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The Role of Natural Products in Promoting Well-being: From Foods to Drugs

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

Deadline for manuscript submissions: closed (30 June 2023) | Viewed by 96740

Special Issue Editors

Prof. Dr. Bruno Botta

E-Mail Website
Guest Editor
Department of Chemistry and Technology of Drugs, Sapienza - University of Rome, Rome, Italy
Interests: secondary metabolites; natural products chemistry; natural products as anticancer agents; antibiotic resistance modulation by natural products; targeted therapy; molecular recognition; industrial hemp (Cannabis sativa L.)
Special Issues, Collections and Topics in MDPI journals
Dr. Cinzia Ingallina

E-Mail Website
Guest Editor
Department of Chemistry and Technology of Drugs, Sapienza - University of Rome, Rome, Italy
Interests: food chemistry; NMR metabolomics; characterization of chemical food profile; monitoring the foodstuff metabolic profiles; monitoring diet and nutrition studies; industrial hemp product characterization
Dr. Andrea Calcaterra

E-Mail Website
Guest Editor
Department of Chemistry and Technology of Drugs, Sapienza - University of Rome, Rome, Italy
Interests: natural products chemistry; isolation and total synthesis of natural products; natural products as anticancer agents; antibiotic resistance modulation by natural products; synthesis of macrocycles for drug delivery and molecular recognition
Dr. Deborah Quaglio

E-Mail Website
Guest Editor
Department of Chemistry and Technology of Drugs, Sapienza - University of Rome, Rome, Italy
Interests: plant-derived anticancer agents; naturally-occurring adjuvants for antibiotic resistance; bioconjugate-drug development; synthesis of artificial receptors; biosensors development

Special Issue Information

Dear Colleagues,

Natural products have long been considered a unique source of drugs, and are still considered a profitable starting point in modern drug discovery due to their unique chemical diversity, which is uncommon in synthetic compounds libraries. However, by the end of the 20th century, research efforts aiming to identify natural products as a pool for drug discovery had declined. The research efforts of many pharmaceutical companies were more focused on new technologies such as combinatorial chemistry, metagenomics, and high-throughput screening to identify new drug candidates. However, these new methodologies did not deliver the expected results and, recently, natural products were reevaluated as one of the best sources of drugs and drug leads.

Among the natural products sources, foodstuffs are recently being considered not only for their nutritional values (due to macro- and micronutrients content), but also for their possible beneficial roles in human health (due to the presence of secondary metabolites). Foodstuffs may play a pivotal role in human health, and thus it is important that we develop our knowledge of the chemical-biological profiles of foodstuffs .

The present Special Issue will gather the latest research trends in natural products investigation, comprising both drug discovery and food consumption. By collecting the contributions of specialist scientists of the field, this Issue will aim to advance the knowledge and to increase the expertise on natural products, food chemistry, and biology. We invite authors to report multimethodological approaches, including synthetic chemistry, computational chemistry, biology, and pharmacology. We welcome the submission of both original research articles and review articles on organic synthesis, medicinal chemistry, food chemistry, chemical biology, bioconjugate chemistry, and nanotechnology for drug delivery.

Prof. Dr. Bruno Botta
Dr. Cinzia Ingallina
Dr. Andrea Calcaterra
Dr. Deborah Quaglio
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

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. Molecules is an international peer-reviewed open access semimonthly 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 2700 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 products isolation
  • natural products synthesis
  • natural products library
  • theoretical and computational chemistry
  • screening in silico
  • targeted drug delivery/discovery
  • anticancer drugs
  • antiviral drugs
  • drug resistance
  • food chemistry

Published Papers (31 papers)

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13 pages, 3359 KiB  
Article
(−)-Epicatechin Inhibits Metastatic-Associated Proliferation, Migration, and Invasion of Murine Breast Cancer Cells In Vitro
by Javier Pérez-Durán, Aglaé Luna, Andrés Portilla, Pamela Martínez, Guillermo Ceballos, Miguel Ángel Ortíz-Flores, Juan Mario Solis-Paredes and Nayelli Nájera
Molecules 2023, 28(17), 6229; https://doi.org/10.3390/molecules28176229 - 24 Aug 2023
Viewed by 1662
Abstract
Breast cancer, due to its high incidence and mortality, is a public health problem worldwide. Current chemotherapy uses non-specific cytotoxic drugs, which inhibit tumor growth but cause significant adverse effects. (−)-Epicatechin (EC) is part of a large family of biomolecules called flavonoids. It [...] Read more.
Breast cancer, due to its high incidence and mortality, is a public health problem worldwide. Current chemotherapy uses non-specific cytotoxic drugs, which inhibit tumor growth but cause significant adverse effects. (−)-Epicatechin (EC) is part of a large family of biomolecules called flavonoids. It is widely distributed in the plant kingdom; it can be found in green tea, grapes, and cocoa. Several studies in animals and humans have shown that EC induces beneficial effects in the skeletal muscle and the cardiovascular system, reducing risk factors such as arterial hypertension, endothelial dysfunction, damage to skeletal muscle structure, and mitochondrial malfunction by promoting mitochondrial biogenesis, with no adverse effects reported. Recently, we reported that EC had an antitumor effect in a murine triple-negative mammary gland tumor model, decreasing tumoral size and volume and increasing survival by 44%. This work aimed to characterize the effects of flavanol EC on proliferation, migration, and metastasis markers of triple-negative murine breast (4T1) cancer cells in culture. We found proliferation diminished and Bax/Bcl2 ratio increased. When the migration of culture cells was evaluated, we observed a significant reduction in migration. Also, the relative expression of the genes associated with metastasis, Cdh1, Mtss1, Pten, Bmrs, Fat1, and Smad4, was increased. In conclusion, these results contribute to understanding molecular mechanisms activated by EC that can inhibit metastatic-associated proliferation, migration, and invasion of murine breast cancer cells. Full article
(This article belongs to the Special Issue The Role of Natural Products in Promoting Well-being: From Foods to Drugs)
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16 pages, 11140 KiB  
Article
Pyrrolyldihydropyrazino[1,2-a]indoletrione Analogue Microtubule Inhibitor Induces Cell-Cycle Arrest and Apoptosis in Colorectal Cancer Cells
by Dong-Lin Yang, Hong-Xia Qin, Na-Na Zhang, Ya-Jun Zhang, Jiu-Hong Huang, Chun-Sheng Hu, Xiao-Xue Zhang, Yong Li and Liu-Jun He
Molecules 2023, 28(4), 1948; https://doi.org/10.3390/molecules28041948 - 17 Feb 2023
Cited by 1 | Viewed by 1498
Abstract
In this study, 2-benzyl-10a-(1H-pyrrol-2-yl)-2,3-dihydropyrazino[1,2-a]indole-1,4,10(10aH)-trione (DHPITO), a previously identified inhibitor against hepatocellular carcinoma cells, is shown to exert its cytotoxic effects by suppressing the proliferation and growth of CRC cells. An investigation of its molecular mechanism confirmed that [...] Read more.
In this study, 2-benzyl-10a-(1H-pyrrol-2-yl)-2,3-dihydropyrazino[1,2-a]indole-1,4,10(10aH)-trione (DHPITO), a previously identified inhibitor against hepatocellular carcinoma cells, is shown to exert its cytotoxic effects by suppressing the proliferation and growth of CRC cells. An investigation of its molecular mechanism confirmed that the cytotoxic activity of DHPITO is mediated through the targeting of microtubules with the promotion of subsequent microtubule polymerisation. With its microtubule-stabilising ability, DHPITO also consistently arrested the cell cycle of the CRC cells at the G2/M phase by promoting the phosphorylation of histone 3 and the accumulation of EB1 at the cell equator, reduced the levels of CRC cell migration and invasion, and induced cellular apoptosis. Furthermore, the compound could suppress both tumour size and tumour weight in a CRC xenograft model without any obvious side effects. Taken together, the findings of the present study reveal the antiproliferative and antitumour mechanisms through which DHPITO exerts its activity, indicating its potential as a putative chemotherapeutic agent and lead compound with a novel structure. Full article
(This article belongs to the Special Issue The Role of Natural Products in Promoting Well-being: From Foods to Drugs)
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27 pages, 1119 KiB  
Article
Cinnamomum sp. and Pelargonium odoratissimum as the Main Contributors to the Antibacterial Activity of the Medicinal Drink Horchata: A Study Based on the Antibacterial and Chemical Analysis of 21 Plants
by Paulina Fernandez-Soto, Diana Celi, Eduardo Tejera, José Miguel Alvarez-Suarez and António Machado
Molecules 2023, 28(2), 693; https://doi.org/10.3390/molecules28020693 - 10 Jan 2023
Cited by 2 | Viewed by 3141
Abstract
Horchata, a herbal infusion drink from Ecuador containing a mixture of medicinal plants, has been reported to exhibit anti-inflammatory, analgesic, diuretic, and antioxidant activity. The antibacterial activity of each of the plants contained in the horchata mixture has not been fully evaluated. Thus, [...] Read more.
Horchata, a herbal infusion drink from Ecuador containing a mixture of medicinal plants, has been reported to exhibit anti-inflammatory, analgesic, diuretic, and antioxidant activity. The antibacterial activity of each of the plants contained in the horchata mixture has not been fully evaluated. Thus, in this study, we analysed the antibacterial activity of 21 plants used in horchata, collected from the Ecuadorian Andes region, against bacterial strains of clinical importance. The methanolic extract of Cinnamomum sp. showed minimal inhibitory concentration (MIC) values of 250 µg/mL against Staphylococcus aureus ATCC25923 and Methicillin-resistant S. aureus (MRSA), while Pelargonium odoratissimum exhibited a MIC value of 500 µg/mL towards S. aureus ATCC25923. The high-performance liquid chromatography-diode array detector-tandem mass spectrometry (HPLC-DAD-MS/MS) analyses identified in Cinnamomum sp. epicatechin tannins, cinnamaldehyde, and prehelminthosporol molecules, whereas in P. odoratissimum, gallocatechin and epigallocatechin tannins, some flavonoids, and gallic acid and derivatives were identified. Finally, Cinnamomum sp. and P. odoratissimum showed partial inhibition of biofilm formation of S. aureus ATCC25923 and MRSA. Overall, our findings revealed which of the plants used in horchata are responsible for the antibacterial activity attributed to this herbal drink and exhibit the potential for Cinnamomum sp. and P. odoratissimum secondary metabolites to be explored as scaffolds in drug development. Full article
(This article belongs to the Special Issue The Role of Natural Products in Promoting Well-being: From Foods to Drugs)
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12 pages, 5288 KiB  
Article
Comparative Metabolomic Profiling Reveals Key Secondary Metabolites Associated with High Quality and Nutritional Value in Broad Bean (Vicia faba L.)
by Shou-Heng Shi, Seung-Seop Lee, Ya-Ming Zhu, Zhu-Qun Jin, Fei-Bo Wu and Cheng-Wei Qiu
Molecules 2022, 27(24), 8995; https://doi.org/10.3390/molecules27248995 - 16 Dec 2022
Cited by 1 | Viewed by 1421
Abstract
High quality and nutritional benefits are ultimately the desirable features that influence the commercial value and market share of broad bean (Vicia faba L.). Different cultivars vary greatly in taste, flavor, and nutrition. However, the molecular basis of these traits remains largely [...] Read more.
High quality and nutritional benefits are ultimately the desirable features that influence the commercial value and market share of broad bean (Vicia faba L.). Different cultivars vary greatly in taste, flavor, and nutrition. However, the molecular basis of these traits remains largely unknown. Here, the grain metabolites of the superior Chinese landrace Cixidabaican (CX) were detected by a widely targeted metabolomics approach and compared with the main cultivar Lingxiyicun (LX) from Japan. The analyses of global metabolic variations revealed a total of 149 differentially abundant metabolites (DAMs) were identified between these two genotypes. Among them, 84 and 65 were up- and down-regulated in CX compared with LX. Most of the DAMs were closely related to healthy eating substances known for their antioxidant and anti-cancer properties, and some others were involved in the taste formation. The KEGG-based classification further revealed that these DAMs were significantly enriched in 21 metabolic pathways, particularly in flavone and flavonol biosynthesis. The differences in key secondary metabolites, including flavonoids, terpenoids, amino acid derivates, and alkaloids, may lead to more nutritional value in a healthy diet and better adaptability for the seed germination of CX. The present results provide important insights into the taste/quality-forming mechanisms and contributes to the conservation and utilization of germplasm resources for breeding broad bean with superior eating quality. Full article
(This article belongs to the Special Issue The Role of Natural Products in Promoting Well-being: From Foods to Drugs)
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14 pages, 1987 KiB  
Article
Protective Effects of Hippophae rhamnoides L. Phenylpropanoids on Doxorubicin-Induced Cardiotoxicity in Zebrafish
by Gang Li, Ming Chu, Yingying Tong, Yuexin Liang, Shenghui Wang, Chengjun Ma, Zhenhua Wang and Wenna Zhou
Molecules 2022, 27(24), 8858; https://doi.org/10.3390/molecules27248858 - 13 Dec 2022
Cited by 3 | Viewed by 1384
Abstract
Hippophae rhamnoides L. is a deciduous shrub that contains many unique bioactive substances. This sea buckthorn possesses anticancer, antioxidant, anti-inflammatory, and cardiovascular protective properties. Herein, the effects of phenylpropyl compounds extracted from H. rhamnoides L. on doxorubicin (Dox)-induced cardiotoxicity were evaluated in zebrafish. [...] Read more.
Hippophae rhamnoides L. is a deciduous shrub that contains many unique bioactive substances. This sea buckthorn possesses anticancer, antioxidant, anti-inflammatory, and cardiovascular protective properties. Herein, the effects of phenylpropyl compounds extracted from H. rhamnoides L. on doxorubicin (Dox)-induced cardiotoxicity were evaluated in zebrafish. Cardiac injury in zebrafish was induced using 35 μM Dox for 96 h, and 30 μM phenylpropanoid compounds were used as the protective treatment. The cardioprotective effects and mechanisms of the four phenylpropanoids were investigated using microscopy, behavioral analysis, acridine orange staining, western blotting, flow cytometry, and real-time quantitative polymerase chain reaction. The extracted phenylpropanoids could significantly relieve Dox-induced cardiac injury in zebrafish and inhibit cardiomyocyte apoptosis. The mechanisms of action were mainly related to the stability of mitochondrial biogenesis and function maintained by phenylpropanoids in zebrafish. To our knowledge, this is the first report on the protective effect of sea buckthorn against myocardial injury in zebrafish. Our findings provide support for the further research and development of sea buckthorn and its components. Full article
(This article belongs to the Special Issue The Role of Natural Products in Promoting Well-being: From Foods to Drugs)
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13 pages, 5683 KiB  
Article
Isoginkgetin—A Natural Compound to Control U87MG Glioblastoma Cell Growth and Migration Activating Apoptosis and Autophagy
by Maria Antonietta Oliva, Sabrina Staffieri, Massimo Sanchez and Antonietta Arcella
Molecules 2022, 27(23), 8335; https://doi.org/10.3390/molecules27238335 - 29 Nov 2022
Cited by 4 | Viewed by 1670
Abstract
Isoginkgetin (Iso) is a natural bioflavonoid isolated from the leaves of Ginkgo biloba, this natural substance exhibits many healing properties, among which the antitumor effect stands out. Here we tested the effect of Iso on the growth of U87MG glioblastoma cells. Growth [...] Read more.
Isoginkgetin (Iso) is a natural bioflavonoid isolated from the leaves of Ginkgo biloba, this natural substance exhibits many healing properties, among which the antitumor effect stands out. Here we tested the effect of Iso on the growth of U87MG glioblastoma cells. Growth curves and MTT toxicity assays showed time and dose-dependent growth inhibition of U87MG after treatment with Iso (15/25 µM) for 1, 2, and 3 days. The cell growth block of U87MG was further investigated with the colony formation test, which showed that iso treatment for 24 h reduced colony formation. The present study also aimed to evaluate the effect of Iso on U87MG glioblastoma cell migration. The FACS analysis, on the other hand, showed that treatment with Iso 15 µM determines a blockage of the cell cycle in the S1 phase. Further investigation shows that Iso treatment of U87MG altered the protein pathways of homeostasis including autophagy and apoptosis. The present study demonstrated, for the first time, that Iso could represent an excellent adjuvant drug for the treatment of glioblastoma by simultaneously activating multiple mechanisms that control the growth and migration of neoplastic cells. Full article
(This article belongs to the Special Issue The Role of Natural Products in Promoting Well-being: From Foods to Drugs)
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23 pages, 2230 KiB  
Article
Influence of Altitudes and Development Stages on the Chemical Composition, Antioxidant, and Antimicrobial Capacity of the Wild Andean Blueberry (Vaccinium floribundum Kunth)
by Mabel Guevara-Terán, Katherine Padilla-Arias, Andrea Beltrán-Novoa, Ana M. González-Paramás, Francesca Giampieri, Maurizio Battino, Wilson Vásquez-Castillo, Paulina Fernandez-Soto, Eduardo Tejera and José M. Alvarez-Suarez
Molecules 2022, 27(21), 7525; https://doi.org/10.3390/molecules27217525 - 03 Nov 2022
Cited by 8 | Viewed by 2691
Abstract
The chemical composition and biological capacities of berries depend on environmental parameters, maturity, and location. The Andean blueberry (Vaccinium floribundum Kunth), also known as mortiño, presents a unique combination of several phytochemicals, which play a synergistic role in its characterization as a [...] Read more.
The chemical composition and biological capacities of berries depend on environmental parameters, maturity, and location. The Andean blueberry (Vaccinium floribundum Kunth), also known as mortiño, presents a unique combination of several phytochemicals, which play a synergistic role in its characterization as a functional food. We aimed to expose the possible variations that exist in the profile of the phenolic compounds as well as the antioxidant and antimicrobial capacity of the wild Andean blueberry with respect to three ripeness stages and two different altitudes. We found that polyphenols are the predominant compounds in the berry during the early ripeness stage and are the main bioactive compounds that give rise to the antioxidant capacity and inhibition effect on the growth of gram-positive and gram-negative bacteria. Moreover, the accumulation of ascorbic acid, free amino acids, and anthocyanins increases as the ripening process progresses, and they were the main bioactive compounds in the ripe berry. The latter compounds influence the production of the typical bluish or reddish coloration of ripe blueberries. In addition, it was determined that environmental conditions at high altitudes could have a positive influence in all cases. Overall, our data provide evidence regarding the high functional value of the wild Andean blueberry. Full article
(This article belongs to the Special Issue The Role of Natural Products in Promoting Well-being: From Foods to Drugs)
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11 pages, 940 KiB  
Article
First Evidence of Gastroprotection by Schinus molle: Roles of Nitric Oxide, Prostaglandins, and Sulfhydryls Groups in Its Mechanism of Action
by María Elena Sánchez-Mendoza, Yaraset López-Lorenzo, Leticia Cruz-Antonio, Daniel Arrieta-Baez, Miranda Carolina Pérez-González and Jesús Arrieta
Molecules 2022, 27(21), 7321; https://doi.org/10.3390/molecules27217321 - 28 Oct 2022
Cited by 1 | Viewed by 946
Abstract
Schinus molle is a plant traditionally used in Mexico to treat gastric disorders. However, no scientific evidence has been reported on its gastroprotective effect. The aim of the current contribution was to conduct a bioassay-guided study on S. molle to evaluate its gastroprotective [...] Read more.
Schinus molle is a plant traditionally used in Mexico to treat gastric disorders. However, no scientific evidence has been reported on its gastroprotective effect. The aim of the current contribution was to conduct a bioassay-guided study on S. molle to evaluate its gastroprotective activity in a model of Wistar rats given ethanol orally to induce gastric lesions. The hexane and dichloromethane extracts from the tested plant showed over 99% gastroprotection at a dose of 100 mg/kg. From the hexane extract, two of the three fractions (F1 and F2) afforded over 99% gastroprotection. The F1 fraction was subjected to column chromatography, which revealed a white solid. Based on the ESI-MS analysis, the two main compounds in this solid were identified. The predominant compound was probably a triterpene. This mixture of compounds furnished about 67% gastroprotection at a dose of 100 mg/kg. Pretreatment with L-NAME, indomethacin, and NEM was carried out to explore the possible involvement of nitric oxide, prostaglandins, and/or sulfhydryl groups, respectively, in the gastroprotective activity of the white solid. We found evidence for the participation of all three factors. No antisecretory activity was detected (tested by pylorus ligation). In conclusion, evidence is herein provided for the first time of the gastroprotective effect of S. molle. Full article
(This article belongs to the Special Issue The Role of Natural Products in Promoting Well-being: From Foods to Drugs)
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17 pages, 3587 KiB  
Article
Green Extraction of Forsythoside A, Phillyrin and Phillygenol from Forsythia suspensa Leaves Using a β-Cyclodextrin-Assisted Method
by Jing Li, Qiao Qin, Sheng-Hua Zha, Qing-Sheng Zhao, Hang Li, Lu-Peng Liu, Shou-Bu Hou and Bing Zhao
Molecules 2022, 27(20), 7055; https://doi.org/10.3390/molecules27207055 - 19 Oct 2022
Cited by 5 | Viewed by 1490
Abstract
In this study, a green process of β-cyclodextrin (β-CD)-assisted extraction of active ingredients from Forsythia suspensa leaves was developed. Firstly, the optimal process of extraction was as follows: the ratio between Forsythia suspensa leaves and β-CD was 3.61:5, the solid–liquid ratio was 1:36.3, [...] Read more.
In this study, a green process of β-cyclodextrin (β-CD)-assisted extraction of active ingredients from Forsythia suspensa leaves was developed. Firstly, the optimal process of extraction was as follows: the ratio between Forsythia suspensa leaves and β-CD was 3.61:5, the solid–liquid ratio was 1:36.3, the temperature was 75.25 °C and the pH was 3.94. The yields of forsythoside A, phillyrin and phillygenol were 11.80 ± 0.141%, 5.49 ± 0.078% and 0.319 ± 0.004%, respectively. Then, the structure characteristics of the β-CD-assisted extract of Forsythia suspensa leaves (FSE-β-CD) were analyzed using powder X-ray diffraction (PXRD), Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), scanning electron microscopy (SEM) and molecular docking to demonstrate that the natural active products from Forsythia suspensa leaves had significant interactions with the β-CD. Additionally, the loss of forsythoside A from aqueous FSE-CD at 80 °C was only 12%, compared with Forsythia suspensa leaf extract (FSE) which decreased by 13%. In addition, the aqueous solubility of FSE-CD was significantly increased to 70.2 g/L. The EC50 for scavenging DPPH and ABTS radicals decreased to 28.98 ug/mL and 25.54 ug/mL, respectively. The results showed that the β-CD-assisted extraction process would be a promising technology for bioactive compounds extracted from plants. Full article
(This article belongs to the Special Issue The Role of Natural Products in Promoting Well-being: From Foods to Drugs)
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16 pages, 2123 KiB  
Article
Differences in Metabolite Composition of Aloe barbadensis Mill. Extracts Lead to Differential Effects on Human Blood T Cell Activity In Vitro
by Bani Ahluwalia, Maria K. Magnusson, Fredrik Larsson, Otto Savolainen, Alastair B. Ross and Lena Öhman
Molecules 2022, 27(19), 6643; https://doi.org/10.3390/molecules27196643 - 06 Oct 2022
Cited by 3 | Viewed by 1647
Abstract
Aloe barbadensis Mill. (Aloe) is used for diverse therapeutic properties including immunomodulation. However, owing to the compositionally complex nature of Aloe, bioactive component(s) responsible for its beneficial properties, though thought to be attributed to polysaccharides (acemannan), remain unknown. We therefore aimed to determine [...] Read more.
Aloe barbadensis Mill. (Aloe) is used for diverse therapeutic properties including immunomodulation. However, owing to the compositionally complex nature of Aloe, bioactive component(s) responsible for its beneficial properties, though thought to be attributed to polysaccharides (acemannan), remain unknown. We therefore aimed to determine the metabolite composition of various commercial Aloe extracts and assess their effects on human blood T cell activity in vitro. Peripheral blood mononuclear cells (PBMC) from healthy donors were stimulated polyclonally in presence or absence of various Aloe extracts. T cell phenotype and proliferation were investigated by flow cytometry. Aloe extracts were analyzed using targeted 1H-NMR spectroscopy for standard phytochemical quality characterization and untargeted gas chromatography mass spectrometry (GC-MS) for metabolite profiling. Aloe extracts differing in their standard phytochemical composition had varying effects on T cell activation, proliferation, apoptosis, and cell-death in vitro, although this was not related to the acemannan content. Furthermore, each Aloe extract had its own distinct metabolite profile, where extracts rich in diverse sugar and sugar-derivatives were associated with reduced T cell activity. Our results demonstrate that all commercial Aloe extracts are unique with distinct metabolite profiles, which lead to differential effects on T cell activity in vitro, independent of the acemannan content. Full article
(This article belongs to the Special Issue The Role of Natural Products in Promoting Well-being: From Foods to Drugs)
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13 pages, 519 KiB  
Article
Drimane-Type Sesquiterpenoids Derived from the Tropical Basidiomycetes Perenniporia centrali-africana and Cerrena sp. nov
by Paomephan Pathompong, Sebastian Pfütze, Frank Surup, Thitiya Boonpratuang, Rattaket Choeyklin, Josphat C. Matasyoh, Cony Decock, Marc Stadler and Chuenchit Boonchird
Molecules 2022, 27(18), 5968; https://doi.org/10.3390/molecules27185968 - 14 Sep 2022
Cited by 4 | Viewed by 1854
Abstract
Five new drimane-type sesquiterpenoids were isolated from cultures of the tropical basidiomycetes, Perenniporia centrali-africana (originating from Kenya) and Cerrena sp. nov. (originating from Thailand). A new pereniporin A derivative (1), a new drimane-type sesquiterpene lactam (2), and the new [...] Read more.
Five new drimane-type sesquiterpenoids were isolated from cultures of the tropical basidiomycetes, Perenniporia centrali-africana (originating from Kenya) and Cerrena sp. nov. (originating from Thailand). A new pereniporin A derivative (1), a new drimane-type sesquiterpene lactam (2), and the new 6,7-Dehydro-isodrimenediol (3) were isolated from P. centrali-africana. In parallel, the two new drimane-type sesquiterpene lactams 5 and 6 were isolated together with known isodrimenediol (4) from Cerrena sp. This is the first report of drimane-type sesquiterpene lactams from basidiomycetes. The structures were elucidated based on 1D and 2D nuclear magnetic resonance (NMR) spectroscopic data, in combination with high-resolution electrospray mass spectrometric (HR-ESIMS) data. The compounds were devoid of significant antimicrobial and cytotoxic activities. Full article
(This article belongs to the Special Issue The Role of Natural Products in Promoting Well-being: From Foods to Drugs)
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21 pages, 2439 KiB  
Article
Synthesis of Tyrosol and Hydroxytyrosol Glycofuranosides and Their Biochemical and Biological Activities in Cell-Free and Cellular Assays
by Peter Kis, Eva Horváthová, Eliška Gálová, Andrea Ševčovičová, Veronika Antalová, Elena Karnišová Potocká, Vladimír Mastihuba and Mária Mastihubová
Molecules 2021, 26(24), 7607; https://doi.org/10.3390/molecules26247607 - 15 Dec 2021
Cited by 1 | Viewed by 2612
Abstract
Tyrosol (T) and hydroxytyrosol (HOT) and their glycosides are promising candidates for applications in functional food products or in complementary therapy. A series of phenylethanoid glycofuranosides (PEGFs) were synthesized to compare some of their biochemical and biological activities with T and HOT. The [...] Read more.
Tyrosol (T) and hydroxytyrosol (HOT) and their glycosides are promising candidates for applications in functional food products or in complementary therapy. A series of phenylethanoid glycofuranosides (PEGFs) were synthesized to compare some of their biochemical and biological activities with T and HOT. The optimization of glycosylation promoted by environmentally benign basic zinc carbonate was performed to prepare HOT α-L-arabino-, β-D-apio-, and β-D-ribofuranosides. T and HOT β-D-fructofuranosides, prepared by enzymatic transfructosylation of T and HOT, were also included in the comparative study. The antioxidant capacity and DNA-protective potential of T, HOT, and PEGFs on plasmid DNA were determined using cell-free assays. The DNA-damaging potential of the studied compounds for human hepatoma HepG2 cells and their DNA-protective potential on HepG2 cells against hydrogen peroxide were evaluated using the comet assay. Experiments revealed a spectrum of different activities of the studied compounds. HOT and HOT β-D-fructofuranoside appear to be the best-performing scavengers and protectants of plasmid DNA and HepG2 cells. T and T β-D-fructofuranoside display almost zero or low scavenging/antioxidant activity and protective effects on plasmid DNA or HepG2 cells. The results imply that especially HOT β-D-fructofuranoside and β-D-apiofuranoside could be considered as prospective molecules for the subsequent design of supplements with potential in food and health protection. Full article
(This article belongs to the Special Issue The Role of Natural Products in Promoting Well-being: From Foods to Drugs)
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15 pages, 3220 KiB  
Article
Epithelial-to-Mesenchymal Transition Is Not a Major Modulating Factor in the Cytotoxic Response to Natural Products in Cancer Cell Lines
by Baris Kucukkaraduman, Ekin Gokce Cicek, Muhammad Waqas Akbar, Secil Demirkol Canli, Burcak Vural and Ali Osmay Gure
Molecules 2021, 26(19), 5858; https://doi.org/10.3390/molecules26195858 - 27 Sep 2021
Cited by 1 | Viewed by 2368
Abstract
Numerous natural products exhibit antiproliferative activity against cancer cells by modulating various biological pathways. In this study, we investigated the potential use of eight natural compounds (apigenin, curcumin, epigallocatechin gallate, fisetin, forskolin, procyanidin B2, resveratrol, urolithin A) and two repurposed agents (fulvestrant and [...] Read more.
Numerous natural products exhibit antiproliferative activity against cancer cells by modulating various biological pathways. In this study, we investigated the potential use of eight natural compounds (apigenin, curcumin, epigallocatechin gallate, fisetin, forskolin, procyanidin B2, resveratrol, urolithin A) and two repurposed agents (fulvestrant and metformin) as chemotherapy enhancers and mesenchymal-to-epithelial (MET) inducers of cancer cells. Screening of these compounds in various colon, breast, and pancreatic cancer cell lines revealed anti-cancer activity for all compounds, with curcumin being the most effective among these in all cell lines. Although some of the natural products were able to induce MET in some cancer cell lines, the MET induction was not related to increased synergy with either 5-FU, irinotecan, gemcitabine, or gefitinib. When synergy was observed, for example with curcumin and irinotecan, this was unrelated to MET induction, as assessed by changes in E-cadherin and vimentin expression. Our results show that MET induction is compound and cell line specific, and that MET is not necessarily related to enhanced chemosensitivity. Full article
(This article belongs to the Special Issue The Role of Natural Products in Promoting Well-being: From Foods to Drugs)
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16 pages, 2205 KiB  
Article
NMR, RP-HPLC-PDA-ESI-MSn, and RP-HPLC-FD Characterization of Green and Oolong Teas (Camellia sinensis L.)
by Anatoly P. Sobolev, Arianna Di Lorenzo, Simone Circi, Cristina Santarcangelo, Cinzia Ingallina, Maria Daglia and Luisa Mannina
Molecules 2021, 26(17), 5125; https://doi.org/10.3390/molecules26175125 - 24 Aug 2021
Cited by 3 | Viewed by 2802
Abstract
Untargeted (NMR) and targeted (RP-HPLC-PDA-ESI-MSn, RP-HPLC-FD) analytical methodologies were used to determine the bioactive components of 19 tea samples, characterized by different production processes (common tea and GABA tea), degrees of fermentation (green and oolong teas), and harvesting season (autumn and [...] Read more.
Untargeted (NMR) and targeted (RP-HPLC-PDA-ESI-MSn, RP-HPLC-FD) analytical methodologies were used to determine the bioactive components of 19 tea samples, characterized by different production processes (common tea and GABA tea), degrees of fermentation (green and oolong teas), and harvesting season (autumn and spring). The combination of NMR data and a multivariate statistical approach led to a statistical model able to discriminate between GABA and non-GABA teas and green and oolong teas. Targeted analyses showed that green and GABA green teas had similar polyphenol and caffeine contents, but the GABA level was higher in GABA green teas than in regular green tea samples. GABA oolong teas showed lower contents of polyphenols, caffeine, and amino acids, and a higher content of GABA, in comparison with non-GABA oolong teas. In conclusion, the results of this study suggest that the healthy properties of teas, especially GABA teas, have to be evaluated via comprehensive metabolic profiling rather than only the GABA content. Full article
(This article belongs to the Special Issue The Role of Natural Products in Promoting Well-being: From Foods to Drugs)
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11 pages, 466 KiB  
Article
Pharmacokinetics-Driven Evaluation of the Antioxidant Activity of Curcuminoids and Their Major Reduced Metabolites—A Medicinal Chemistry Approach
by Gábor Girst, Sándor B. Ötvös, Ferenc Fülöp, György T. Balogh and Attila Hunyadi
Molecules 2021, 26(12), 3542; https://doi.org/10.3390/molecules26123542 - 10 Jun 2021
Cited by 9 | Viewed by 2536
Abstract
Curcuminoids are the main bioactive components of the well-known Asian spice and traditional medicine turmeric. Curcuminoids have poor chemical stability and bioavailability; in vivo they are rapidly metabolized to a set of bioreduced derivatives and/or glucuronide and sulfate conjugates. The reduced curcuminoid metabolites [...] Read more.
Curcuminoids are the main bioactive components of the well-known Asian spice and traditional medicine turmeric. Curcuminoids have poor chemical stability and bioavailability; in vivo they are rapidly metabolized to a set of bioreduced derivatives and/or glucuronide and sulfate conjugates. The reduced curcuminoid metabolites were also reported to exert various bioactivities in vitro and in vivo. In this work, we aimed to perform a comparative evaluation of curcuminoids and their hydrogenated metabolites from a medicinal chemistry point of view, by determining a set of key pharmacokinetic parameters and evaluating antioxidant potential in relation to such properties.Reduced metabolites were prepared from curcumin and demethoxycurcumin through continuous-flow hydrogenation. As selected pharmacokinetic parameters, kinetic solubility, chemical stability, metabolic stability in human liver microsomes, and parallel artificial membrane permeability assay (PAMPA)-based gastrointestinal and blood-brain barrier permeability were determined. Experimentally determined logP for hydrocurcumins in octanol-water and toluene-water systems provided valuable data on the tendency for intramolecular hydrogen bonding by these compounds. Drug likeness of the compounds were further evaluated by a in silico calculations. Antioxidant properties in diphenyl-2-picrylhydrazyl (DPPH) radical scavenging and oxygen radical absorbance capacity (ORAC) assays were comparatively evaluated through the determination of ligand lipophilic efficiency (LLE). Our results showed dramatically increased water solubility and chemical stability for the reduced metabolites as compared to their corresponding parent compound. Hexahydrocurcumin was found the best candidate for drug development based on a complex pharmacokinetical comparison and high LLE values for its antioxidant properties. Development of tetrahydrocurcumin and tetrahydro-demethoxycurcumin would be limited by their very poor metabolic stability, therefore such an effort would rely on formulations bypassing first-pass metabolism. Full article
(This article belongs to the Special Issue The Role of Natural Products in Promoting Well-being: From Foods to Drugs)
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9 pages, 2085 KiB  
Article
An Insight to the Composition of Pre-Hispanic Mayan Funerary Pigments by 1H-NMR Analysis
by Kadwin J. Pérez-López, Vera Tiesler, Patricia Quintana, Emanuel Hernández-Nuñez and Gloria I. Hernández-Bolio
Molecules 2021, 26(10), 2972; https://doi.org/10.3390/molecules26102972 - 17 May 2021
Viewed by 1862
Abstract
The funerary rites of particular members of the pre-Hispanic Mayan society included the pigmentation of the corpse with a red color. In order to understand this ritual, it is first necessary to identify the constituents of the pigment mixture and then, based on [...] Read more.
The funerary rites of particular members of the pre-Hispanic Mayan society included the pigmentation of the corpse with a red color. In order to understand this ritual, it is first necessary to identify the constituents of the pigment mixture and then, based on its properties, analyze the possible form and moment of application. In the present approach, 1H-NMR analysis was carried to detect organic components in the funerary pigments of Xcambó, a small Maya settlement in the Yucatan Peninsula. The comparison of the spectra belonging to the pigment found in the bone remains of seven individuals, and those from natural materials, led to the identification of beeswax and an abietane resin as constituents of the pigment, thus conferring it agglutinant and aromatic properties, respectively. The 1H-NMR analysis also allowed to rule out the presence of copal, a resin found in the pigment cover from paramount chiefs from the Mayan society. Additionally, a protocol for the extraction of the organic fraction from the bone segment without visible signs of analysis was developed, thus broadening the techniques available to investigate these valuable samples. Full article
(This article belongs to the Special Issue The Role of Natural Products in Promoting Well-being: From Foods to Drugs)
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17 pages, 3022 KiB  
Article
Concentration-Dependent Pro- and Antitumor Activities of Quercetin in Human Melanoma Spheroids: Comparative Analysis of 2D and 3D Cell Culture Models
by Harald Hundsberger, Anna Stierschneider, Victoria Sarne, Doris Ripper, Jasmin Schimon, Hans Peter Weitzenböck, Dominik Schild, Nico Jacobi, Andreas Eger, Josef Atzler, Christian T. Klein and Christoph Wiesner
Molecules 2021, 26(3), 717; https://doi.org/10.3390/molecules26030717 - 30 Jan 2021
Cited by 11 | Viewed by 3556
Abstract
Quercetin, a dietary flavonoid found in fruits and vegetables, has been described as a substance with many anti-cancer properties in a variety of preclinical investigations. In the present study, we demonstrate that 2D and 3D melanoma models exhibit not only different sensitivities to [...] Read more.
Quercetin, a dietary flavonoid found in fruits and vegetables, has been described as a substance with many anti-cancer properties in a variety of preclinical investigations. In the present study, we demonstrate that 2D and 3D melanoma models exhibit not only different sensitivities to quercetin, but also opposite, cancer-promoting effects when metastatic melanoma spheroids are treated with quercetin. Higher concentrations of quercetin reduce melanoma growth in three tested cell lines, whereas low concentrations induce the opposite effect in metastatic melanoma spheroids but not in the non-metastatic cell line. High (>12.5 µM) or low (<6.3 µM) quercetin concentrations decrease or enhance cell viability, spheroid size, and cell proliferation, respectively. Additionally, melanoma cells cultivated in 2D already show significant caspase 3 activity at very low concentrations (>0.4 µM), whereas in 3D spheroids apoptotic cells, caspase 3 activity can only be detected in concentrations ≥12.5 µM. Further, we show that the tumor promoting or repressing effect in the 3D metastatic melanoma spheroids are likely to be elicited by a precisely controlled regulation of Nrf2/ARE-mediated cytoprotective genes, as well as ERK and NF-κB phosphorylation. According to the results obtained here, further studies are needed to better characterize the mechanisms of action underlying the pro- and anti-carcinogenic effects of quercetin on human melanomas. Full article
(This article belongs to the Special Issue The Role of Natural Products in Promoting Well-being: From Foods to Drugs)
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12 pages, 2703 KiB  
Article
A Methanol Extract of Scabiosa atropurpurea Enhances Doxorubicin Cytotoxicity against Resistant Colorectal Cancer Cells In Vitro
by Imene Ben Toumia, Mansour Sobeh, Marco Ponassi, Barbara Banelli, Anas Dameriha, Michael Wink, Leila Chekir Ghedira and Camillo Rosano
Molecules 2020, 25(22), 5265; https://doi.org/10.3390/molecules25225265 - 12 Nov 2020
Cited by 14 | Viewed by 2633
Abstract
Colorectal cancer is a malignancy with a high incidence. Currently, the drugs used in chemotherapy are often accompanied by strong side effects. Natural secondary metabolites can interfere with chemotherapeutic drugs and intensify their cytotoxic effects. This study aimed to profile the secondary metabolites [...] Read more.
Colorectal cancer is a malignancy with a high incidence. Currently, the drugs used in chemotherapy are often accompanied by strong side effects. Natural secondary metabolites can interfere with chemotherapeutic drugs and intensify their cytotoxic effects. This study aimed to profile the secondary metabolites from the methanol extract of Scabiosa atropurpurea and investigate their in vitro activities, alone or in combination with the chemotherapeutic agent doxorubicin. MTT assay was used to determine the cytotoxic activities. Annexin-V/PI double-staining analysis was employed to evaluate the apoptotic concentration. Multicaspase assay, quantitative reverse transcription real-time PCR (RT-qPCR), and ABC transporter activities were also performed. LC-MS analysis revealed 31 compounds including phenolic acids, flavonoids, and saponins. S. atropurpurea extract intensified doxorubicin anti-proliferative effects against resistant tumor cells and enhanced the cytotoxic effects towards Caco-2 cells after 48 h. The mRNA expression levels of Bax, caspase-3, and p21 were increased significantly whereas Bcl-2 expression level was decreased. Furthermore, the methanol extract reversed P-glycoprotein or multidrug resistance-associated protein in Caco-2 cells. In conclusion, S. atropurpurea improved chemosensitivity and modulated multidrug resistance in Caco-2 cells which makes it a good candidate for further research in order to develop a new potential cancer treatment. Full article
(This article belongs to the Special Issue The Role of Natural Products in Promoting Well-being: From Foods to Drugs)
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Review

Jump to: Research

28 pages, 2842 KiB  
Review
The Epigenetic Effects of Coffee
by Qi Ding, Yan-Ming Xu and Andy T. Y. Lau
Molecules 2023, 28(4), 1770; https://doi.org/10.3390/molecules28041770 - 13 Feb 2023
Cited by 6 | Viewed by 5152
Abstract
In this review, we discuss the recent knowledge regarding the epigenetic effects of coffee extract and the three essential active ingredients in coffee (caffeine, chlorogenic acid, and caffeic acid). As a popular beverage, coffee has many active ingredients which have a variety of [...] Read more.
In this review, we discuss the recent knowledge regarding the epigenetic effects of coffee extract and the three essential active ingredients in coffee (caffeine, chlorogenic acid, and caffeic acid). As a popular beverage, coffee has many active ingredients which have a variety of biological functions such as insulin sensitization, improvement of sugar metabolism, antidiabetic properties, and liver protection. However, recent researches have shown that coffee is not only beneficial for human, but also bad, which may be due to its complex components. Studies suggest that coffee extract and its components can potentially impact gene expression via alteration of DNA methylation, histone modifications, and ncRNA expression; thus, exert long lasting impacts on the epigenome. More importantly, coffee consumption during pregnancy has been linked to multiple negative effects on offspring due to epigenetic modifications; on the other hand, it has also been linked to improvements in many diseases, including cancer. Therefore, understanding more about the epigenetic effects associated with coffee components is crucial to finding ways for improving human health. Full article
(This article belongs to the Special Issue The Role of Natural Products in Promoting Well-being: From Foods to Drugs)
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24 pages, 866 KiB  
Review
Antioxidant and Anti-Inflammatory Compounds from Edible Plants with Anti-Cancer Activity and Their Potential Use as Drugs
by Sofía Isabel Cuevas-Cianca, Cristian Romero-Castillo, José Luis Gálvez-Romero, Zaida Nelly Juárez and Luis Ricardo Hernández
Molecules 2023, 28(3), 1488; https://doi.org/10.3390/molecules28031488 - 03 Feb 2023
Cited by 12 | Viewed by 4088
Abstract
Food is our daily companion, performing numerous beneficial functions for our bodies. Many of them can help to alleviate or prevent ailments and diseases. In this review, an extensive bibliographic search is conducted in various databases to update information on unprocessed foods with [...] Read more.
Food is our daily companion, performing numerous beneficial functions for our bodies. Many of them can help to alleviate or prevent ailments and diseases. In this review, an extensive bibliographic search is conducted in various databases to update information on unprocessed foods with anti-inflammatory and antioxidant properties that can aid in treating diseases such as cancer. The current state of knowledge on inflammatory processes involving some interleukins and tumor necrosis factor-alpha (TNF-α) is reviewed. As well as unprocessed foods, which may help reduce inflammation and oxidative stress, both of which are important factors in cancer development. Many studies are still needed to take full advantage of the food products we use daily. Full article
(This article belongs to the Special Issue The Role of Natural Products in Promoting Well-being: From Foods to Drugs)
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48 pages, 7519 KiB  
Review
Synthesis, Biosynthesis, and Biological Activity of Diels–Alder Adducts from Morus Genus: An Update
by Carola Tortora, Luca Pisano, Valeria Vergine, Francesca Ghirga, Antonia Iazzetti, Andrea Calcaterra, Violeta Marković, Bruno Botta and Deborah Quaglio
Molecules 2022, 27(21), 7580; https://doi.org/10.3390/molecules27217580 - 04 Nov 2022
Cited by 4 | Viewed by 2148
Abstract
The plants of the Moraceae family are producers of a great variety of polyphenolic natural products. Among these, the Diels–Alder type adducts (DAAs) are endowed with a unique cyclohexene scaffold, since they are biosynthesized from [4+2] cycloaddition of different polyphenolic precursors such as [...] Read more.
The plants of the Moraceae family are producers of a great variety of polyphenolic natural products. Among these, the Diels–Alder type adducts (DAAs) are endowed with a unique cyclohexene scaffold, since they are biosynthesized from [4+2] cycloaddition of different polyphenolic precursors such as chalcones and dehydroprenyl polyphenols. To date, more than 150 DAAs have been isolated and characterized from Moraceous and related plants. The main source of DAAs is the mulberry root bark, also known as “Sang-Bai-Pi” in Traditional Chinese Medicine, but they have also been isolated from root bark, stem barks, roots, stems or twigs, leaves, and callus cultures of Moraceous and other related plants. Since 1980, many biological activities of DAAs have been identified, including anti-HIV, antimicrobial, anti-inflammatory, and anticancer ones. For these reasons, natural DAAs have been intensively investigated, and a lot of efforts have been made to study their biosynthesis and to establish practical synthetic access. In this review, we summarized all the updated knowledge on biosynthesis, chemoenzymatic synthesis, racemic and enantioselective total synthesis, and biological activity of natural DAAs from Moraceous and related plants. Full article
(This article belongs to the Special Issue The Role of Natural Products in Promoting Well-being: From Foods to Drugs)
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50 pages, 4220 KiB  
Review
Combination Anticancer Therapies Using Selected Phytochemicals
by Wamidh H. Talib, Dima Awajan, Reem Ali Hamed, Aya O. Azzam, Asma Ismail Mahmod and Intisar Hadi AL-Yasari
Molecules 2022, 27(17), 5452; https://doi.org/10.3390/molecules27175452 - 25 Aug 2022
Cited by 23 | Viewed by 3984
Abstract
Cancer is still one of the most widespread diseases globally, it is considered a vital health challenge worldwide and one of the main barriers to long life expectancy. Due to the potential toxicity and lack of selectivity of conventional chemotherapeutic agents, discovering alternative [...] Read more.
Cancer is still one of the most widespread diseases globally, it is considered a vital health challenge worldwide and one of the main barriers to long life expectancy. Due to the potential toxicity and lack of selectivity of conventional chemotherapeutic agents, discovering alternative treatments is a top priority. Plant-derived natural products have high potential in cancer treatment due to their multiple mechanisms of action, diversity in structure, availability in nature, and relatively low toxicity. In this review, the anticancer mechanisms of the most common phytochemicals were analyzed. Furthermore, a detailed discussion of the anticancer effect of combinations consisting of natural product or natural products with chemotherapeutic drugs was provided. This review should provide a strong platform for researchers and clinicians to improve basic and clinical research in the development of alternative anticancer medicines. Full article
(This article belongs to the Special Issue The Role of Natural Products in Promoting Well-being: From Foods to Drugs)
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37 pages, 2324 KiB  
Review
Natural Products in Mitigation of Bisphenol A Toxicity: Future Therapeutic Use
by Srinivasa Rao Sirasanagandla, Isehaq Al-Huseini, Hussein Sakr, Marzie Moqadass, Srijit Das, Norsham Juliana and Izuddin Fahmy Abu
Molecules 2022, 27(17), 5384; https://doi.org/10.3390/molecules27175384 - 24 Aug 2022
Cited by 13 | Viewed by 4082
Abstract
Bisphenol A (BPA) is a ubiquitous environmental toxin with deleterious endocrine-disrupting effects. It is widely used in producing epoxy resins, polycarbonate plastics, and polyvinyl chloride plastics. Human beings are regularly exposed to BPA through inhalation, ingestion, and topical absorption routes. The prevalence of [...] Read more.
Bisphenol A (BPA) is a ubiquitous environmental toxin with deleterious endocrine-disrupting effects. It is widely used in producing epoxy resins, polycarbonate plastics, and polyvinyl chloride plastics. Human beings are regularly exposed to BPA through inhalation, ingestion, and topical absorption routes. The prevalence of BPA exposure has considerably increased over the past decades. Previous research studies have found a plethora of evidence of BPA’s harmful effects. Interestingly, even at a lower concentration, this industrial product was found to be harmful at cellular and tissue levels, affecting various body functions. A noble and possible treatment could be made plausible by using natural products (NPs). In this review, we highlight existing experimental evidence of NPs against BPA exposure-induced adverse effects, which involve the body’s reproductive, neurological, hepatic, renal, cardiovascular, and endocrine systems. The review also focuses on the targeted signaling pathways of NPs involved in BPA-induced toxicity. Although potential molecular mechanisms underlying BPA-induced toxicity have been investigated, there is currently no specific targeted treatment for BPA-induced toxicity. Hence, natural products could be considered for future therapeutic use against adverse and harmful effects of BPA exposure. Full article
(This article belongs to the Special Issue The Role of Natural Products in Promoting Well-being: From Foods to Drugs)
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29 pages, 2246 KiB  
Review
Curcumin-Based Nanoformulations: A Promising Adjuvant towards Cancer Treatment
by Salar Hafez Ghoran, Andrea Calcaterra, Milad Abbasi, Fatemeh Taktaz, Kay Nieselt and Esmaeil Babaei
Molecules 2022, 27(16), 5236; https://doi.org/10.3390/molecules27165236 - 16 Aug 2022
Cited by 33 | Viewed by 6853
Abstract
Throughout the United States, cancer remains the second leading cause of death. Traditional treatments induce significant medical toxic effects and unpleasant adverse reactions, making them inappropriate for long-term use. Consequently, anticancer-drug resistance and relapse are frequent in certain situations. Thus, there is an [...] Read more.
Throughout the United States, cancer remains the second leading cause of death. Traditional treatments induce significant medical toxic effects and unpleasant adverse reactions, making them inappropriate for long-term use. Consequently, anticancer-drug resistance and relapse are frequent in certain situations. Thus, there is an urgent necessity to find effective antitumor medications that are specific and have few adverse consequences. Curcumin is a polyphenol derivative found in the turmeric plant (Curcuma longa L.), and provides chemopreventive, antitumor, chemo-, and radio-sensitizing properties. In this paper, we summarize the new nano-based formulations of polyphenolic curcumin because of the growing interest in its application against cancers and tumors. According to recent studies, the use of nanoparticles can overcome the hydrophobic nature of curcumin, as well as improving its stability and cellular bioavailability in vitro and in vivo. Several strategies for nanocurcumin production have been developed, each with its own set of advantages and unique features. Because the majority of the curcumin-based nanoformulation evidence is still in the conceptual stage, there are still numerous issues impeding the provision of nanocurcumin as a possible therapeutic option. To support the science, further work is necessary to develop curcumin as a viable anti-cancer adjuvant. In this review, we cover the various curcumin nanoformulations and nanocurcumin implications for therapeutic uses for cancer, as well as the current state of clinical studies and patents. We further address the knowledge gaps and future research orientations required to develop curcumin as a feasible treatment candidate. Full article
(This article belongs to the Special Issue The Role of Natural Products in Promoting Well-being: From Foods to Drugs)
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23 pages, 2894 KiB  
Review
Natural Polyphenols as SERCA Activators: Role in the Endoplasmic Reticulum Stress-Related Diseases
by Jana Viskupicova and Petronela Rezbarikova
Molecules 2022, 27(16), 5095; https://doi.org/10.3390/molecules27165095 - 10 Aug 2022
Cited by 3 | Viewed by 3308
Abstract
Sarco/endoplasmic reticulum Ca2+-ATPase (SERCA) is a key protein responsible for transporting Ca2+ ions from the cytosol into the lumen of the sarco/endoplasmic reticulum (SR/ER), thus maintaining Ca2+ homeostasis within cells. Accumulating evidence suggests that impaired SERCA function is associated [...] Read more.
Sarco/endoplasmic reticulum Ca2+-ATPase (SERCA) is a key protein responsible for transporting Ca2+ ions from the cytosol into the lumen of the sarco/endoplasmic reticulum (SR/ER), thus maintaining Ca2+ homeostasis within cells. Accumulating evidence suggests that impaired SERCA function is associated with disruption of intracellular Ca2+ homeostasis and induction of ER stress, leading to different chronic pathological conditions. Therefore, appropriate strategies to control Ca2+ homeostasis via modulation of either SERCA pump activity/expression or relevant signaling pathways may represent a useful approach to combat pathological states associated with ER stress. Natural dietary polyphenolic compounds, such as resveratrol, gingerol, ellagic acid, luteolin, or green tea polyphenols, with a number of health-promoting properties, have been described either to increase SERCA activity/expression directly or to affect Ca2+ signaling pathways. In this review, potential Ca2+-mediated effects of the most studied polyphenols on SERCA pumps or related Ca2+ signaling pathways are summarized, and relevant mechanisms of their action on Ca2+ regulation with respect to various ER stress-related states are depicted. All data were collected using scientific search tools (i.e., Science Direct, PubMed, Scopus, and Google Scholar). Full article
(This article belongs to the Special Issue The Role of Natural Products in Promoting Well-being: From Foods to Drugs)
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17 pages, 1679 KiB  
Review
Pathophysiology of Depression: Stingless Bee Honey Promising as an Antidepressant
by Fatin Haniza Zakaria, Ismail Samhani, Mohd Zulkifli Mustafa and Nazlahshaniza Shafin
Molecules 2022, 27(16), 5091; https://doi.org/10.3390/molecules27165091 - 10 Aug 2022
Cited by 4 | Viewed by 7014
Abstract
Depression is a debilitating psychiatric disorder impacting an individual’s quality of life. It is the most prevalent mental illness across all age categories, incurring huge socio-economic impacts. Most depression treatments currently focus on the elevation of neurotransmitters according to the monoamine hypothesis. Conventional [...] Read more.
Depression is a debilitating psychiatric disorder impacting an individual’s quality of life. It is the most prevalent mental illness across all age categories, incurring huge socio-economic impacts. Most depression treatments currently focus on the elevation of neurotransmitters according to the monoamine hypothesis. Conventional treatments include tricyclic antidepressants (TCAs), norepinephrine–dopamine reuptake inhibitors (NDRIs), monoamine oxidase inhibitors (MAOIs), and serotonin reuptake inhibitors (SSRIs). Despite numerous pharmacological strategies utilising conventional drugs, the discovery of alternative medicines from natural products is a must for safer and beneficial brain supplement. About 30% of patients have been reported to show resistance to drug treatments coupled with functional impairment, poor quality of life, and suicidal ideation with a high relapse rate. Hence, there is an urgency for novel discoveries of safer and highly effective depression treatments. Stingless bee honey (SBH) has been proven to contain a high level of antioxidants compared to other types of honey. This is a comprehensive review of the potential use of SBH as a new candidate for antidepressants from the perspective of the monoamine, inflammatory and neurotrophin hypotheses. Full article
(This article belongs to the Special Issue The Role of Natural Products in Promoting Well-being: From Foods to Drugs)
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27 pages, 2194 KiB  
Review
The Potential of Lamiaceae Herbs for Mitigation of Overweight, Obesity, and Fatty Liver: Studies and Perspectives
by Farah Diab, Hawraa Zbeeb, Francesca Baldini, Piero Portincasa, Mohamad Khalil and Laura Vergani
Molecules 2022, 27(15), 5043; https://doi.org/10.3390/molecules27155043 - 08 Aug 2022
Cited by 5 | Viewed by 3522
Abstract
Numerous plants, plant extracts, and plant-derived compounds are being explored for their beneficial effects against overweight and liver diseases. Obesity is associated with the increased prevalence of non-alcoholic fatty liver disease (NAFLD), becoming the most common liver disease in Western countries. Obesity and [...] Read more.
Numerous plants, plant extracts, and plant-derived compounds are being explored for their beneficial effects against overweight and liver diseases. Obesity is associated with the increased prevalence of non-alcoholic fatty liver disease (NAFLD), becoming the most common liver disease in Western countries. Obesity and NAFLD are closely associated with many other metabolic alternations such as insulin resistance, diabetes mellitus, and cardiovascular diseases. Many herbs of the Lamiaceae family are widely employed as food and spices in the Mediterranean area, but also in folk medicine, and their use for the management of metabolic disorders is well documented. Hereby, we summarized the scientific results of the medicinal and nutraceutical potential of plants from the Lamiaceae family for prevention and mitigation of overweight and fatty liver. The evidence indicates that Lamiaceae plants may be a cost-effective source of nutraceuticals and/or phytochemicals to be used in the management of metabolic-related conditions such as obesity and NAFLD. PubMed, Google Scholar, Scopus, and SciFinder were accessed to collect data on traditional medicinal plants, compounds derived from plants, their reported anti-obesity mechanisms, and therapeutic targets. Full article
(This article belongs to the Special Issue The Role of Natural Products in Promoting Well-being: From Foods to Drugs)
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41 pages, 3661 KiB  
Review
Plants as a Source of Anticancer Agents: From Bench to Bedside
by Wamidh H. Talib, Safa Daoud, Asma Ismail Mahmod, Reem Ali Hamed, Dima Awajan, Sara Feras Abuarab, Lena Hisham Odeh, Samar Khater and Lina T. Al Kury
Molecules 2022, 27(15), 4818; https://doi.org/10.3390/molecules27154818 - 27 Jul 2022
Cited by 24 | Viewed by 4457
Abstract
Cancer is the second leading cause of death after cardiovascular diseases. Conventional anticancer therapies are associated with lack of selectivity and serious side effects. Cancer hallmarks are biological capabilities acquired by cancer cells during neoplastic transformation. Targeting multiple cancer hallmarks is a promising [...] Read more.
Cancer is the second leading cause of death after cardiovascular diseases. Conventional anticancer therapies are associated with lack of selectivity and serious side effects. Cancer hallmarks are biological capabilities acquired by cancer cells during neoplastic transformation. Targeting multiple cancer hallmarks is a promising strategy to treat cancer. The diversity in chemical structure and the relatively low toxicity make plant-derived natural products a promising source for the development of new and more effective anticancer therapies that have the capacity to target multiple hallmarks in cancer. In this review, we discussed the anticancer activities of ten natural products extracted from plants. The majority of these products inhibit cancer by targeting multiple cancer hallmarks, and many of these chemicals have reached clinical applications. Studies discussed in this review provide a solid ground for researchers and physicians to design more effective combination anticancer therapies using plant-derived natural products. Full article
(This article belongs to the Special Issue The Role of Natural Products in Promoting Well-being: From Foods to Drugs)
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22 pages, 2755 KiB  
Review
A Double-Edged Sword: Thioxanthenes Act on Both the Mind and the Microbiome
by Marianne Ø. Poulsen, Sujata G. Dastidar, Debalina Sinha Roy, Shauroseni Palchoudhuri, Jette Elisabeth H. Kristiansen and Stephen J. Fey
Molecules 2022, 27(1), 196; https://doi.org/10.3390/molecules27010196 - 29 Dec 2021
Cited by 4 | Viewed by 2639
Abstract
The rising tide of antibacterial drug resistance has given rise to the virtual elimination of numerous erstwhile antibiotics, intensifying the urgent demand for novel agents. A number of drugs have been found to possess potent antimicrobial action during the past several years and [...] Read more.
The rising tide of antibacterial drug resistance has given rise to the virtual elimination of numerous erstwhile antibiotics, intensifying the urgent demand for novel agents. A number of drugs have been found to possess potent antimicrobial action during the past several years and have the potential to supplement or even replace the antibiotics. Many of these ‘non-antibiotics’, as they are referred to, belong to the widely used class of neuroleptics, the phenothiazines. Another chemically and pharmacologically related class is the thioxanthenes, differing in that the aromatic N of the central phenothiazine ring has been replaced by a C atom. Such “carbon-analogues” were primarily synthesized with the hope that these would be devoid of some of the toxic effects of phenothiazines. Intensive studies on syntheses, as well as chemical and pharmacological properties of thioxanthenes, were initiated in the late 1950s. Although a rather close parallelism with respect to structure activity relationships could be observed between phenothiazines and thioxanthenes; several thioxanthenes were synthesized in pharmaceutical industries and applied for human use as neuroleptics. Antibacterial activities of thioxanthenes came to be recognized in the early 1980s in Europe. During the following years, many of these drugs were found not only to be antibacterial agents but also to possess anti-mycobacterial, antiviral (including anti-HIV and anti-SARS-CoV-2) and anti-parasitic properties. Thus, this group of drugs, which has an inhibitory effect on the growth of a wide variety of microorganisms, needs to be explored for syntheses of novel antimicrobial agents. The purpose of this review is to summarize the neuroleptic and antimicrobial properties of this exciting group of bioactive molecules with a goal of identifying potential structures worthy of future exploration. Full article
(This article belongs to the Special Issue The Role of Natural Products in Promoting Well-being: From Foods to Drugs)
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32 pages, 7645 KiB  
Review
Drugs That Changed Society: History and Current Status of the Early Antibiotics: Salvarsan, Sulfonamides, and β-Lactams
by Søren Brøgger Christensen
Molecules 2021, 26(19), 6057; https://doi.org/10.3390/molecules26196057 - 07 Oct 2021
Cited by 25 | Viewed by 6079
Abstract
The appearance of antibiotic drugs revolutionized the possibilities for treatment of diseases with high mortality such as pneumonia, sepsis, plaque, diphtheria, tetanus, typhoid fever, and tuberculosis. Today fewer than 1% of mortalities in high income countries are caused by diseases caused by bacteria. [...] Read more.
The appearance of antibiotic drugs revolutionized the possibilities for treatment of diseases with high mortality such as pneumonia, sepsis, plaque, diphtheria, tetanus, typhoid fever, and tuberculosis. Today fewer than 1% of mortalities in high income countries are caused by diseases caused by bacteria. However, it should be recalled that the antibiotics were introduced in parallel with sanitation including sewerage, piped drinking water, high standard of living and improved understanding of the connection between food and health. Development of salvarsan, sulfonamides, and β-lactams into efficient drugs is described. The effects on life expectancy and life quality of these new drugs are indicated. Full article
(This article belongs to the Special Issue The Role of Natural Products in Promoting Well-being: From Foods to Drugs)
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25 pages, 7855 KiB  
Review
Stemodane Diterpenes and Diterpenoids: Isolation, Structure Elucidation, Biogenesis, Biosynthesis, Biological Activity, Biotransformations, Metabolites and Derivatives Biological Activity, Rearrangements
by Francesca Leonelli, Luisa Maria Migneco, Alessio Valletta and Rinaldo Marini Bettolo
Molecules 2021, 26(9), 2761; https://doi.org/10.3390/molecules26092761 - 07 May 2021
Cited by 3 | Viewed by 2196
Abstract
The scientific activity carried out over forty-five years on stemodane diterpenes and diterpenoids structure elucidation, biogenesis, biosynthesis, biological activity and biotransformations was reviewed. Full article
(This article belongs to the Special Issue The Role of Natural Products in Promoting Well-being: From Foods to Drugs)
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