Special Issue "Extraction, Characterization and Pharmacology of Natural Products"

A special issue of Processes (ISSN 2227-9717). This special issue belongs to the section "Biological Processes and Systems".

Deadline for manuscript submissions: closed (31 August 2020) | Viewed by 30282

Special Issue Editors

Special Issue Information

Dear Colleagues,

We are pleased to invite you to submit original articles to the Special Issue entitled "Extraction, Characterization and Pharmacology of Natural Products".

This Special Issue aims to highlight all aspects related to the quality of plant-based products and the effects of manipulation processes. Studies on extract optimization and comparative studies of extraction techniques and their effects on qualitative and quantitative composition and pharmacological profile are encouraged, as well as comparative studies to investigate quality with respect to the variability of natural sources. Also, investigations of the effects of selected steps of the productive chain (from plant growth to final formulation of herbal-based manufactures) on product quality are encouraged.

The goal of this Special Issue is related to the characterization of phytochemical and botanical aspects of plant material-based extracts, with regard to the optimization and validation of analytical methods for the qualitative and quantitative fingerprint of secondary metabolites. Additionally, eco-toxicological evaluations are encouraged in order to investigate the biocompatibility of extracts in multiple biological models.

This Special Issue will explore potential pharmacological applications of medicinal plant-derived extracts. In this regard, in vivo, ex vivo, and in vitro studies are welcome. The main pharmacological topic includes the investigation of extracts’ and isolated metabolites’ activity in relation to safety, quality, and potential applications of plants and derived products as tools for managing human and animal health.

Finally, the effects of chemical and technological processes on biocompatibility are of great interest. In this regard, authors could discuss experimental data reporting intrinsic and production process-induced toxicity. The evaluation of toxicity via in vivo studies, despite being significantly relevant, is not mandatory. Authors could also submit manuscripts reporting preliminary toxicological profiles obtained from in vitro and ex vivo studies, in agreement with world’s recognized ethical principles. Innovative and eco-biocompatible approaches are encouraged as well, with a special emphasis on the modern concept of circular economy.

Prof. Dr. Luigi Menghini
Prof. Dr. Claudio Ferrante
Guest Editors

Manuscript Submission Information

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Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Processes is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2000 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

  • botanical characterization
  • pharmacological activity
  • eco-toxicological fingerprint
  • phytochemistry
  • analytical methods

Published Papers (17 papers)

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Research

Article
Pharmacological Properties and Chemical Profiles of Passiflora foetida L. Extracts: Novel Insights for Pharmaceuticals and Nutraceuticals
Processes 2020, 8(9), 1034; https://doi.org/10.3390/pr8091034 - 24 Aug 2020
Cited by 5 | Viewed by 1763
Abstract
In the present study, Passiflora foetida extracts characterized by different polarities were studied for their phytochemical profile, enzyme inhibitory, and antioxidant potentials. In silico, in vitro and ex vivo studies were also carried out on methanol and water extracts for predicting pharmacokinetics [...] Read more.
In the present study, Passiflora foetida extracts characterized by different polarities were studied for their phytochemical profile, enzyme inhibitory, and antioxidant potentials. In silico, in vitro and ex vivo studies were also carried out on methanol and water extracts for predicting pharmacokinetics and pharmacodynamics. In this regard, neuronal HypoE22 cells, isolated mouse skin tissues, and pathogen dermatophytes strains were exposed to extracts. Emphasis was given to the preventing effects induced by the extracts on hydrogen peroxide-induced alterations of prostaglandin E2 (PGE2), l-dopa, and serotonin. Chemical analysis revealed the presence of similar compounds in infusion and methanolic extracts. The ex vivo studies also showed protective skin properties by P. foetida water and methanol extracts, as evidenced by the decrease of hydrogen peroxide-induced PGE2 level. Additionally, the blunting effects on hydrogen peroxide-induced l-dopa levels are consistent with the anti-tyrosinase effect exerted by both extracts. In silico studies demonstrated the affinity of extracts’ phytochemicals, namely apigenin, chrysoeriol, loliolide, luteolin, quercetin, and vitexin, towards cyclo-oxygenase-2 and tyrosinase. Finally, microbiological tests demonstrated the efficacy of P. foetida methanol and water extracts as anti-mycotic agents against Trichophyton and Arthroderma species, involved in skin inflammation. Hence, P. foetida L. extracts could represent potential sources of pharmaceuticals and nutraceuticals. Full article
(This article belongs to the Special Issue Extraction, Characterization and Pharmacology of Natural Products)
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Article
Saudi Rosmarinus officinalis and Ocimum basilicum L. Polyphenols and Biological Activities
Processes 2020, 8(4), 446; https://doi.org/10.3390/pr8040446 - 10 Apr 2020
Cited by 13 | Viewed by 1692
Abstract
Investigating the polyphenolic profile of natural Rosmarinus officinalis and Ocimum basilicum populations may reveal essential compounds that have biological activities. Natural populations of R. officinalis and O. basilicum in Northern Riyadh were investigated by HPLC-DAD analyses. Several polyphenols, including rosmarinic acid, gentisic acid, [...] Read more.
Investigating the polyphenolic profile of natural Rosmarinus officinalis and Ocimum basilicum populations may reveal essential compounds that have biological activities. Natural populations of R. officinalis and O. basilicum in Northern Riyadh were investigated by HPLC-DAD analyses. Several polyphenols, including rosmarinic acid, gentisic acid, 3,4-dihydroxyphenylacetic acid, rutoside, and others, out of 38 screened were confirmed. Rosmarinic acid was the major polyphenol in both of R. officinalis and O. basilicum. R. officinalis methanolic leaf extracts contained other phenols such as gentisic acid while O. basilicum contained also 3,4-dihydroxyphenylacetic acid and rutoside as well as others. R. officinalis showed higher antioxidant activities than O. basilicum using 2,2-diphenyl-1-picrylhydrazyl (DPPH), ferric reducing antioxidant power (FRAP), and β-carotene bleaching assays. These higher activities are associated with a higher composition of rosmarinic acid in leaf extracts. The antioxidant activities of O. basilicum were attributed to identified phenols of rosmarinic acid, 3,4-dihydroxyphenylacetic acid, and rutoside. There were antiproliferative and cytotoxic activities of leaf extracts, as well as identified polyphenols, against several cancer cells. These activities were attributed to the accumulation of necrotic and apoptotic cells in treated cancer cells with leaf extracts as well as identified polyphenols. The antibacterial and antifungal activities of leaf extracts were mainly attributed to 3,4-dihydroxyphenylacetic acid and rutoside in O. basilicum and rosmarinic acid and caffeic acid in R. officinalis. This study proved that R. officinalis and O. basilicum natural populations might be considered as promising sources of natural polyphenols with biological activities. Full article
(This article belongs to the Special Issue Extraction, Characterization and Pharmacology of Natural Products)
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Article
Antidiabetic and Antilipidemic Activity of Root Extracts of Salacia oblonga against Streptozotocin-Induced Diabetes in Wistar Rats
Processes 2020, 8(3), 301; https://doi.org/10.3390/pr8030301 - 05 Mar 2020
Cited by 2 | Viewed by 1260
Abstract
Salacia oblonga is used to treat diabetes, hypocholesteremia, gonorrhea, rheumatism, asthma, inflammation, oxidative stress, etc. In the present study, the antidiabetic activity of S. oblonga methanolic root extracts collected from three geographical locations, viz., Eleshwaram (Andhra Pradesh), Thoothukudi (Tamil Nadu), and Karwar (Karnataka), [...] Read more.
Salacia oblonga is used to treat diabetes, hypocholesteremia, gonorrhea, rheumatism, asthma, inflammation, oxidative stress, etc. In the present study, the antidiabetic activity of S. oblonga methanolic root extracts collected from three geographical locations, viz., Eleshwaram (Andhra Pradesh), Thoothukudi (Tamil Nadu), and Karwar (Karnataka), was studied in vitro. Among the three extracts, S. oblonga root extracts from Eleshwaram showed maximum α-glucosidase and α-amylase inhibitory activities, indicating better antidiabetic activity. Acute toxicity studies of S. oblonga carried out in Albino Wistar rats showed no toxicity. Further, in vivo studies showed antidiabetic and antilipidemic activities in Albino Wistar rats with induced type II diabetes mellitus. Type II diabetes mellitus was induced in the experimental rats by intraperitoneal injection of nicotinamide and streptozotocin. The rats were orally fed different doses (ranging from 0 to 400 mg/kg body weight) of S. oblonga root extracts from Eleshwaram for 14 days. Blood glucose, lipid, bilirubin, and creatinine levels were analyzed on day 0, 7, and 14. The S. oblonga root extract from Eleshwaram decreased the glucose levels in a dose-dependent manner as well as the lipid, creatinine, and bilirubin levels in diabetic rats. Thus, the present study demonstrates antidiabetic and antilipidemic properties of S. oblonga root extracts. Full article
(This article belongs to the Special Issue Extraction, Characterization and Pharmacology of Natural Products)
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Article
Malus baccata var. gracilis and Malus toringoides Bark Polyphenol Studies and Antioxidant, Antimicrobial and Anticancer Activities
Processes 2020, 8(3), 283; https://doi.org/10.3390/pr8030283 - 02 Mar 2020
Cited by 8 | Viewed by 1634
Abstract
Exploring new sources of polyphenols with biological activities that work against human diseases is the target of natural product studies. This study determined the polyphenol composition of the bark of Malus species M. baccata var. gracilis (Rehder) T.C.Ku and M. toringoides (Rehder) Hughes, [...] Read more.
Exploring new sources of polyphenols with biological activities that work against human diseases is the target of natural product studies. This study determined the polyphenol composition of the bark of Malus species M. baccata var. gracilis (Rehder) T.C.Ku and M. toringoides (Rehder) Hughes, using high-performance liquid chromatography with a diode-array detector (HPLC-DAD) analysis. The antiproliferative, cytotoxic, antioxidant and antimicrobial applications of these extracts, as well as the identified phenol, were studied. The HPLC-DAD analysis confirmed three polyphenols in the extracts out of the 21 screened compounds: protocatechuic acid, gallic acid, and catechin. The major constituents in M. baccata and M. toringoides were protocatechuic acid, at 3.16 and 7.15 mg 100 g−1 dry weight (DW), respectively, and catechin, at 5.55 and 6.80 mg 100 g−1 DW, respectively. M. baccata and M. toringoides bark extracts showed antioxidant activities using 2,2-diphenyl-1-picrylhydrazyl (DPPH), β-carotene bleaching, and ferric-reducing antioxidant power (FRAP) assays, which were attributed to the dominance of protocatechuic acid. The highest antiproliferative and cytotoxic effects were against Jurkat cells. Against MCF-7 and Hela cells, there was necrotic cell accumulation in the early apoptotic as well as the late apoptotic phase. The bark extracts showed noticeable antibacterial effects against Listeria monocytogenes, Bacillus cereus, and Escherichia coli. Protocatechuic acid showed comparable results to bark extracts. There were antifungal effects against Aspergillus ochraceus, A. niger, and Candida albicans, and the activities were higher than the commercial reagent. M. baccata and M. toringoides could be considered as a new source of phenolic acids, including protocatechuic acid with anticancer, antibacterial antifungal, and antioxidant-promising effects. Full article
(This article belongs to the Special Issue Extraction, Characterization and Pharmacology of Natural Products)
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Article
Metabolite Profiling of Aquilaria malaccensis Leaf Extract Using Liquid Chromatography-Q-TOF-Mass Spectrometry and Investigation of Its Potential Antilipoxygenase Activity In-Vitro
Processes 2020, 8(2), 202; https://doi.org/10.3390/pr8020202 - 06 Feb 2020
Cited by 7 | Viewed by 1794
Abstract
The Aquilaria malaccensis species of the genus Aquilaria is an abundant source of agarwood resin and many bioactive phytochemicals. Recent data regarding the chemical constituents and biological activities of Aquilaria leaves led us to attempt to qualitatively profile the metabolites of Aquilaria malaccensis [...] Read more.
The Aquilaria malaccensis species of the genus Aquilaria is an abundant source of agarwood resin and many bioactive phytochemicals. Recent data regarding the chemical constituents and biological activities of Aquilaria leaves led us to attempt to qualitatively profile the metabolites of Aquilaria malaccensis leaves from a healthy, noninoculated tree through phytochemical screening, GC-MS, and LC/Q-TOF-MS. The present work is also the first to report the antilipoxygenase activity of A. malaccensis leaves from healthy noninoculated tree and investigate its toxicity on oral mucosal cells. A total of 53 compounds were tentatively identified in the extract, some of which have been described in literature as exhibiting anti-inflammatory activity. A number of compounds were identified for the first time in the extract of A. malaccensis leaf, including quercetin, quercetin-O-hexoside, kaempferol-O-dirhamnoside, isorhamnetin-O-hexoside, syringetin-O-hexoside, myricetin, tetrahydroxyflavanone, hesperetin, sissotrin, and lupeol. The antilipoxygenase assay was used to determine the lipoxygenase (LOX) inhibitory potential of the extract, while a WST-1 assay was conducted to investigate the effect of the extract on oral epithelial cells (OEC). The extract implied moderate anti-LOX activity with IC50 value of 71.6 µg/mL. Meanwhile, the cell viability of OEC ranged between 92.55% (10 µg/mL)–76.06% ± (100 µg/mL) upon treatment, indicating some potential toxicity risks. The results attained encourage future studies of the isolation of bioactive compounds from Aquilaria malaccensis leaves, as well as further investigation on the anti-inflammatory mechanisms and toxicity associated with their use. Full article
(This article belongs to the Special Issue Extraction, Characterization and Pharmacology of Natural Products)
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Article
Mass Spectral Fragmentation of Pelargonium graveolens Essential Oil Using GC–MS Semi-Empirical Calculations and Biological Potential
Processes 2020, 8(2), 128; https://doi.org/10.3390/pr8020128 - 21 Jan 2020
Cited by 13 | Viewed by 2442
Abstract
The volatile constituents of the essential oil of local Pelargonium graveolens growing in Egypt was investigated by gas chromatography–mass spectrometry (GC–MS), and the main constituents were citronellol (27.67%), cis-Menthone (10.23%), linalool (10.05%), eudesmol (9.40%), geraniol formate 6.87%, and rose oxide (5.77%), which represent [...] Read more.
The volatile constituents of the essential oil of local Pelargonium graveolens growing in Egypt was investigated by gas chromatography–mass spectrometry (GC–MS), and the main constituents were citronellol (27.67%), cis-Menthone (10.23%), linalool (10.05%), eudesmol (9.40%), geraniol formate 6.87%, and rose oxide (5.77%), which represent the major components in the obtained GC total ion chromatogram. The structural determination of the main constitutes based on their electron ionization mass spectra have been investigated. The MS of these compounds are absolutely identical in mass values of peaks of fragment ions, where their relative intensities have minor differences. In the spectra of all studied compounds, the observed characteristic ions were [M-H2O]+ and [M-CH3]+. The latter has a structure with m/z 69, 83. Different quantum parameters were obtained using Modified Neglect of Diatomic Overlap (MNDO) semi-empirical method as total energy, binding energy, heat of formations, ionization energy, the energy of highest occupied molecular orbital (HOMO), the energy of the lowest unoccupied molecular orbital (LUMO), energy gap Δ, and dipole moment. The antibacterial and antifungal activities of P. graveolens essential oil and identified compounds were tested against wide collection of organisms. The individual identified compounds in the essential oil—citronellol, cis-Menthone, and linalool (except eudesmol)—showed comparable activity to antibiotics. The most active isolated compound was the citronellol and the lowest MIC was found against E. coli. The essential oil showed high antifungal effects and this activity was attributed to cis-Menthone, eudesmol, and citronellol (excluding linalool). cis-Menthone was the most active compound against selected fungi followed by the eudesmol The study recommends local P. graveolens and identified active compounds for further applications in the pharmaceutical industries. Full article
(This article belongs to the Special Issue Extraction, Characterization and Pharmacology of Natural Products)
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Article
Correlation between Antibacterial Activity and Free-Radical Scavenging: In-Vitro Evaluation of Polar/Non-Polar Extracts from 25 Plants
Processes 2020, 8(1), 117; https://doi.org/10.3390/pr8010117 - 17 Jan 2020
Cited by 7 | Viewed by 1673
Abstract
Objectives: The current study aimed to measure the antioxidant and antibacterial activities of 25 wild Palestinian edible plants, which were subjected to extraction by polar and non-polar solvents. Correlations between free radical scavenging activity and antibacterial activity of the extracts were assessed for [...] Read more.
Objectives: The current study aimed to measure the antioxidant and antibacterial activities of 25 wild Palestinian edible plants, which were subjected to extraction by polar and non-polar solvents. Correlations between free radical scavenging activity and antibacterial activity of the extracts were assessed for both polar and non-polar fractions. Materials: Twenty-five wild edible plant species that are frequently consumed by people in Palestine (mainly in a rural area) were examined. Among them, 10 plant species were among those with the highest mean cultural importance values, according to an ethnobotanical survey that was conducted in the West Bank, Palestine, a few years ago. Method: The protocol of the DPPH assay for testing free-radical scavenging was utilized for determining EC50 values, while microdilution tests were conducted to determine the 50% inhibitory concentration (IC50) of the extracts for the microorganism Staphylococcus mutans. Results and Discussion: Eight extracts (non-polar fractions) were found to possess an antibacterial IC50 of less than 20 ppm, such as Foeniculum vulgare, Salvia palaestinafruticose, Micromeria fruticose, Trigonella foenum-graecum, Cichorium pumilum jacq, Salvia hierosolymitana boiss, Ruta chalepensis, and Chrysanthemum coronarium. The polar fractions possess higher antioxidant activity, while non-polar fraction possess higher antibacterial activity. Looking at all the results together can deceive and lead to the conclusion that there is no correlation between antibacterial activity against S. mutans and free radical scavenging (R2 equals 0.0538). However, in-depth analysis revealed that non-polar plant extracts with an EC50 of free radical scavenging ≤100 ppm have a four-fold order of enrichment toward more activity against S. mutans. These findings are of high importance for screening projects. A four-fold order of enrichment could save plenty of time and many in screening projects. The antibacterial active extracts marked by low-medium free radical scavenging might act through a mechanism of action other than that of highly active, free radical scavenging extracts. Conclusion: The screening of antioxidant and antimicrobial activity performed on 25 selected wild plant extracts revealed a satisfactory free radical scavenging and antimicrobial potential that could be of value in the management of oxidative stress. Further studies are recommended to explore novel and highly active natural antibacterial products. Full article
(This article belongs to the Special Issue Extraction, Characterization and Pharmacology of Natural Products)
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Article
Tree Bark Phenols Regulate the Physiological and Biochemical Performance of Gladiolus Flowers
Processes 2020, 8(1), 71; https://doi.org/10.3390/pr8010071 - 05 Jan 2020
Cited by 8 | Viewed by 1332
Abstract
The postharvest physiology of cut flowers is largely dependent on vase life, which is the maximum number of days before flower senescence. The use of tree bark extracts (major forest plant residues), as an eco-friendly and natural antioxidant preservative in holding solutions, is [...] Read more.
The postharvest physiology of cut flowers is largely dependent on vase life, which is the maximum number of days before flower senescence. The use of tree bark extracts (major forest plant residues), as an eco-friendly and natural antioxidant preservative in holding solutions, is a novel tool for extending flower longevity. The morphological, physiological, biochemical, and genetic responses of Gladiolus grandiflorus cut spikes to Magnolia acuminata and Taxus cuspidata bark extracts as additives in holding solutions were investigated. G. grandiflorus subjected to bark extracts as well as catechin and protocatechuic acid (main phenols) displayed significant increased longevity (up to 18 days), an increased number of open florets, and increased floret fresh weight. Increases in the relative water content, leaf chlorophyll, carotenoids, soluble sugars, and protein content were observed in addition to a reduction in microbial growth in the cut spikes. Gas exchange parameters were higher in the bark extract treatments than in the controls. Higher antioxidant activities were detected and associated with increased superoxide dismutase and catalase enzyme activities and reduced H2O2 accumulation. The bark extract treatments associated with reduced expression of GgCyP1 (produces cysteine protease) and increased expression of both GgDAD1 (defends against apoptotic activity) and GgEXPA1 (regulates petal expansion). Several mechanisms were implicated in these effects, including maintenance of water content, enhanced management of reactive oxygen species (ROS), increased sugar and protein composition, and control of microbial growth. Thus, bark extracts and isolated phenols could be developed as an eco-friendly, non-toxic, and cost-effective natural preservative for cut gladiolus flowers. Full article
(This article belongs to the Special Issue Extraction, Characterization and Pharmacology of Natural Products)
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Article
In Vitro Antidiabetic Activity Affecting Glucose Uptake in HepG2 Cells Following Their Exposure to Extracts of Lauridia tetragona (L.f.) R.H. Archer
Processes 2020, 8(1), 33; https://doi.org/10.3390/pr8010033 - 30 Dec 2019
Cited by 8 | Viewed by 2408
Abstract
The incidence of diabetes is on the rise and one of the medically active plants used for the treatment of diabetes in South Africa is Lauridia tetragona. The aim of this study is to investigate the antidiabetic property of the polyphenolics (PP) [...] Read more.
The incidence of diabetes is on the rise and one of the medically active plants used for the treatment of diabetes in South Africa is Lauridia tetragona. The aim of this study is to investigate the antidiabetic property of the polyphenolics (PP) compounds isolated from the methanolic extract of Lauridia tetragona. The α-amylase, α-glucosidase, dipeptidyl peptidase IV (DPPIV), lipase inhibitory activities, and glucose uptake in HepG2 were investigated. The methanolic extract fractions of L. tetragona yielded six fractions (PP1–PP6) all of which showed weak inhibition against DPPIV and lipase compared to the standards. However, PP4 and PP6 showed the best inhibition against α-amylase (IC50 of 359.3 ± 2.11 and 416.82 ± 2.58 μg/mL, respectively) and α-glucosidase (IC50 of 95.93 ± 2.34 and 104.49 ± 2.21 μg/mL, respectively) and only PP4 (173.6%) resulted in enhanced glucose uptake in HepG2 cells compared to berberine (129.89%) and metformin (187.16%) used as positive controls. The previous investigation on PP4 and PP6 showed the presence of polyphenolics such as ferulic acid, coumaric acid, and caffeic acid. The results of this study suggest that L. tetragona could be suitable as an antidiabetic agent and justifies the folkloric use of the plant to treat diabetes. Full article
(This article belongs to the Special Issue Extraction, Characterization and Pharmacology of Natural Products)
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Article
Antioxidant Activity and Selenium and Polyphenols Content from Selected Medicinal Plants Natives from Various Areas Abundant in Selenium (Poland, Lithuania, and Western Ukraine)
Processes 2019, 7(12), 878; https://doi.org/10.3390/pr7120878 - 25 Nov 2019
Cited by 7 | Viewed by 1388
Abstract
The study was performed on Centaurea cyanus, Chamomilla recutita, Majorana hortensis, Ocimum basilicum, Plantago lanceolata, Sinapis alba, and Valeriana officinalis harvested in Lithuania, Poland, and Ukraine. Our aim was to determine the differences in selenium concentrations, total [...] Read more.
The study was performed on Centaurea cyanus, Chamomilla recutita, Majorana hortensis, Ocimum basilicum, Plantago lanceolata, Sinapis alba, and Valeriana officinalis harvested in Lithuania, Poland, and Ukraine. Our aim was to determine the differences in selenium concentrations, total polyphenols, and the antioxidant activity in same-species samples from different regions. Another goal was to assess the correlations between these variables within the species. We found variations in most species, but not in all regions of harvesting. In four of the six species from Ukraine, we observed the highest concentration of Se. The selenium concentrations ranged from 15–182 µg/kg DW, and the greatest variation between the regions occurred in S. alba. The level of polyphenols was 5.52–53.25 mg TAE/100 g DW, and the largest differences between the sampling regions occurred in P. lanceolata and O. basilicum. ABTS radicals scavenging ability ranged from 5.20–59.79 μM AAE/100 g DW, while the FRAP potential was 13.56–409.14 μM FeE/100 g DW. The largest differences in antioxidant activity were found in O. basilicum and M. hortensis. Pearson’s correlation coefficients indicate that polyphenols may be responsible for antioxidant activity in Ch. recutita, O. basilicum, and V. officinalis, and selenium is responsible for antioxidant activity in M. hortensis. However, both polyphenols and selenium play a role in the antioxidant properties of C. cyanus and P. lanceolata. Also, selenium in C. cyanus and Ch. recutita may affect the level of total polyphenols. The examined species may supplement the human diet with exogenous antioxidants. Full article
(This article belongs to the Special Issue Extraction, Characterization and Pharmacology of Natural Products)
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Article
Pulsed Electric Field-Assisted Ethanolic Extraction of Date Palm Fruits: Bioactive Compounds, Antioxidant Activity and Physicochemical Properties
Processes 2019, 7(9), 585; https://doi.org/10.3390/pr7090585 - 03 Sep 2019
Cited by 23 | Viewed by 1590
Abstract
The current study was aimed to observe the influence of pulsed electric field (PEF) on the extraction of bioactive components; antioxidant activity and physicochemical properties of date palm fruit extract (DPFE) as compared to the extract untreated by PEF. The fruit was treated [...] Read more.
The current study was aimed to observe the influence of pulsed electric field (PEF) on the extraction of bioactive components; antioxidant activity and physicochemical properties of date palm fruit extract (DPFE) as compared to the extract untreated by PEF. The fruit was treated with PEF (frequency: 10 Hz, time: 100 µs, pulses number: 30, electric field strength (EFS): 1, 2, and 3 kV/cm. The results show that PEF has a positive impact on the total content of carotenoids, anthocyanins, flavonoids, and phenolics by increasing the EFS. DPFE treated with PEF exhibit a strong antioxidant activity as compared to untreated extract, while electrical conductivity, pH values, and titratable acidity were not affected by PEF. The results indicate a notable increase in the volatile components in DPFE treated with PEF at 3 kV/cm. Thus, PEF treatment can assist the ethanolic extraction of DPFE to improve the bioactivity and antioxidative activity. These findings suggest that PEF can be a more suitable technique to enhance solvent extraction on a commercial basis. Full article
(This article belongs to the Special Issue Extraction, Characterization and Pharmacology of Natural Products)
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Article
In Vitro Antifungal Efficacy of White Radish (Raphanus sativus L.) Root Extract and Application as a Natural Preservative in Sponge Cake
Processes 2019, 7(9), 549; https://doi.org/10.3390/pr7090549 - 21 Aug 2019
Cited by 1 | Viewed by 1502
Abstract
The study attempts the optimization of the total flavonoid content (TFC) and the 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) antioxidant activity of the white radish (Raphanus sativus L.) root ethanolic extract (WRE) with regard to several parameters including ethanol concentration, the ratio of solvent/material, temperature [...] Read more.
The study attempts the optimization of the total flavonoid content (TFC) and the 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) antioxidant activity of the white radish (Raphanus sativus L.) root ethanolic extract (WRE) with regard to several parameters including ethanol concentration, the ratio of solvent/material, temperature and extraction time. Then antifungal analysis of WRE was performed against four fungal species including Aspergillus flavus NBRC 33021, Aspergillus niger NBRC 4066, Aspergillus clavatus NBRC 33020, and Fusarium solani NBRC 31094. At the WRE concentration of 75 mg/mL, diameters of inhibition zone were 9.11 ± 1.5, 19.55 ± 1.68, 17.72 ± 0.25, and 17.50 ± 0.73 mm respectively against the four examined species. Minimum fungal concentration (MFC) values of WRE against the four species were 30, 10, 20 and 30 mg/mL respectively. Evaluation of the sponge cake added with white radish root extract suggested that shelf-life of the sponge cake is 8 weeks in air-cooled condition (20 °C) and two weeks in warm condition (37 °C). Full article
(This article belongs to the Special Issue Extraction, Characterization and Pharmacology of Natural Products)
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Article
Effects of Bromelain and Trypsin Hydrolysis on the Phytochemical Content, Antioxidant Activity, and Antibacterial Activity of Roasted Butterfly Pea Seeds
Processes 2019, 7(8), 534; https://doi.org/10.3390/pr7080534 - 14 Aug 2019
Cited by 6 | Viewed by 2222
Abstract
Butterfly pea (Clitoria ternatea L.) is a traditional medicinal and edible herb, whose health-promoting benefits have been attributed to its phenolic constituents. In this study, the effects of enzymatic hydrolysis on total phenolic content (TPC) and total flavonoid content (TFC), antioxidant (2,2’-azino-bis(3-ethylbenzothiazoline-6-sulphonic [...] Read more.
Butterfly pea (Clitoria ternatea L.) is a traditional medicinal and edible herb, whose health-promoting benefits have been attributed to its phenolic constituents. In this study, the effects of enzymatic hydrolysis on total phenolic content (TPC) and total flavonoid content (TFC), antioxidant (2,2’-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) diammonium salt (ABTS), 2,2-diphenyl-1-picrylhydrazyl (DPPH), and ferric reducing antioxidant power (FRAP)) and antibacterial activities of raw and roasted (200 °C, 10–20 min) butterfly pea seeds were investigated. Roasting reduced the yield of seed aqueous extracts, but it increased the TPC and FRAP values, hence the reducing ability, of the extracts. Bromelain hydrolysis enhanced the TPC and TFC of the roasted seeds up to 2- and 18-fold higher, respectively. Trypsin hydrolysis drastically increased the TPC, but not TFC, of roasted seeds; trypsin-hydrolyzed, 20 min roasted sample had the highest TPC (54.07 μg gallic acid equivalent (GAE)/mg) among all samples. Bromelain hydrolysis significantly improved the antioxidant activity of the roasted seed samples, where the antioxidant activity of bromelain-hydrolyzed, 20 min roasted sample was about 50% greater than the non-hydrolyzed 20 min roasted sample. Trypsin hydrolysis raised the FRAP values of the 20 min roasted sample to 70.28 mg Fe(II) equivalent/g, the highest among all samples. Nevertheless, trypsin only weakly elevated the ABTS scavenging activity of the roasted samples, showing no enhancement of the DPPH scavenging activity. On the other hand, only bromelain hydrolysates of raw and 10 min roasted seeds were active against Staphylococcus aureus. Taken together, bromelain hydrolysis can be used to enhance the extractable phytochemical contents and antioxidant activity of roasted butterfly pea seeds. Full article
(This article belongs to the Special Issue Extraction, Characterization and Pharmacology of Natural Products)
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Article
Qualitative Fingerprint Analysis and Multidirectional Assessment of Different Crude Extracts and Essential Oil from Wild Artemisia santonicum L.
Processes 2019, 7(8), 522; https://doi.org/10.3390/pr7080522 - 07 Aug 2019
Cited by 5 | Viewed by 1602
Abstract
Artemisia species are used as folk medicines in several countries. This work was aimed to shed more light on the effect of methanol, water, ethyl acetate extracts, and essential oil (EO) of A. santonicum on selected enzymes (cholinesterase, tyrosinase α-amylase, and α-glucosidase) as [...] Read more.
Artemisia species are used as folk medicines in several countries. This work was aimed to shed more light on the effect of methanol, water, ethyl acetate extracts, and essential oil (EO) of A. santonicum on selected enzymes (cholinesterase, tyrosinase α-amylase, and α-glucosidase) as well of their antioxidant and pharmacological effects. The chemical profile of the essential oil was determined using gas chromatography coupled to mass spectrometry (GC-MS) analysis, while the extracts were chemically characterized by high performance liquid chromatography coupled to mass spectrometry (HPLC-MS). Forty-nine constituents were identified and camphor (36.6%), 1,8-cineole (10.2%), α-thujone (10.1%), borneol (4.5%), and β-thujone (3.6%) were the major components. Overall, 45, 74, and 67 components were identified from the ethyl acetate, methanol, and water extracts, respectively. The EO and extracts showed significant antioxidant properties, in a cell-free model; particularly, methanol and water extracts revealed promising sources of antioxidant compounds. Additionally, we evaluated protective effects of EO and extracts in isolated rat colon tissue challenged with lipopolysaccharide (LPS), as an ex vivo model of colon inflammation, and human colon cancer HCT116 cell line. Particularly, we observed that, among all tested samples, A. santonicum ethyl acetate displayed the best pharmacological profile, being able to blunt LPS-induced levels of all tested biomarkers of inflammation and oxidative stress, including colon nitrites, lactate dehydrogenase, prostaglandin E2, and serotonin. Additionally, this extract was also able to reduce HCT116 cell viability, thus suggesting potential antiproliferative effects against colon cancer cells. Based on our results, A. santonicum has great potential for developing novel functional agents including pharmaceuticals, cosmeceuticals, and nutraceuticals. Full article
(This article belongs to the Special Issue Extraction, Characterization and Pharmacology of Natural Products)
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Article
Curcumin Analogues with Aldose Reductase Inhibitory Activity: Synthesis, Biological Evaluation, and Molecular Docking
Processes 2019, 7(7), 417; https://doi.org/10.3390/pr7070417 - 02 Jul 2019
Cited by 3 | Viewed by 1693
Abstract
Curcumin, a constituent of Curcuma longa, has shown numerous biological and pharmacological activities, including antidiabetic effects. Here, a novel series of curcumin analogues were synthesized and evaluated for in vitro inhibition of aldose reductase (AR), the first and rate-limiting enzyme of the [...] Read more.
Curcumin, a constituent of Curcuma longa, has shown numerous biological and pharmacological activities, including antidiabetic effects. Here, a novel series of curcumin analogues were synthesized and evaluated for in vitro inhibition of aldose reductase (AR), the first and rate-limiting enzyme of the polyol pathway, which plays a key role in the onset and progression of diabetic complications. Biological activity studies showed that all the curcuminoids exhibited moderate to good AR inhibitory (ARI) activities compared with that of the quercetin standard. Importantly, compounds 8d, 8h, 9c, 9e, and 10g demonstrated promising ARI activities, with the 50% inhibitory concentration (IC50) values of 5.73, 5.95, 5.11, 5.78, and 5.10 µM, respectively. Four other compounds exhibited IC50 values in the range of 6.04–6.18 µM. Methyl and methoxy derivatives showed a remarkable ARI potential compared with that of other substitutions on the aromatic ring. Molecular docking experiments demonstrated that the most active curcuminoid (10g) was able to favorably bind in the active site of the AR enzyme. The potent ARI activities exhibited by the curcuminoids were attributed to their substitution patterns on the aromatic moiety, which may provide novel leads in the development of therapeutics for the treatment of diabetic complications. Full article
(This article belongs to the Special Issue Extraction, Characterization and Pharmacology of Natural Products)
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Article
Optimization of Ultrasound-Assisted Extraction on Antioxidative Activity of Malus toringoides Using Response Surface Methodology
Processes 2019, 7(5), 270; https://doi.org/10.3390/pr7050270 - 08 May 2019
Cited by 5 | Viewed by 1386
Abstract
Ultrasonic-assisted extraction (UAE) was optimized using response surface methodology (RSM) to maintain the cyto-protective activity of M.toringoides against oxidative stress. The optimal conditions for UAE were a 58 mL/g liquid-solid ratio, a 38 °C extraction temperature, an 85% solvent concentration, and a 19-min [...] Read more.
Ultrasonic-assisted extraction (UAE) was optimized using response surface methodology (RSM) to maintain the cyto-protective activity of M.toringoides against oxidative stress. The optimal conditions for UAE were a 58 mL/g liquid-solid ratio, a 38 °C extraction temperature, an 85% solvent concentration, and a 19-min extraction time, which resulted in a protection rate of 54.57% against hydrogen peroxide-induced oxidative stress in human umbilical vein endothelial cells (HUVECs). These results were comparable to the predicted value of 53.75%. The extracts showed excellent antioxidant activity, and phlorizin was detected in the dried leaves of Malus.toringoides. The highest yield of phlorizin (101.239 mg/g) was also obtained using these conditions. Taken together, these results showed that the method successfully integrated RSM and partial least squares regression methods to optimize M.toringoides extraction to yield the highest cyto-protective activity and effectively increase the yield of phlorizin from M.toringoides. Full article
(This article belongs to the Special Issue Extraction, Characterization and Pharmacology of Natural Products)
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Article
Benzoic Acid Derivatives of Ifloga spicata (Forssk.) Sch.Bip. as Potential Anti-Leishmanial against Leishmania tropica
Processes 2019, 7(4), 208; https://doi.org/10.3390/pr7040208 - 11 Apr 2019
Cited by 12 | Viewed by 2399
Abstract
This study aimed to appraise the anti-leishmanial potentials of benzoic acid derivatives, including methyl 3,4-dihydroxybenzoate (compound 1) and octadecyl benzoate (compound 2), isolated from the ethnomedicinally important plant Ifloga spicata (I. spicata). Chemical structures were elucidated via FT-IR, [...] Read more.
This study aimed to appraise the anti-leishmanial potentials of benzoic acid derivatives, including methyl 3,4-dihydroxybenzoate (compound 1) and octadecyl benzoate (compound 2), isolated from the ethnomedicinally important plant Ifloga spicata (I. spicata). Chemical structures were elucidated via FT-IR, mass spectrometry, and multinuclear (1H and 13C) NMR spectroscopy. Anti-leishmanial potentials of the compounds were assessed using Leishmania tropica promastigotes. Moreover, acridine orange fluorescent staining was performed to visualize the apoptosis-associated changes in promastigotes under a fluorescent microscope. A SYTOX assay was used to check rupturing of Leishmania promastigote cell membranes using 0.1% Triton X-100 as positive control. A DNA interaction assay was carried out to assess DNA attachment potential. AutoDock software was used to check the binding affinity of compounds with surface enzyme leishmanolysin gp63 (1LML). Both compounds exhibited considerable anti-leishmanial potential, with LD50 values of 10.40 ± 0.09 and 14.11 ± 0.11 μg/mL for compound 1 and compound 2, respectively. Both compounds showed higher binding affinity with the leishmanolysin (gp63) receptor/protease of Leishmania, as assessed using computational analysis. The binding scores of compounds 1 and 2 with target gp63 were −5.3 and −5.6, respectively. The attachment of compounds with this receptor resulted in their entry into the cell where they bound with Leishmania DNA, causing apoptosis. The results confirmed that the investigated compounds have anti-leishmanial potential and are potential substitutes as natural anti-leishmanial agents against L. tropica. Full article
(This article belongs to the Special Issue Extraction, Characterization and Pharmacology of Natural Products)
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