/10.3390/molecules26144237 - 12 Jul 2021
Viewed by 712
Abstract
Systemic steroids are used to treat acute graft-versus-host disease (aGVHD) caused by allogenic bone marrow transplantation (allo-BMT); however, their prolonged use results in complications. Hence, new agents for treating aGVHD are required. Recently, a new compound A (CpdA), with anti-inflammatory activity and reduced [...] Read more.
Systemic steroids are used to treat acute graft-versus-host disease (aGVHD) caused by allogenic bone marrow transplantation (allo-BMT); however, their prolonged use results in complications. Hence, new agents for treating aGVHD are required. Recently, a new compound A (CpdA), with anti-inflammatory activity and reduced side effects compared to steroids, has been identified. Here, we aimed to determine whether CpdA can improve the outcome of aGVHD when administered after transplantation in a mouse model (C57BL/6 in B6D2F1). After conditioning with 9Gy total body irradiation, mice were infused with bone marrow (BM) cells and splenocytes from either syngeneic (B6D2F1) or allogeneic (C57BL/6) donors. The animals were subsequently treated (3 days/week) with 7.5 mg/kg CpdA from day +15 to day +28; the controls received 0.9% NaCl. Thereafter, the incidence and severity of aGVHD in aGVHD target organs were analyzed. Survival and clinical scores did not differ significantly; however, CpdA-treated animals showed high cell infiltration in the target organs. In bulk mixed lymphocyte reactions, CpdA treatment reduced the cell proliferation and expression of inflammatory cytokines and chemokines compared to controls, whereas levels of TNF, IL-23, chemokines, and chemokine receptors increased. CpdA significantly reduced proliferation in vitro but increased T cell infiltration in target organs. Full article
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Article
GC-MS Metabolic Profile and α-Glucosidase-, α-Amylase-, Lipase-, and Acetylcholinesterase-Inhibitory Activities of Eight Peach Varieties
Molecules 2021, 26(14), 4183; https://doi.org/10.3390/molecules26144183 - 09 Jul 2021
Cited by 3 | Viewed by 1115
Abstract
The inhibition of certain digestive enzymes by target food matrices represents a new approach in the treatment of socially significant diseases. Proving the ability of fruits to inhibit such enzymes can support the inclusion of specific varieties in the daily diets of patients [...] Read more.
The inhibition of certain digestive enzymes by target food matrices represents a new approach in the treatment of socially significant diseases. Proving the ability of fruits to inhibit such enzymes can support the inclusion of specific varieties in the daily diets of patients with diabetes, obesity, Alzheimer’s disease, etc., providing them with much more than just valuable micro- and macromolecules. The current study aimed atidentifying and comparing the GC-MS metabolic profiles of eight peach varieties (“Filina”, “Ufo 4, “Gergana”, “Laskava”, “July Lady”, “Flat Queen”, “Evmolpiya”, and “Morsiani 90”) grown in Bulgaria (local and introduced) and to evaluate the inhibitory potential of their extracts towards α-glucosidase, α-amylase, lipase, and acetylcholinesterase. In order to confirm samples’ differences or similarities, principal component analysis (PCA) and hierarchical cluster analysis (HCA) were also applied to the identified metabolites. The results provide important insights into the metabolomic profiles of the eight peach varieties and represent a first attempt to characterize the peels of the peach varieties with respect to α-glucosidase-, α-amylase-, lipase-, and acetylcholinesterase-inhibitory activities. All of the studied peach extracts displayed inhibitory activity towards α-glucosidase (IC50: 125–757 mg/mL) and acetylcholinesterase (IC50: 60–739 mg/mL), but none of them affected α-amylase activity. Five of the eight varieties showed inhibitory activity towards porcine pancreatic lipase (IC50: 24–167 mg/mL). The obtained results validate the usefulness of peaches and nectarines as valuable sources of natural agents beneficial for human health, although further detailed investigation should be performed in order to thoroughly identify the enzyme inhibitors responsible for each activity. Full article
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Article
Antioxidant Effects and Phytochemical Properties of Seven Taiwanese Cirsium Species Extracts
Molecules 2021, 26(13), 3935; https://doi.org/10.3390/molecules26133935 - 28 Jun 2021
Viewed by 595
Abstract
In the present investigation, we compared the radical-scavenging activities and phenolic contents of seven Taiwanese Cirsium species with a spectrophotometric method. We further analyzed their phytochemical profiles with high-performance liquid chromatography–photodiode array detection (HPLC–DAD). We found that the flower part of Cirsium japonicum [...] Read more.
In the present investigation, we compared the radical-scavenging activities and phenolic contents of seven Taiwanese Cirsium species with a spectrophotometric method. We further analyzed their phytochemical profiles with high-performance liquid chromatography–photodiode array detection (HPLC–DAD). We found that the flower part of Cirsium japonicum var. australe (CJF) showed the best radical-scavenging activities against 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), and the hypochlorite ion, for which the equivalents were 6.44 ± 0.17 mg catechin/g, 54.85 ± 0.66 mmol Trolox/g and 418.69 ± 10.52 mmol Trolox/g respectively. CJF also had the highest contents of total phenolics (5.23 ± 0.20 mg catechin/g) and phenylpropanoids (29.73 ± 0.72 mg verbascoside/g). According to the Pearson’s correlation coefficient, there was a positive correlation between the total phenylpropanoid content and ABTS radical-scavenging activities (r = 0.979). The radical-scavenging activities of the phenylpropanoids are closely related to their reducing power (r = 0.986). HPLC chromatograms obtained in validated HPLC conditions confirm that they have different phytochemical profiles by which they can be distinguished. Only CJF contained silicristin (0.66 ± 0.03 mg/g) and silydianin (9.13 ± 0.30 mg/g). CJF contained the highest contents of apigenin (5.56 ± 0.09 mg/g) and diosmetin (2.82 ± 0.10 mg/g). Among the major constituents, silicristin had the best radical-scavenging activities against DPPH (71.68 ± 0.66 mg catechin/g) and ABTS (3.01 ± 0.01 mmol Trolox/g). However, diosmetin had the best reducing power and radical-scavenging activity against the hypochlorite anion (41.57 ± 1.14 mg mmol Trolox/g). Finally, we found that flavonolignans (especial silicristin and silydianin) and diosmetin acted synergistically in scavenging radicals. Full article
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Article
Antiviral Activity of Metabolites from Peruvian Plants against SARS-CoV-2: An In Silico Approach
Molecules 2021, 26(13), 3882; https://doi.org/10.3390/molecules26133882 - 25 Jun 2021
Cited by 1 | Viewed by 1209
Abstract
(1) Background: The COVID-19 pandemic lacks treatments; for this reason, the search for potential compounds against therapeutic targets is still necessary. Bioinformatics tools have allowed the rapid in silico screening of possible new metabolite candidates from natural resources or repurposing known ones. Thus, [...] Read more.
(1) Background: The COVID-19 pandemic lacks treatments; for this reason, the search for potential compounds against therapeutic targets is still necessary. Bioinformatics tools have allowed the rapid in silico screening of possible new metabolite candidates from natural resources or repurposing known ones. Thus, in this work, we aimed to select phytochemical candidates from Peruvian plants with antiviral potential against three therapeutical targets of SARS-CoV-2. (2) Methods: We applied in silico technics, such as virtual screening, molecular docking, molecular dynamics simulation, and MM/GBSA estimation. (3) Results: Rutin, a compound present in Peruvian native plants, showed affinity against three targets of SARS-CoV-2. The molecular dynamics simulation demonstrated the high stability of receptor–ligand systems during the time of the simulation. Our results showed that the Mpro-Rutin system exhibited higher binding free energy than PLpro-Rutin and N-Rutin systems through MM/GBSA analysis. (4) Conclusions: Our study provides insight on natural metabolites from Peruvian plants with therapeutical potential. We found Rutin as a potential candidate with multiple pharmacological properties against SARS-CoV-2. Full article
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Article
Kinetic Study on Chlorophyll and Antioxidant Activity from Polyscias fruticosa (L.) Harms Leaves via Microwave-Assisted Extraction
Molecules 2021, 26(12), 3761; https://doi.org/10.3390/molecules26123761 - 21 Jun 2021
Viewed by 941
Abstract
Polyscias fruticosa (L.) leaves contain significant bioactive compounds with high antioxidant activity such as chlorophylls, total polyphenols, etc. but these have still been underutilized. In this study, the kinetics of chlorophyll and antioxidant activity extraction from P. fruticosa leaves by microwave-assisted extraction (MAE) [...] Read more.
Polyscias fruticosa (L.) leaves contain significant bioactive compounds with high antioxidant activity such as chlorophylls, total polyphenols, etc. but these have still been underutilized. In this study, the kinetics of chlorophyll and antioxidant activity extraction from P. fruticosa leaves by microwave-assisted extraction (MAE) were investigated. Microwave power was 300, 450, or 600 (W); the ratio of material/solvent varied from 1:40 to 1:80 (g/mL). In this study, the second-order kinetic model successfully predicted the change of chlorophyll and antioxidant activity during MAE. The increase of microwave power or/and the solvent amount increased saturated extraction efficiency and the extraction rate constant. However, the saturated concentration of chlorophyll and antioxidant activity increased with the increment of microwave power and the decrease in solvent amount. Full article
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Article
Antioxidant, Anti-Inflammatory, and Anti-Diabetic Activity of Phenolic Acids Fractions Obtained from Aerva lanata (L.) Juss.
Molecules 2021, 26(12), 3486; https://doi.org/10.3390/molecules26123486 - 08 Jun 2021
Viewed by 919
Abstract
Many plants that are commonly used in folk medicine have multidirectional biological properties confirmed by scientific research. One of them is Aerva lanata (L.) Juss. (F. Amaranthaceae). It is widely used, but there are very few scientific data about its chemical composition and [...] Read more.
Many plants that are commonly used in folk medicine have multidirectional biological properties confirmed by scientific research. One of them is Aerva lanata (L.) Juss. (F. Amaranthaceae). It is widely used, but there are very few scientific data about its chemical composition and pharmacological activity. The aim of the present study was to investigate the chemical composition of phenolic acid (PA)-rich fractions isolated from methanolic extracts of A. lanata (L.) Juss. herb using the liquid/liquid extraction method and their potential antioxidant, anti-inflammatory, and anti-diabetic properties. The free PA fraction (FA), the PA fraction (FB) released after acid hydrolysis, and the PA fraction (FC) obtained after alkaline hydrolysis were analysed using liquid chromatography/electrospray ionization triple quadrupole mass spectrometry (LC-ESI-MS/MS). The phenolic profile of each sample showed a high concentration of PAs and their presence in A. lanata (L.) Juss. herb mainly in bound states. Thirteen compounds were detected and quantified in all samples, including some PAs that had not been previously detected in this plant species. Bioactivity assays of all fractions revealed high 2,2-diphenyl-1-picrylhydrazyl (DPPH) (2.85 mM Trolox equivalents (TE)/g) and 2,2-azino-bis-3(ethylbenzthiazoline-6-sulphonic acid) (ABTS•+) (2.88 mM TE/g) scavenging activity. Fraction FB definitely exhibited not only the highest antiradical activity but also the strongest xanthine oxidase (XO) (EC50 = 1.77 mg/mL) and lipoxygenase (LOX)(EC50 = 1.88 mg/mL) inhibitory potential. The fraction had the best anti-diabetic properties, i.e., mild inhibition of α-amylase (EC50 = 7.46 mg/mL) and strong inhibition of α-glucosidase (EC50 = 0.30 mg/mL). The activities of all analysed samples were strongly related to the presence of PA compounds and the total PA content. Full article
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Article
Biochemical Studies in Perfundates and Homogenates of Isolated Porcine Kidneys after Flushing with Zinc or Zinc–Prolactin Modified Preservation Solution Using a Static Cold Storage Technique
Molecules 2021, 26(11), 3465; https://doi.org/10.3390/molecules26113465 - 07 Jun 2021
Cited by 1 | Viewed by 806
Abstract
Zinc is an effective anti-inflammatory and antioxidant trace element. The aim of this study was to analyse the protective effect of zinc and zinc–prolactin systems as additives of preservation solutions in the prevention of nephron damage caused during ischemia. The study used a [...] Read more.
Zinc is an effective anti-inflammatory and antioxidant trace element. The aim of this study was to analyse the protective effect of zinc and zinc–prolactin systems as additives of preservation solutions in the prevention of nephron damage caused during ischemia. The study used a model for storing isolated porcine kidneys in Biolasol®. The solution was modified with the addition of Zn at a dose of 1 µg/L and Zn: 1 µg/L with prolactin (PRL): 0.1 µg/L. After 2 h and 48 h of storage, the levels of alanine aminotransferase, aspartate aminotransferase, lactate dehydrogenase, sodium, potassium, creatinine and total protein were determined. Zinc added to the Biolasol® composition at a dose of 1 µg/L showed minor effectiveness in the protection of nephrons. In turn, Zn2+ added to Biolasol + PRL (PRL: 0.1 µg/L) acted as a prolactin inhibitor. We do not recommend the addition of Zn(II) (1 µg/L) and Zn(II) (1 µg/L) + PRL (0.1 µg/L) to the Biolasol solution. Full article
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Article
Ameliorative Potential of Hydroethanolic Leaf Extract of Parquetina nigrescens on d-Galactose-Induced Testicular Injury
Molecules 2021, 26(11), 3424; https://doi.org/10.3390/molecules26113424 - 05 Jun 2021
Viewed by 1113
Abstract
Background: There is an increasing need for botanicals to be used as an alternative and complementary medicine in the management of male infertility. Male infertility has been a major health/social challenge to people all over the world. This study, therefore, investigated the ameliorative [...] Read more.
Background: There is an increasing need for botanicals to be used as an alternative and complementary medicine in the management of male infertility. Male infertility has been a major health/social challenge to people all over the world. This study, therefore, investigated the ameliorative potential of hydroethanolic leaf extract of Parquetina nigrescens (HELEPN) against d-galactose-induced testicular injury. Methods: Thirty male Wistar rats were randomly allotted into six groups (n = 5). Group I (Normal control), Group II (300 mg/kg b.w. d-galactose), Group III and IV (250 and 500 mg/kg b.w. HELEPN, respectively), Group V and VI (both received 300 mg/kg b.w. of d-galactose with 250 and 500 mg/kg b.w of HELEPN, respectively). d-galactose administration started two weeks prior to HELEPN treatment which lasted for six weeks. All assays were carried out using established protocols. Results: Administration of HELEPN at 250mg/kg and 500mg/kg concomitantly with d-galactose improved paired and relative testicular weights, levels of gonadotropins (LH and FSH) and testosterone, and poor sperm quality. HELEPN treatment reduced the levels of oxidative stress biomarkers (MDA, 8-OHDG, and AGEs) and inflammatory response (TNF-alpha and NO) to normal, as well as restoring the reduced activities of antioxidant enzymes (glutathione peroxidase, superoxide dismutase, and catalase). In addition, HELEPN treatment mitigated testicular DNA fragmentation and down-regulated caspase 3-activities. HELEPN at 500 mg/kg was observed to have the greatest ameliorative effect. Conclusion: HELEPN protects against d-galactose-induced testicular injury through antioxidative, anti-inflammatory, and antiapoptotic mechanisms. Full article
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Article
Antimutagenic, Cytoprotective and Antioxidant Properties of Ficus deltoidea Aqueous Extract In Vitro
Molecules 2021, 26(11), 3287; https://doi.org/10.3390/molecules26113287 - 29 May 2021
Cited by 1 | Viewed by 897
Abstract
Ficus deltoidea var. deltoidea is used as traditional medicine for diabetes, inflammation, and nociception. However, the antimutagenic potential and cytoprotective effects of this plant remain unknown. In this study, the mutagenic and antimutagenic activities of F. deltoidea aqueous extract (FDD) on both Salmonella [...] Read more.
Ficus deltoidea var. deltoidea is used as traditional medicine for diabetes, inflammation, and nociception. However, the antimutagenic potential and cytoprotective effects of this plant remain unknown. In this study, the mutagenic and antimutagenic activities of F. deltoidea aqueous extract (FDD) on both Salmonella typhimurium TA 98 and TA 100 strains were assessed using Salmonella mutagenicity assay (Ames test). Then, the cytoprotective potential of FDD on menadione-induced oxidative stress was determined in a V79 mouse lung fibroblast cell line. The ferric-reducing antioxidant power (FRAP) assay was conducted to evaluate FDD antioxidant capacity. Results showed that FDD (up to 50 mg/mL) did not exhibit a mutagenic effect on either TA 98 or TA 100 strains. Notably, FDD decreased the revertant colony count induced by 2-aminoanthracene in both strains in the presence of metabolic activation (p < 0.05). Additionally, pretreatment of FDD (50 and 100 µg/mL) demonstrated remarkable protection against menadione-induced oxidative stress in V79 cells significantly by decreasing superoxide anion level (p < 0.05). FDD at all concentrations tested (12.5–100 µg/mL) exhibited antioxidant power, suggesting the cytoprotective effect of FDD could be partly attributed to its antioxidant properties. This report highlights that F. deltoidea may provide a chemopreventive effect on mutagenic and oxidative stress inducers. Full article
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Article
Comprehensive Evaluation of Late Season Peach Varieties (Prunus persica L.): Fruit Nutritional Quality and Phytochemicals
Molecules 2021, 26(9), 2818; https://doi.org/10.3390/molecules26092818 - 10 May 2021
Cited by 1 | Viewed by 975
Abstract
Peaches are one of the most preferred seasonal fruits, and a reliable source of nutrients. They possess biologically active substances that largely differ among varieties. Hence, revealing the potential of several late season peaches is of present interest. Three commonly consumed varieties (“Flat [...] Read more.
Peaches are one of the most preferred seasonal fruits, and a reliable source of nutrients. They possess biologically active substances that largely differ among varieties. Hence, revealing the potential of several late season peaches is of present interest. Three commonly consumed varieties (“Flat Queen”; “Evmolpiya”; “Morsiani 90”) were studied in terms of nutritive and phytochemical content, as well as antioxidant activity with the use of reliable spectrophotometric and High Performance Liquid Chromatographic (HPLC) methods. An analysis of the soil was also made. The phytochemical data were subjected to principal component analysis in order to evaluate their relationship. The “Morsiani 90” variety had the highest minerals concentration (2349.03 mg/kg fw), total carbohydrates (16.21 g/100 g fw), and α-tocopherol (395.75 µg/100 g fresh weight (fw)). Similar amounts of TDF (approx. 3 g/100 g fw) were reported for all three varieties. “Flat Queen’s” peel extract was the richest in monomeric anthocyanins (2279.33 µg cyanidin-3-glucoside (C3GE)/100 g fw). The “Morsiani 90” variety extracts had the highest antioxidant potential, defined by 2,2-diphenil-1-picrylhydrazyl (DPPH), ferric-reducing antioxidant power (FRAP) and cupric ion-reducing antioxidant capacity (CUPRAC) assays. Full article
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Article
LC-HRMS Profiling and Antidiabetic, Anticholinergic, and Antioxidant Activities of Aerial Parts of Kınkor (Ferulago stellata)
Molecules 2021, 26(9), 2469; https://doi.org/10.3390/molecules26092469 - 23 Apr 2021
Cited by 4 | Viewed by 780
Abstract
Kınkor (Ferulago stellata) is Turkish medicinal plant species and used in folk medicine against some diseases. As far as we know, the data are not available on the biological activities and chemical composition of this medicinal plant. In this study, [...] Read more.
Kınkor (Ferulago stellata) is Turkish medicinal plant species and used in folk medicine against some diseases. As far as we know, the data are not available on the biological activities and chemical composition of this medicinal plant. In this study, the phytochemical composition; some metabolic enzyme inhibition; and antidiabetic, anticholinergic, and antioxidant activities of this plant were assessed. In order to evaluate the antioxidant activity of evaporated ethanolic extract (EEFS) and lyophilized water extract (WEFS) of kınkor (Ferulago stellata), some putative antioxidant methods such as DPPH· scavenging activity, ABTS•+ scavenging activity, ferric ions (Fe3+) reduction method, cupric ions (Cu2+) reducing capacity, and ferrous ions (Fe2+)-binding activities were separately performed. Furthermore, ascorbic acid, BHT, and α-tocopherol were used as the standard compounds. Additionally, the main phenolic compounds that are responsible for antioxidant abilities of ethanol and water extracts of kınkor (Ferulago stellata) were determined by liquid chromatography-high-resolution mass spectrometry (LC-HRMS). Ethanol and water extracts of kınkor (Ferulago stellata) demonstrated effective antioxidant abilities when compared to standards. Moreover, ethanol extract of kınkor (Ferulago stellata) demonstrated IC50 values of 1.772 μg/mL against acetylcholinesterase (AChE), 33.56 ± 2.96 μg/mL against α-glycosidase, and 0.639 μg/mL against α-amylase enzyme respectively. Full article
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Article
Phytochemical Analysis, Pharmacological and Safety Evaluations of Halophytic Plant, Salsola cyclophylla
Molecules 2021, 26(8), 2384; https://doi.org/10.3390/molecules26082384 - 20 Apr 2021
Cited by 2 | Viewed by 762
Abstract
Salsola cyclophylla, an edible halophyte, is traditionally used for inflammation and pain. To confirm the claimed anti-inflammatory and analgesic properties, a detailed study on respective pharmacological actions was undertaken. The activities are contemplated to arise from its phytoconstituents. The LC-MS analysis of [...] Read more.
Salsola cyclophylla, an edible halophyte, is traditionally used for inflammation and pain. To confirm the claimed anti-inflammatory and analgesic properties, a detailed study on respective pharmacological actions was undertaken. The activities are contemplated to arise from its phytoconstituents. The LC-MS analysis of S. cyclophylla 95% aqueous-ethanolic extract revealed the presence of 52 compounds belonging to phenols, flavonoids, coumarins, and aliphatics class. A high concentration of Mn, Fe, and Zn was detected by atomic absorption spectroscopic analysis. The ethyl acetate extract showed the highest flavonoid contents (5.94 ± 0.04 mg/g, Quercetin Equivalents) and Fe2+-chelation (52%) potential with DPPH radicals-quenching IC50 at 1.35 ± 0.16 mg/mL, while the aqueous ethanolic extract exhibited maximum phenolics contents (136.08 ± 0.12 mg/g, gallic acid equivalents) with DPPH scavenging potential at IC50 0.615 ± 0.06 mg/mL. Aqueous ethanolic extract and standard quercetin DPPH radicals scavenging’s were equal potent at 10 mg/mL concentrations. The aqueous ethanolic extract showed highest analgesic effect with pain reduction rates 89.86% (p = 0.03), 87.50% (p < 0.01), and 99.66% (p = 0.0004) after 60, 90, and 120 min, respectively. Additionally, aqueous ethanolic extract exhibited the highest anti-inflammation capacity at 41.07% (p < 0.0001), 34.51% (p < 0.0001), and 24.82% (p < 0.0001) after 2, 3, and 6 h of extract’s administration, respectively. The phytochemical constituents, significant anti-oxidant potential, remarkable analgesic, and anti-inflammatory bioactivities of extracts supported the traditionally claimed anti-inflammatory and analgesic plant activities. Full article
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Article
UHPLC-DAD Characterization of Origanum vulgare L. from Atacama Desert Andean Region and Antioxidant, Antibacterial and Enzyme Inhibition Activities
Molecules 2021, 26(7), 2100; https://doi.org/10.3390/molecules26072100 - 06 Apr 2021
Cited by 2 | Viewed by 947
Abstract
The Lamiaceae family is an important source of species among medicinal plants highly valued for their biological properties and numerous uses in folk medicine. Origanum is one of the main genera that belong to this family. The purpose of the study was to [...] Read more.
The Lamiaceae family is an important source of species among medicinal plants highly valued for their biological properties and numerous uses in folk medicine. Origanum is one of the main genera that belong to this family. The purpose of the study was to determine the phenolic composition of the Origanum vulgare extract and evaluate the antimicrobial, antioxidant, and inhibitory activities of this species that grows in the Andean region of the Atacama Desert. High-performance liquid chromatography was performed to determine the main phenols. Rosmarinic acid was identified as the predominant phenolic compound in this species (76.01 mg/100 g DW), followed by protocatechuic acid, which to our knowledge, no previous study reported similar concentrations in O. vulgare. The oregano extract exhibited a content of total phenolic (3948 mg GAE/100 g DW) and total flavonoid (593 mg QE/100 g DW) with a higher DPPH antioxidant activity (IC50 = 40.58 µg/mL), compared to the same species grown under other conditions. Furthermore, it was found to inhibit α-glucosidase activity with an IC50 value (7.11 mg/mL) lower than acarbose (129.32 mg/mL). Pseudomonas syringae and Pantoea agglomerans (both MIC 0.313 mg/mL and MBC 1.25 mg/mL) were the bacteria most susceptible to oregano extract with the lowest concentration necessary to inhibit bacterial growth. These results open the door for the potential use of this plant to manage chronic diseases, and they expand the knowledge of the species cultivated in arid environmental conditions. Full article
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Article
Modulation of Renal Function in a Metabolic Syndrome Rat Model by Antioxidants in Hibiscus sabdariffa L.
Molecules 2021, 26(7), 2074; https://doi.org/10.3390/molecules26072074 - 04 Apr 2021
Cited by 1 | Viewed by 1080
Abstract
Metabolic syndrome (MS) is the association of three or more pathologies among which obesity, hypertension, insulin resistance, dyslipidemia, and diabetes are included. It causes oxidative stress (OS) and renal dysfunction. Hibiscus sabdariffa L. (HSL) is a source of natural antioxidants that may control [...] Read more.
Metabolic syndrome (MS) is the association of three or more pathologies among which obesity, hypertension, insulin resistance, dyslipidemia, and diabetes are included. It causes oxidative stress (OS) and renal dysfunction. Hibiscus sabdariffa L. (HSL) is a source of natural antioxidants that may control the renal damage caused by the MS. The objective of this work was to evaluate the effect of a 2% HSL infusion on renal function in a MS rat model induced by the administration of 30% sucrose in drinking water. 24 male Wistar rats were divided into 3 groups: Control rats, MS rats and MS + HSL rats. MS rats had increased body weight, systolic blood pressure, triglycerides, insulin, HOMA index, and leptin (p ≤ 0.04). Renal function was impaired by an increase in perfusion pressure in the isolated and perfused kidney, albuminuria (p ≤ 0.03), and by a decrease in clearance of creatinine (p ≤ 0.04). The activity of some antioxidant enzymes including the superoxide dismutase isoforms, peroxidases, glutathione peroxidase, glutathione-S-transferase was decreased (p ≤ 0.05). Lipoperoxidation and carbonylation were increased (p ≤ 0.001). The nitrates/nitrites ratio, total antioxidant capacity, glutathione levels and vitamin C were decreased (p ≤ 0.03). The treatment with 2% HSL reversed these alterations. The results suggest that the treatment with 2% HSL infusion protects renal function through its natural antioxidants which favor an improved renal vascular response. The infusion contributes to the increase in the glomerular filtration rate, by promoting an increase in the enzymatic and non-enzymatic antioxidant systems leading to a decrease in OS and reestablishing the normal renal function. Full article
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Article
Statistical Optimization of Flavonoid and Antioxidant Recovery from Macerated Chinese and Malaysian Lotus Root (Nelumbo nucifera) Using Response Surface Methodology
Molecules 2021, 26(7), 2014; https://doi.org/10.3390/molecules26072014 - 01 Apr 2021
Viewed by 575
Abstract
In this study, the combination of parameters required for optimal extraction of anti-oxidative components from the Chinese lotus (CLR) and Malaysian lotus (MLR) roots were carefully investigated. Box–Behnken design was employed to optimize the pH (X1: 2–3), extraction time (X2 [...] Read more.
In this study, the combination of parameters required for optimal extraction of anti-oxidative components from the Chinese lotus (CLR) and Malaysian lotus (MLR) roots were carefully investigated. Box–Behnken design was employed to optimize the pH (X1: 2–3), extraction time (X2: 0.5–1.5 h) and solvent-to-sample ratio (X3: 20–40 mL/g) to obtain a high flavonoid yield with high % DPPHsc free radical scavenging and Ferric-reducing power assay (FRAP). The analysis of variance clearly showed the significant contribution of quadratic model for all responses. The optimal conditions for both Chinese lotus (CLR) and Malaysian lotus (MLR) roots were obtained as: CLR: X1 = 2.5; X2 = 0.5 h; X3 = 40 mL/g; MLR: X1 = 2.4; X2 = 0.5 h; X3 = 40 mL/g. These optimum conditions gave (a) Total flavonoid content (TFC) of 0.599 mg PCE/g sample and 0.549 mg PCE/g sample, respectively; (b) % DPPHsc of 48.36% and 29.11%, respectively; (c) FRAP value of 2.07 mM FeSO4 and 1.89 mM FeSO4, respectively. A close agreement between predicted and experimental values was found. The result obtained succinctly revealed that the Chinese lotus exhibited higher antioxidant and total flavonoid content when compared with the Malaysia lotus root at optimum extraction condition. Full article
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Article
Antiangiogenic and Antioxidant In Vitro Properties of Hydroethanolic Extract from açaí (Euterpe oleracea) Dietary Powder Supplement
Molecules 2021, 26(7), 2011; https://doi.org/10.3390/molecules26072011 - 01 Apr 2021
Cited by 3 | Viewed by 760
Abstract
The Euterpe oleracea fruit (açaí) is a promising source of polyphenols with health-promoting properties. To our knowledge, few studies have focused on the influence of açaí phytochemicals on angiogenesis, with a significant impact on cancer. This study aimed at investigating the phytochemical profile [...] Read more.
The Euterpe oleracea fruit (açaí) is a promising source of polyphenols with health-promoting properties. To our knowledge, few studies have focused on the influence of açaí phytochemicals on angiogenesis, with a significant impact on cancer. This study aimed at investigating the phytochemical profile of a purple açaí hydroethanolic extract (AHE) obtained from a commercial dietary powder supplement by high-performance liquid chromatography coupled to diode array detection and electrospray ionization mass spectrometry, and evaluate its in vitro effects on distinct angiogenic steps during vessel growth and on oxidative markers in human microvascular endothelial cells (HMEC-1). The phenolic profile of AHE revealed the presence of significant levels of anthocyanins, mainly cyanidin-3-O-rutinoside, and other flavonoids with promising health effects. The in vitro studies demonstrated that AHE exerts antiangiogenic activity with no cytotoxic effect. The AHE was able to decrease HMEC-1 migration and invasion potential, as well as to inhibit the formation of capillary-like structures. Additionally, AHE increased antioxidant defenses by upregulating superoxide dismutase and catalase enzymatic activities, accompanied by a reduction in the production of reactive oxygen species. These data bring new insights into the potential application of angiogenic inhibitors present in AHE on the development of novel therapeutic approaches for angiogenesis-dependent diseases. Full article
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Communication
Combined Antimicrobial Effect of Bio-Waste Olive Leaf Extract and Remote Cold Atmospheric Plasma Effluent
Molecules 2021, 26(7), 1890; https://doi.org/10.3390/molecules26071890 - 26 Mar 2021
Cited by 4 | Viewed by 1005
Abstract
A novel strategy involving Olive Leaf Extract (OLE) and Cold Atmospheric Plasma (CAP) was developed as a green antimicrobial treatment. Specifically, we reported a preliminary investigation on the combined use of OLE + CAP against three pathogens, chosen to represent medical and food [...] Read more.
A novel strategy involving Olive Leaf Extract (OLE) and Cold Atmospheric Plasma (CAP) was developed as a green antimicrobial treatment. Specifically, we reported a preliminary investigation on the combined use of OLE + CAP against three pathogens, chosen to represent medical and food industries (i.e., E. coli, S. aureus and L. innocua). The results indicated that a concentration of 100 mg/mL (total polyphenols) in OLE can exert an antimicrobial activity, but still insufficient for a total bacterial inactivation. By using plain OLE, we significantly reduced the growth of Gram positive S. aureus and L. innocua, but not Gram-negative E. coli. Instead, we demonstrated a remarkable decontamination effect of OLE + CAP in E. coli, S. aureus and L. innocua samples after 6 h. This effect was optimally maintained up to 24 h in S. aureus strain. E. coli and L. innocua grew again in 24 h. In the latter strain, OLE alone was most effective to significantly reduce bacterial growth. By further adjusting the parameters of OLE + CAP technology, e.g., OLE amount and CAP exposure, it could be possible to prolong the initial powerful decontamination over a longer time. Since OLE derives from a bio-waste and CAP is a non-thermal technology based on ionized air, we propose OLE + CAP as a potential green platform for bacterial decontamination. As a combination, OLE and CAP can lead to better antimicrobial activity than individually and may replace or complement conventional thermal procedures in food and biomedical industries. Full article
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Communication
Comparison of the Phenolic Compound Profile and Antioxidant Potential of Achillea atrata L. and Achillea millefolium L.
Molecules 2021, 26(6), 1530; https://doi.org/10.3390/molecules26061530 - 11 Mar 2021
Cited by 2 | Viewed by 682
Abstract
In the present study, Achillea atrata L. and A. millefolium L. were compared for the first time with regard to their phenolic compound profile and antioxidant activity by applying the 2,2-diphenyl-picryl hydrazyl radical assay. For this purpose, aerial plant parts were consecutively extracted [...] Read more.
In the present study, Achillea atrata L. and A. millefolium L. were compared for the first time with regard to their phenolic compound profile and antioxidant activity by applying the 2,2-diphenyl-picryl hydrazyl radical assay. For this purpose, aerial plant parts were consecutively extracted with solvents of increasing polarity (dichloromethane, n-butanol, ethyl acetate), revealing that the A. atrata ethyl acetate fraction showed the highest antioxidant activity with an IC50 value of 12.2 ± 0.29 µg/mL compared to 17.0 ± 0.26 µg/mL for A. millefolium. Both species revealed the presence of luteolin, apigenin, centaureidin, and nevadensin exclusively in this most polar fraction, which are known as effective 2,2-diphenyl-picryl hydrazyl radical scavengers. The antioxidant capacity of the aforementioned fractions strikingly correlated with their total phenolic contents, which was highest in the ethyl acetate fraction of A. atrata. Characterization of the metabolite profiles of both Achillea species showed only marginal differences in the presence of key compounds, whereas the concentrations of individual compounds appeared to be species-specific. Our results suggest that A. atrata, based on its compound pattern and bioactivity characteristics, has similar qualities for phytotherapy as A. millefolium. Full article
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Article
Comparison of the Phytochemical Properties, Antioxidant Activity and Cytotoxic Effect on HepG2 Cells in Mongolian and Taiwanese Rhubarb Species
Molecules 2021, 26(5), 1217; https://doi.org/10.3390/molecules26051217 - 25 Feb 2021
Cited by 1 | Viewed by 1548
Abstract
The Mongolian rhubarb—Rheum undulatum L. (RU)—and Rumex crispus L. (RC)—a Taiwanese local rhubarb belonging to the family of Polygonaceae—are principal therapeutic materials in integrative medicine due to their rich quantities of bioactive compounds; however, their phytochemical and antioxidant properties, [...] Read more.
The Mongolian rhubarb—Rheum undulatum L. (RU)—and Rumex crispus L. (RC)—a Taiwanese local rhubarb belonging to the family of Polygonaceae—are principal therapeutic materials in integrative medicine due to their rich quantities of bioactive compounds; however, their phytochemical and antioxidant properties, and anti-cancer activity is poorly investigated. Furthermore, the phytochemical characteristics of both species may be affected by their different geographical distribution and climatic variance. The current study aimed to compare RU with RC extracts in different polarity solvents (n-hexane, ethyl acetate, acetone, ethanol, and water) for their phytochemical contents including the total phenolic content (TPC), total anthraquinone content (TAC), total flavonoid content (TFC), antioxidant and free radical scavenging capacities, and anticancer ability on the HepG2 cell. Except for the n-hexane extract, all of the RU extracts had considerably higher TPCs than RC extracts, ranging from 8.39 to 11.16 mg gallic acid equivalent (GAE) per gram of dry weight, and the TPCs of each extract were also significantly correlated with their antioxidant capacities by ABTS, DPPH, and FRAP assays (p < 0.05). Moreover, there was no remarkable association between the antioxidant capacities and either TACs or TFCs in both the RU and RC extracts. Besides, high-performance liquid chromatography (HPLC) analysis revealed that both the RU and RC extracts contained chrysophanol, emodin, and physcion, and those bioactive compounds were relatively higher in the n-hexane solvent extracts. Additionally, we observed different levels of dose-dependent cytotoxic effects in all the extracts by cell viability assay. Notably, the ethanol extract of RU had a compelling cytotoxic effect with the lowest half-maximum inhibition concentration (IC50-171.94 ± 6.56 µg/mL at 48 h) among the RU extracts than the ethanol extract of RC. Interestingly, the ethanol extract of RU but not RC significantly induced apoptosis in the human liver cancer cell line, HepG2, with a distinct pattern in caspase-3 activation, resulting in increased PARP cleavage and DNA damage. In summary, Mongolian Rhubarb, RU, showed more phytochemical contents, as well as a higher antioxidant capacity and apoptotic effect to HepG2 than RC; thus, it can be exploited for the proper source of natural antioxidants and liver cancer treatment in further investigation. Full article
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Article
Impact of In Vitro Gastrointestinal Digestion on the Bioaccessibility of Phytochemical Compounds from Eight Fruit Juices
Molecules 2021, 26(4), 1187; https://doi.org/10.3390/molecules26041187 - 23 Feb 2021
Cited by 5 | Viewed by 1392
Abstract
Fruits contain a number of useful substances including antioxidants. Their bio-accessibility after passing through the digestive tract is of primary importance when considering their benefits. In this respect, we investigated the effect of in vitro digestion on the phytochemicals of eight fruit juices. [...] Read more.
Fruits contain a number of useful substances including antioxidants. Their bio-accessibility after passing through the digestive tract is of primary importance when considering their benefits. In this respect, we investigated the effect of in vitro digestion on the phytochemicals of eight fruit juices. Freshly prepared juices from pomegranate, orange and grapefruit were used as well as commercially available juices from cherry, black grapes and aloe vera, blackberry and chokeberry, and two types of chokeberry and raspberries. Spectrophotometric and HPLC methods were used in order to analyse the sugar content, the total phenolic (TPC) and flavonoid contents (TFC), anthocyanins, phenolic acids and antioxidant activity. Principle component analysis was used to explain the differentiation among the types of fruit juice. Sugar recovery variation was between 4–41%. The bio-accessibility of TPC ranged from 13.52–26.49% and of flavonoids between 24.25–67.00%. The pomegranate juice and the juice of black grapes and aloe vera kept 58.12 and 50.36% of their initial anthocyanins content, while for the other samples less than 1.10% was established. As a result, a maximum of 30% remaining antioxidant activity was measured for some of the samples, but for most this was less than 10%. In conclusion, fruit juices are a rich source of biologically active substances, but a more detailed analysis of food transformation during digestion is needed. Full article
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Article
Phytochemical Investigation of New Algerian Lichen Species: Physcia Mediterranea Nimis
Molecules 2021, 26(4), 1121; https://doi.org/10.3390/molecules26041121 - 20 Feb 2021
Cited by 1 | Viewed by 808
Abstract
The present study provides new data concerning the chemical characterisation of Physcia mediterranea Nimis, a rare Mediterranean species belonging to the family Physciaceae. The phytochemical screening was carried out using GC-MS, HPLC-ESI-MS-MS, and NMR techniques. Hot extraction of n-hexane was carried out, followed [...] Read more.
The present study provides new data concerning the chemical characterisation of Physcia mediterranea Nimis, a rare Mediterranean species belonging to the family Physciaceae. The phytochemical screening was carried out using GC-MS, HPLC-ESI-MS-MS, and NMR techniques. Hot extraction of n-hexane was carried out, followed by separation of the part insoluble in methanol: wax (WA-hex), from the part soluble in methanol (ME-hex). GC-MS analysis of the ME-hex part revealed the presence of methylbenzoic acids such as sparassol and atraric acid and a diterpene with a kaurene skeleton which has never been detected before in lichen species. Out of all the compounds identified by HPLC-ESI-MS-MS, sixteen compounds are common between WA-hex and ME-hex. Most are aliphatic fatty acids, phenolic compounds and depsides. The wax part is characterised by the presence of atranorin, a depside of high biological value. Proton 1H and carbon 13C NMR have confirmed its identification. Atranol, chloroatranol (depsides compound), Ffukinanolide (sesquiterpene lactones), leprolomin (diphenyl ether), muronic acid (triterpenes), and ursolic acid (triterpenes) have also been identified in ME-hex. The results suggested that Physcia mediterranea Nimis is a valuable source of bioactive compounds that could be useful for several applications as functional foods, cosmetics, and pharmaceuticals. Full article
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Article
Phytochemicals of Conocarpus spp. as a Natural and Safe Source of Phenolic Compounds and Antioxidants
Molecules 2021, 26(4), 1069; https://doi.org/10.3390/molecules26041069 - 18 Feb 2021
Viewed by 754
Abstract
Optimization of the extraction conditions of polyphenolic compounds for different parts of the Damas species, Conocarpus lancifolius and Conocarpus erectus, grown under UAE conditions was studied. The combination of ethanol concentration (50, 75, and 100%), temperature (45, 55, and 65 °C) and [...] Read more.
Optimization of the extraction conditions of polyphenolic compounds for different parts of the Damas species, Conocarpus lancifolius and Conocarpus erectus, grown under UAE conditions was studied. The combination of ethanol concentration (50, 75, and 100%), temperature (45, 55, and 65 °C) and time (1, 2, and 3 h) was used by applying the Response Surface Methodology. The data showed that the extracts (n = 90) contained phenolic compounds, flavonoids, and tannins, and were free of alkaloids. Changing the extraction conditions had a significant effect on the detection of phytosterols, saponins, and glycosides and on the solubility of vanillic acid, p-coumaric acid, sinapic acid, t-ferulic acid, rutin hydrate, protocatechuic acid, quercetin, and flavone. The data reveal that the roots and leaves of C. erectus and the leaves and fruits of C.lancifolius are the most important plant parts from which to extract these compounds. This study draws attention to the unordinary use of Conocarpus spp. as a source of natural food additive. Full article
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Article
Chemical Composition, Antioxidant and Antimicrobial Activity of Raspberry, Blackberry and Raspberry-Blackberry Hybrid Leaf Buds
Molecules 2021, 26(2), 327; https://doi.org/10.3390/molecules26020327 - 10 Jan 2021
Cited by 2 | Viewed by 1165
Abstract
In our investigation, the chemical composition and bioactive potential of leaf buds of raspberry, blackberry, and a raspberry-blackberry hybrid were determined. Antioxidant and antimicrobial properties were tested in water (W), ethanol-water (EW), and glycerol-water (GW) extracts from the buds. These plant organs contain [...] Read more.
In our investigation, the chemical composition and bioactive potential of leaf buds of raspberry, blackberry, and a raspberry-blackberry hybrid were determined. Antioxidant and antimicrobial properties were tested in water (W), ethanol-water (EW), and glycerol-water (GW) extracts from the buds. These plant organs contain relatively large amounts of minerals, especially Fe. The total antioxidant capacity (TAC) measured by the ABTS and DPPH methods ranged from 2.86 to 12.19 and 6.75 to 24.26 mmol per 100 g fresh weight (FW) of buds, respectively. TAC values were generally higher in the raspberry than in the case of blackberry and raspberry-blackberry hybrid extracts. The antioxidant properties of the extracts were strongly positively correlated with their content of total phenolic (TP). No such relationship was noted for ascorbic acid (AA), whose concentration in all extracts was at a similarly low level. Antioxidant properties determined in vitro were confirmed for the GW extract from raspberry leaf buds in biological test based on the growth parameters of Δsod1 Saccharomyces cerevisiae mutant cells in hypertonic medium. The extracts also exhibited strong antibacterial properties against Staphylococcus aureus and Enterococcus faecalis and weaker against Enterobacter aerogenes. The studied leaf buds could be therefore an unconventional source of minerals, natural antioxidants and antibacterial compounds with potential applications in the food, pharmaceutical, and cosmetics industries. Full article
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Article
Myricitrin, a Glycosyloxyflavone in Myrica esculenta Bark Ameliorates Diabetic Nephropathy via Improving Glycemic Status, Reducing Oxidative Stress, and Suppressing Inflammation
Molecules 2021, 26(2), 258; https://doi.org/10.3390/molecules26020258 - 06 Jan 2021
Cited by 5 | Viewed by 1014
Abstract
The present study evaluated the therapeutic potential of myricitrin (Myr), a glycosyloxyflavone extracted from Myrica esculenta bark, against diabetic nephropathy. Myr exhibited a significant hypoglycemic effect in high fat-fed and a single low-dose streptozotocin-induced type 2 diabetic (T2D) rats. Myr was found to [...] Read more.
The present study evaluated the therapeutic potential of myricitrin (Myr), a glycosyloxyflavone extracted from Myrica esculenta bark, against diabetic nephropathy. Myr exhibited a significant hypoglycemic effect in high fat-fed and a single low-dose streptozotocin-induced type 2 diabetic (T2D) rats. Myr was found to improve glucose uptake by the skeletal muscle via activating IRS-1/PI3K/Akt/GLUT4 signaling in vitro and in vivo. Myr significantly attenuated high glucose (HG)-induced toxicity in NRK cells and in the kidneys of T2D rats. In this study, hyperglycemia caused nephrotoxicity via endorsing oxidative stress and inflammation resulting in the induction of apoptosis, fibrosis, and inflammatory damages. Myr was found to attenuate oxidative stress via scavenging/neutralizing oxidative radicals and improving endogenous redox defense through Nrf-2 activation in both in vitro and in vivo systems. Myr was also found to attenuate diabetes-triggered renal inflammation via suppressing NF-κB activation. Myr inhibited hyperglycemia-induced apoptosis and fibrosis in renal cells evidenced by the changes in the expressions of the apoptotic and fibrotic factors. The molecular docking predicted the interactions between Myr and different signal proteins. An in silico absorption, distribution, metabolism, excretion, and toxicity (ADMET) study predicted the drug-likeness character of Myr. Results suggested the possibility of Myr to be a potential therapeutic agent for diabetic nephropathy in the future. Full article
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Article
Assessment of the Biological Activity and Phenolic Composition of Ethanol Extracts of Pomegranate (Punica granatum L.) Peels
Molecules 2020, 25(24), 5916; https://doi.org/10.3390/molecules25245916 - 14 Dec 2020
Cited by 5 | Viewed by 1155
Abstract
Pomegranate (Punica granatum L.) is a rich source of constituents with confirmed strong biological activities. However, pomegranate peel, which encompasses approximately 30–40% of its weight, is treated as a biological waste. The aim of this paper was to evaluate the potential of [...] Read more.
Pomegranate (Punica granatum L.) is a rich source of constituents with confirmed strong biological activities. However, pomegranate peel, which encompasses approximately 30–40% of its weight, is treated as a biological waste. The aim of this paper was to evaluate the potential of pomegranate peel extracts and to propose its functional properties that can be used for development of functional products. Eight ethanol extracts of pomegranate peels (PPEs) were characterized by use of direct infusion quadrupole-time of flight (Q-TOF), and afterwards tested on their antioxidant, antibacterial and antiproliferative activities. Mass spectrometry analysis revealed that the most prevalent compounds in pomegranate peels were punicalagin, granatin and their derivatives. Analysed extracts had high total phenolic contents that ranged from 5766.44 to 10599.43 mg GAE/100 g, and strong antioxidant activity (7551.31–7875.42 and 100.25–176.60 μmol TE/100 g for DPPH and FRAP assays, respectively). The results of biological activity assays showed that all PPEs possessed antibacterial activity, and that S. aureus was the most sensitive specie with minimum inhibitory concentration and minimum bactericidal concentrations ranging from 0.8 to 6.4 mg/mL. Additionally, the analysis of antiproliferative activity revealed high potency of PPEs, as the IC50 values ranged from 0.132 mg/mL to 0.396 mg/mL. Multivariate analysis pointed out the most discriminative metabolites for antioxidant or antiproliferative activity. Overall, the pomegranate peel confirmed to be a highly valuable source of bioactive compounds that could be used to improve the food functional characteristics. Full article
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Article
Effects of Supplementary Blue and UV-A LED Lights on Morphology and Phytochemicals of Brassicaceae Baby-Leaves
Molecules 2020, 25(23), 5678; https://doi.org/10.3390/molecules25235678 - 02 Dec 2020
Cited by 6 | Viewed by 874
Abstract
Brassicaceae baby-leaves are good source of functional phytochemicals. To investigate how Chinese kale and pak-choi baby-leaves in response to different wavebands of blue (430 nm and 465 nm) and UV-A (380 nm and 400 nm) LED, the plant growth, glucosinolates, antioxidants, and minerals [...] Read more.
Brassicaceae baby-leaves are good source of functional phytochemicals. To investigate how Chinese kale and pak-choi baby-leaves in response to different wavebands of blue (430 nm and 465 nm) and UV-A (380 nm and 400 nm) LED, the plant growth, glucosinolates, antioxidants, and minerals were determined. Both agronomy traits and phytochemical contents were significantly affected. Blue and UV-A light played a predominant role in increasing the plant biomass and morphology, as well as the contents of antioxidant compounds (vitamin C, vitamin E, phenolics, and individual flavonols), the antioxidant activity (DPPH and FRAP), and the total glucosinolates accumulation. In particular, four light wavebands significantly decreased the content of progoitrin, while 400 nm UV-A light and 430 nm blue light were efficient in elevating the contents of sinigrin and glucobrassicin in Chinese kale. Meanwhile, 400 nm UV-A light was able to increase the contents of glucoraphanin, sinigrin, and glucobrassicin in pak-choi. From the global view of heatmap, blue lights were more efficient in increasing the yield and phytochemical levels of two baby-leaves. Full article
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Article
Inclusion Complexes of Concentrated Orange Oils and β-Cyclodextrin: Physicochemical and Biological Characterizations
Molecules 2020, 25(21), 5109; https://doi.org/10.3390/molecules25215109 - 03 Nov 2020
Cited by 3 | Viewed by 830
Abstract
Concentrated orange oils (5x, 10x, 20x) are ingredients used in different industries as components of flavors and aromas due to their great organoleptic qualities. This research focuses on the search for alternative uses for their application through encapsulation in inclusion complexes with β-cyclodextrin [...] Read more.
Concentrated orange oils (5x, 10x, 20x) are ingredients used in different industries as components of flavors and aromas due to their great organoleptic qualities. This research focuses on the search for alternative uses for their application through encapsulation in inclusion complexes with β-cyclodextrin (β–CD). Inclusion complexes of concentrated orange oils (COEO) and β–CD were developed by the co-precipitated method in ratios of 4:96, 12:88, and 16:84 (w/w, COEO: β–CD). The best powder recovery was in the ratio 16:84 for the three oils, with values between 82% and 84.8%. The 20x oil in relation 12:88 showed the highest entrapment efficiency (89.5%) with 102.3 mg/g of β–CD. The FT-IR analysis may suggest an interaction between the oil and the β–CD. The best antioxidant activity was observed in the ratio 12:88 for the three oils. The antifungal activity was determined for all the inclusion complexes, and the 10x fraction showed the highest inhibition at a concentration of 10 mg/mL in ratios 12:88 and 16:84. Antibacterial activity was determined by the minimum inhibitory concentration (MIC) and was found at a concentration of 1.25 mg/mL in ratios 12:88 and 16:84 for 5x and 20x oils. Full article
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Article
Rhizopus oligosporus and Lactobacillus plantarum Co-Fermentation as a Tool for Increasing the Antioxidant Potential of Grass Pea and Flaxseed Oil-Cake Tempe
Molecules 2020, 25(20), 4759; https://doi.org/10.3390/molecules25204759 - 16 Oct 2020
Cited by 3 | Viewed by 744
Abstract
Tempe-type fermentation originating from Indonesia can enhance the antioxidant activity of plant material. However, this biological potential depends on substrates and applied microorganisms. This study aimed to determine whether co-fermentation with Rhizopus oligosporus and Lactobacillus plantarum improved antioxidant activity of tempe obtained from [...] Read more.
Tempe-type fermentation originating from Indonesia can enhance the antioxidant activity of plant material. However, this biological potential depends on substrates and applied microorganisms. This study aimed to determine whether co-fermentation with Rhizopus oligosporus and Lactobacillus plantarum improved antioxidant activity of tempe obtained from grass pea seeds with flaxseed oil-cake addition (up to 30%). For this purpose, substances reacting with Folin–Ciocalteu reagent and free radicals scavenging potential were measured in water-soluble fractions and dialysates from simulated in vitro digestion. Additionally, the water-soluble phenolic profile was estimated. The higher level of water-extractable compounds with antioxidant activity was determined in co-fermentation products than in fungal fermentation products. Moreover, the fermentation process with the use of L. plantarum contributed to a greater accumulation of some phenolic acids (gallic acid, protocatechuic acid) in tempe without having a negative effect on the levels of other phenolic compounds determined in fungal fermented tempe. During in vitro digestion simulating the human digestive tract, more antioxidant compounds were released from products obtained after co-fermentation than fungal fermentation. An addition of 20% flaxseed oil-cake and the application of bacterial–fungal co-fermentation, can be considered as an alternative tool to enhance the antioxidant parameters of grass pea tempe. Full article
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Article
Flavonoid Profiles of Two New Approved Romanian Ocimum Hybrids
Molecules 2020, 25(19), 4573; https://doi.org/10.3390/molecules25194573 - 07 Oct 2020
Cited by 3 | Viewed by 992
Abstract
Basil (Ocimum spp.) is a traditional herbal medicine abundant in antioxidants such as phenolic compounds. As part of a diet, this herb is proved to have some roles in decreasing the risk of cancer, and in the treatment of inflammation and neurodegenerative [...] Read more.
Basil (Ocimum spp.) is a traditional herbal medicine abundant in antioxidants such as phenolic compounds. As part of a diet, this herb is proved to have some roles in decreasing the risk of cancer, and in the treatment of inflammation and neurodegenerative diseases. This study aims to explore the total phenolic and flavonoid content of two new basil hybrids growing in Romania, namely “Aromat de Buzau” (AB) and “Macedon” (MB). The antioxidant capacity of those two species was also analyzed by DPPH and cyclic voltammetry. Six different flavonoids, such as catechin (+), rutin, hyperoside, naringin, naringenin, and genistein, were separated, identified, and quantified by HPLC–DAD chromatography, for the first time, from romanian basil hybrids. The main flavonoid of the extracts was found to be naringin which is present in the highest amount (26.18 mg/kg) in “Aromat de Buzau” (O. basilicum) methanolic extract. These results suggest that dietary intake of these new hybrids can be a source of antioxidant compounds. Full article
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Article
Comparison of the Partial Structure and Antioxidant Activity of Polysaccharides from Two Species of Chinese Truffles
Molecules 2020, 25(18), 4345; https://doi.org/10.3390/molecules25184345 - 22 Sep 2020
Viewed by 944
Abstract
Truffles are world-renowned premium commodities. Due to their unique aroma and rarity, the price of truffles has always been very high. In this study, Diethylaminoethyl anion exchange chromatography and gel filtration were employed for polysaccharide purification from two different species of Chinese truffles. [...] Read more.
Truffles are world-renowned premium commodities. Due to their unique aroma and rarity, the price of truffles has always been very high. In this study, Diethylaminoethyl anion exchange chromatography and gel filtration were employed for polysaccharide purification from two different species of Chinese truffles. Three polysaccharide fractions were obtained from Tuber panzhihuanense and referred to as TPZ-NP, TPZ-I, and TPZ-II. Additionally, two polysaccharide fractions were purified from T. pseudoexcavatum (TPD-NP and TPD-I). The results of structural elucidation indicated that the polysaccharide from different species showed different monosaccharide composition and linkage units, as well as molecular weight. Two of the polysaccharide fractions with the highest yield, TPZ-I and TPD-I, were chosen for biological testing. The results indicated that both fractions displayed antioxidant properties through mediation of the intestinal cellular antioxidant defense system, which could protect cultured intestinal cells from oxidative stress-induced damage and cell viability suppression. The TPD-I fraction showed stronger antioxidant effects, which may be due to the difference in structure. Further study on the structure-activity relationship is needed to be done. Full article
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Article
Production and Characterization of Antioxidative Hydrolysates and Peptides from Corn Gluten Meal Using Papain, Ficin, and Bromelain
Molecules 2020, 25(18), 4091; https://doi.org/10.3390/molecules25184091 - 07 Sep 2020
Cited by 9 | Viewed by 1111
Abstract
There has been a growing interest in developing natural antioxidants with high efficiency and low cost. Bioactive protein hydrolysates could be a potential source of natural and safer antioxidants. The objectives of this study were to hydrolyze corn gluten meal using three plant-derived [...] Read more.
There has been a growing interest in developing natural antioxidants with high efficiency and low cost. Bioactive protein hydrolysates could be a potential source of natural and safer antioxidants. The objectives of this study were to hydrolyze corn gluten meal using three plant-derived proteases, namely papain, ficin, and bromelain, to produce antioxidative hydrolysates and peptides and to characterize the antioxidant performances using both chemical assays and a ground meat model. The optimum hydrolysis time for papain was 3 h, and for ficin and bromelain was 4 h. The hydrolysates were further separated by sequential ultrafiltration to 5 hydrolysate fractions named F1 to F5 from low molecular weight (MW) (<1 kDa) to high MW range (>10 kDa), which were further characterized for TPC, free radical scavenging capacity against DPPH and ABTS, and metal chelating activity. The fraction F4 produced by papain (CH-P4), F1 produced by ficin (CH-F1), and F3 produced by bromelain (CH-B3) showed the strongest antioxidant activity and yield, respectively. These three fractions were incorporated into ground pork to determine their inhibition effects on lipid oxidation during a 16-day storage period. The inhibition effect was enhanced with the addition of higher amount of hydrolysate (e.g., 1000 vs. 500 mg/kg). The CH-P4 reduced lipid oxidation in ground meat by as much as 30.45%, and CH-B3 reduced oxidation by 27.2% at the same level, but the inhibition was only 13.83% with 1000 mg/kg of CH-F1. The study demonstrated that CGM protein hydrolysates and peptides could be used as naturally derived antioxidant in retarding lipid oxidation and improving product storage stability. Full article
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Review

Jump to: Research

Review
A Narrative Review on the Phytochemistry, Pharmacology and Therapeutic Potentials of Clinacanthus nutans (Burm. f.) Lindau Leaves as an Alternative Source of Future Medicine
Molecules 2022, 27(1), 139; https://doi.org/10.3390/molecules27010139 - 27 Dec 2021
Viewed by 518
Abstract
The application of natural products and supplements has expanded tremendously over the past few decades. Clinacanthus nutans (C. nutans), which is affiliated to the Acanthaceae family, has recently caught the interest of researchers from the countries of subtropical Asia due to [...] Read more.
The application of natural products and supplements has expanded tremendously over the past few decades. Clinacanthus nutans (C. nutans), which is affiliated to the Acanthaceae family, has recently caught the interest of researchers from the countries of subtropical Asia due to its medicinal uses in alternative treatment for skin infection conditions due to insect bites, microorganism infections and cancer, as well as for health well-being. A number of bioactive compounds from this plant’s extract, namely phenolic compounds, sulphur containing compounds, sulphur containing glycosides compounds, terpens-tripenoids, terpens-phytosterols and chlorophyll-related compounds possess high antioxidant activities. This literature search yielded about one hundred articles which were then further documented, including the valuable data and findings obtained from all accessible electronic searches and library databases. The promising pharmacological activities from C. nutans leaves extract, including antioxidant, anti-cancer, anti-viral, anti-bacterial, anti-fungal, anti-venom, analgesic and anti-nociceptive properties were meticulously dissected. Moreover, the authors also discuss a few of the pharmacological aspect of C. nutans leaves extracts against anti-hyperlipidemia, vasorelaxation and renoprotective activities, which are seldom available from the previously discussed review papers. From the aspect of toxicological studies, controversial findings have been reported in both in-vitro and in-vivo experiments. Thus, further investigations on their phytochemical compounds and their mode of action showing pharmacological activities are required to fully grasp both traditional usage and their suitability for future drugs development. Data related to therapeutic activity and the constituents of C. nutans leaves were searched by using the search engines Google scholar, PubMed, Scopus and Science Direct, and accepting literature reported between 2010 to present. On the whole, this review paper compiles all the available contemporary data from this subtropical herb on its phytochemistry and pharmacological activities with a view towards garnering further interest in exploring its use in cardiovascular and renal diseases. Full article
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Review
Bioactive Compounds of Opuntia spp. Acid Fruits: Micro and Nano-Emulsified Extracts and Applications in Nutraceutical Foods
Molecules 2021, 26(21), 6429; https://doi.org/10.3390/molecules26216429 - 25 Oct 2021
Cited by 1 | Viewed by 499
Abstract
The acid fruit of the "xoconostle" cactus belongs to the genus Opuntia family of cacti. It is used as a functional food for its bioactive compounds. Several studies reported that xoconostle fruits have a high amount of ascorbic acid, betalains, phenols, tannins, and [...] Read more.
The acid fruit of the "xoconostle" cactus belongs to the genus Opuntia family of cacti. It is used as a functional food for its bioactive compounds. Several studies reported that xoconostle fruits have a high amount of ascorbic acid, betalains, phenols, tannins, and flavonoids. These compounds confer antioxidant, antibacterial, anti-inflammatory, and hepatoprotective gastroprotective activity. Xoconostle fruit extracts were tested by in vitro assays where the digestion conditions were simulated to measure their stability. At the same time, the extracts were protected by encapsulation (microencapsulation, multiple emulsions, and nanoemulsions). Applications of encapsulated extracts were probed in various food matrices (edible films, meat products, dairy, and fruit coatings). The xoconostle is a natural source of nutraceutical compounds, and the use of this fruit in the new food could help improve consumers’ health. Full article
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Review
Enzymatic Preparation of Bioactive Peptides Exhibiting ACE Inhibitory Activity from Soybean and Velvet Bean: A Systematic Review
Molecules 2021, 26(13), 3822; https://doi.org/10.3390/molecules26133822 - 23 Jun 2021
Viewed by 746
Abstract
The Angiotensin-I-converting enzyme (ACE) is a peptidase with a significant role in the regulation of blood pressure. Within this work, a systematic review on the enzymatic preparation of Angiotensin-I-Converting Enzyme inhibitory (ACEi) peptides is presented. The systematic review is conducted by following PRISMA [...] Read more.
The Angiotensin-I-converting enzyme (ACE) is a peptidase with a significant role in the regulation of blood pressure. Within this work, a systematic review on the enzymatic preparation of Angiotensin-I-Converting Enzyme inhibitory (ACEi) peptides is presented. The systematic review is conducted by following PRISMA guidelines. Soybeans and velvet beans are known to have high protein contents that make them suitable as sources of parent proteins for the production of ACEi peptides. Endopeptidase is commonly used in the preparation of soybean-based ACEi peptides, whereas for velvet bean, a combination of both endo- and exopeptidase is frequently used. Soybean glycinin is the preferred substrate for the preparation of ACEi peptides. It contains proline as one of its major amino acids, which exhibits a potent significance in inhibiting ACE. The best enzymatic treatments for producing ACEi peptides from soybean are as follows: proteolytic activity by Protease P (Amano-P from Aspergillus sp.), a temperature of 37 °C, a reaction time of 18 h, pH 8.2, and an E/S ratio of 2%. On the other hand, the best enzymatic conditions for producing peptide hydrolysates with high ACEi activity are through sequential hydrolytic activity by the combination of pepsin-pancreatic, an E/S ratio for each enzyme is 10%, the temperature and reaction time for each proteolysis are 37 °C and 0.74 h, respectively, pH for pepsin is 2.0, whereas for pancreatin it is 7.0. As an underutilized pulse, the studies on the enzymatic hydrolysis of velvet bean proteins in producing ACEi peptides are limited. Conclusively, the activity of soybean-based ACEi peptides is found to depend on their molecular sizes, the amino acid residues, and positions. Hydrophobic amino acids with nonpolar side chains, positively charged, branched, and cyclic or aromatic residues are generally preferred for ACEi peptides. Full article
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Review
Medicinal Plants with Anti-Leukemic Effects: A Review
Molecules 2021, 26(9), 2741; https://doi.org/10.3390/molecules26092741 - 07 May 2021
Cited by 2 | Viewed by 1067
Abstract
Leukemia is a leukocyte cancer that is characterized by anarchic growth of immature immune cells in the bone marrow, blood and spleen. There are many forms of leukemia, and the best course of therapy and the chance of a patient’s survival depend on [...] Read more.
Leukemia is a leukocyte cancer that is characterized by anarchic growth of immature immune cells in the bone marrow, blood and spleen. There are many forms of leukemia, and the best course of therapy and the chance of a patient’s survival depend on the type of leukemic disease. Different forms of drugs have been used to treat leukemia. Due to the adverse effects associated with such therapies and drug resistance, the search for safer and more effective drugs remains one of the most challenging areas of research. Thus, new therapeutic approaches are important to improving outcomes. Almost half of the drugs utilized nowadays in treating cancer are from natural products and their derivatives. Medicinal plants have proven to be an effective natural source of anti-leukemic drugs. The cytotoxicity and the mechanisms underlying the toxicity of these plants to leukemic cells and their isolated compounds were investigated. Effort has been made throughout this comprehensive review to highlight the recent developments and milestones achieved in leukemia therapies using plant-derived compounds and the crude extracts from various medicinal plants. Furthermore, the mechanisms of action of these plants are discussed. Full article
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Review
Bioactive Compounds, Antioxidants, and Health Benefits of Sweet Potato Leaves
Molecules 2021, 26(7), 1820; https://doi.org/10.3390/molecules26071820 - 24 Mar 2021
Cited by 8 | Viewed by 1401
Abstract
Sweet potato (Ipomoea batatas) is one of the most important food crops worldwide and its leaves provide a dietary source of nutrients and various bioactive compounds. These constituents of sweet potato leaves (SPL) vary among varieties and play important roles in [...] Read more.
Sweet potato (Ipomoea batatas) is one of the most important food crops worldwide and its leaves provide a dietary source of nutrients and various bioactive compounds. These constituents of sweet potato leaves (SPL) vary among varieties and play important roles in treating and preventing various diseases. Recently, more attentions in health-promoting benefits have led to several in vitro and in vivo investigations, as well as the identification and quantification of bioactive compounds in SPL. Among them, many new compounds have been reported as the first identified compounds from SPL with their dominant bioactivities. This review summarizes the current knowledge of the bioactive compositions of SPL and their health benefits. Since SPL serve as a potential source of micronutrients and functional compounds, they can be further developed as a sustainable crop for food and medicinal industries. Full article
Review
The Wonderful Activities of the Genus Mentha: Not Only Antioxidant Properties
Molecules 2021, 26(4), 1118; https://doi.org/10.3390/molecules26041118 - 20 Feb 2021
Cited by 10 | Viewed by 2040
Abstract
Medicinal plants and their derived compounds have drawn the attention of researchers due to their considerable impact on human health. Among medicinal plants, mint (Mentha species) exhibits multiple health beneficial properties, such as prevention from cancer development and anti-obesity, antimicrobial, anti-inflammatory, anti-diabetic, [...] Read more.
Medicinal plants and their derived compounds have drawn the attention of researchers due to their considerable impact on human health. Among medicinal plants, mint (Mentha species) exhibits multiple health beneficial properties, such as prevention from cancer development and anti-obesity, antimicrobial, anti-inflammatory, anti-diabetic, and cardioprotective effects, as a result of its antioxidant potential, combined with low toxicity and high efficacy. Mentha species are widely used in savory dishes, food, beverages, and confectionary products. Phytochemicals derived from mint also showed anticancer activity against different types of human cancers such as cervix, lung, breast and many others. Mint essential oils show a great cytotoxicity potential, by modulating MAPK and PI3k/Akt pathways; they also induce apoptosis, suppress invasion and migration potential of cancer cells lines along with cell cycle arrest, upregulation of Bax and p53 genes, modulation of TNF, IL-6, IFN-γ, IL-8, and induction of senescence phenotype. Essential oils from mint have also been found to exert antibacterial activities against Bacillus subtilis, Streptococcus aureus, Pseudomonas aeruginosa, and many others. The current review highlights the antimicrobial role of mint-derived compounds and essential oils with a special emphasis on anticancer activities, clinical data and adverse effects displayed by such versatile plants. Full article
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Review
Promising Roles of Alternative Medicine and Plant-Based Nanotechnology as Remedies for Urinary Tract Infections
Molecules 2020, 25(23), 5593; https://doi.org/10.3390/molecules25235593 - 28 Nov 2020
Cited by 5 | Viewed by 1379
Abstract
Urinary tract infections (UTIs) are considered to be the most common infections worldwide, having an incidence rate of 40−60% in women. Moreover, the prevalence of this disorder in adult women is 30 times more than in men. UTIs are usually found in many [...] Read more.
Urinary tract infections (UTIs) are considered to be the most common infections worldwide, having an incidence rate of 40−60% in women. Moreover, the prevalence of this disorder in adult women is 30 times more than in men. UTIs are usually found in many hospitals and clinical practice; as disorders, they are complicated and uncomplicated; in uncomplicated cases, there is no structural or functional abnormality in the urogenital tract. However, obstruction, retention of urine flow and use of catheters increase the complexity. There are several bacteria (e.g., E. coli, Klebsiella pneumoniae, Proteus vulgaris, etc.) successfully residing in the tract. The diagnosis must not only be accurate but rapid, so early detection is an important step in the control of UTIs caused by uropathogens. The treatment of UTIs includes appropriate antimicrobial therapy to control the infection and kill the causal microbes inside the body. A long-time usage of antibiotics has resulted in multidrug resistance causing an impediment in treatment. Thus, alternative, combinatorial medication approaches have given some hope. Available treatments considered Homeopathic, Ayurvedic, Unani, and other herbal-based drugs. There are new upcoming roles of nanoparticles in combating UTIs which needs further validation. The role of medicinal plant-based nanotechnology approaches has shown promising results. Therefore, there must be active research in phyto-based therapies of UTIs, such as Ayurvedic Biology. Full article
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Review
The Impact of Herbal Infusion Consumption on Oxidative Stress and Cancer: The Good, the Bad, the Misunderstood
Molecules 2020, 25(18), 4207; https://doi.org/10.3390/molecules25184207 - 14 Sep 2020
Cited by 5 | Viewed by 1473
Abstract
The release of reactive oxygen species (ROS) and oxidative stress is associated with the development of many ailments, including cardiovascular diseases, diabetes and cancer. The causal link between oxidative stress and cancer is well established and antioxidants are suggested as a protective mechanism [...] Read more.
The release of reactive oxygen species (ROS) and oxidative stress is associated with the development of many ailments, including cardiovascular diseases, diabetes and cancer. The causal link between oxidative stress and cancer is well established and antioxidants are suggested as a protective mechanism against cancer development. Recently, an increase in the consumption of antioxidant supplements was observed globally. The main sources of these antioxidants include fruits, vegetables, and beverage. Herbal infusions are highly popular beverages consumed daily for different reasons. Studies showed the potent antioxidant effects of plants used in the preparation of some herbal infusions. Such herbal infusions represent an important source of antioxidants and can be used as a dietary protection against cancer. However, uncontrolled consumption of herbal infusions may cause toxicity and reduced antioxidant activity. In this review, eleven widely consumed herbal infusions were evaluated for their antioxidant capacities, anticancer potential and possible toxicity. These herbal infusions are highly popular and consumed as daily drinks in different countries. Studies discussed in this review will provide a solid ground for researchers to have better understanding of the use of herbal infusions to reduce oxidative stress and as protective supplements against cancer development. Full article
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