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Discovery of Bioactive Ingredients from Natural Products, 5th Edition
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Discovery of Bioactive Ingredients from Natural Products, 5th Edition

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

Deadline for manuscript submissions: closed (31 October 2024) | Viewed by 10185

Special Issue Editors

Dr. Simona Fabroni

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Guest Editor
Council for Agricultural Research and Economics (CREA)—Research Center for Olive, Fruit and Citrus Crops, Corso Savoia 190, 95024 Acireale, Italy
Interests: citrus bioactive compounds; recovery of high value compounds from fruit processing wastes; mild food processing; quality of foods; traceability of organic food productions
Special Issues, Collections and Topics in MDPI journals
Dr. Krystian Marszałek

E-Mail Website
Guest Editor
Department of Fruit and Vegetable Product Technology, Prof. Wacław Dąbrowski Institute of Agricultural and Food Biotechnology, Rakowiecka 36, 02-532 Warsaw, Poland
Interests: fruits; vegetables; emerging techniques; food processing and preservation; bioaccessibility and bioavailability; high-pressure processing; high-pressure homogenization; high-pressure carbon dioxide; ultrasounds; microwaves; food chemistry
Special Issues, Collections and Topics in MDPI journals
Dr. Aldo Todaro

E-Mail Website
Guest Editor
Dipartimento di Agricoltura, Alimentazione e Ambiente, University of Catania, Via S. Sofia 100, 95123 Catania, Italy
Interests: fruit quality; horticultural physiology and preservation recovery of high value compounds from food processing wastes; fruit processing
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The Mediterranean diet is recognized worldwide as being associated with a lower risk of cancer, heart disease, and stroke. This lower risk is universally ascribed to the high intake of vegetables and fruits and, consequently, the high ingestion of phytochemicals. At present, there is a great interest in the development of new nutraceuticals of natural origin for use within the pharmaceutical field and/or as dietary supplements. For instance, the agri-food industry produces a large amount of waste, which can be conveniently used for the recovery of valuable health-promoting compounds for use as natural ingredients.

Therefore, this Special Issue of Molecules is dedicated to original research and review articles that cover the latest findings on new extraction techniques for the recovery of bioactive constituents from fruit and/or vegetables, the chemical characterization of phytoextracts with valuable biological activity, in vivo tests and in vitro bioassays to support biological activity of purified compounds, and complex extracts and/or combined extracts derived from different matrices. Studies focusing on the valorization of bioactive extracts derived from traditional or ancient plant and/or fruit species are also welcome.

Dr. Simona Fabroni
Dr. Krystian Marszałek
Dr. Aldo Todaro
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. 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

  • bioactive constituents
  • phytoextract
  • biological activity
  • natural products
  • natural compounds
  • marine compounds
  • herbals
  • phytochemicals

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Related Special Issues

Published Papers (7 papers)

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Research

19 pages, 3000 KiB  
Article
Immunomodulatory Effects of Copper Bis-Glycinate In Vitro
by Alexander Areesanan, Luise Wolf, Sven Nicolay, Amy Marisa Zimmermann-Klemd and Carsten Gründemann
Molecules 2025, 30(6), 1282; https://doi.org/10.3390/molecules30061282 - 13 Mar 2025
Viewed by 465
Abstract
Copper functions as a cofactor and antioxidants in a large number of enzymes that are important for cellular respiration and the nervous system. In the last century scholars have explored copper’s relationship with the immune system, with copper deficiency drastically upsetting the overall [...] Read more.
Copper functions as a cofactor and antioxidants in a large number of enzymes that are important for cellular respiration and the nervous system. In the last century scholars have explored copper’s relationship with the immune system, with copper deficiency drastically upsetting the overall function of the immune system, as seen in symptoms such as increased susceptibility to pathogens, decreased proliferation of lymphocytes, and impaired function of both cytotoxic T lymphocytes and helper T cells. Among copper’s various forms, copper bis-glycinate (Cbg) has been used as an official EU-approved oral supplement to promote health. In this study, we observed the influence of Cbg on human epithelial cells (HCE-T cells) to determine its cytotoxicity, anti-reactive oxygen (ROS), and wound healing capabilities. We also evaluated Cbg’s anti-inflammatory immune cells like primary human mononuclear cells (PBMCs), monocytic THP-1, and Jurkat cells in the context of anti-inflammation. At all the investigated concentrations of Cbg (0.05–100 μg/mL), ther was no considerable impact detected on the epithelial cells. However, the proliferation rate of stimulated PBMCs was affected progressively (3–50 μg/mL). In CD4+ helper T cells, interleukin (IL)-17 and IL-2 cytokine levels were decreased in a dose-dependent manner, while interferon (IFN)-γ and IL-2 levels were slightly decreased with no noticeable changes between each treated concentration. Furthermore, stimulated monocytic THP-1 cells treated with Cbg reduced IL-6 and significantly reduced tumor necrosis factor (TNF)-α cytokines secretion. Lastly, stimulated Jurkat intracellular Ca2+ influx was significantly inhibited in a dose-dependent manner. Taken together, this study demonstrated that copper possesses modulatory effects on immune cells but not on epithelial cells, but further studies are needed to underline this hypothesis. Full article
(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 5th Edition)
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12 pages, 248 KiB  
Article
Biological and Health-Promoting Potential of Fruits from Three Cold-Hardy Actinidia Species
by Piotr Latocha, Ana Margarida Silva, Manuela M. Moreira, Cristina Delerue-Matos and Francisca Rodrigues
Molecules 2025, 30(2), 246; https://doi.org/10.3390/molecules30020246 - 9 Jan 2025
Viewed by 909
Abstract
Fruits are essential components of the human diet, valued for their diverse bioactive compounds with potential health-promoting properties. This study focuses on three cold-hardy Actinidia species, namely A. arguta, A. kolomikta, and A. polygama, examining their polyphenolic content, antioxidant/antiradical activities, [...] Read more.
Fruits are essential components of the human diet, valued for their diverse bioactive compounds with potential health-promoting properties. This study focuses on three cold-hardy Actinidia species, namely A. arguta, A. kolomikta, and A. polygama, examining their polyphenolic content, antioxidant/antiradical activities, scavenging capacity and effects on intestinal cell viability (Caco-2 and HT29-MTX). A comprehensive profile of their phenolic compounds was identified, in descending order of total polyphenol content: A. kolomikta > A. arguta > A. polygama. Across species, 16 phenolic acids, 2 flavanols, 2 flavanones, 11 flavonols, and 3 flavones were quantified, with caffeine as a prominent compound. A. kolomikta achieved the highest antioxidant activity, with ‘Vitakola’ cultivar showing almost double the antioxidant activity compared to ‘Tallinn’ and ‘Pozdni’. By contrast, A. arguta ‘Geneva’ and A. polygama ‘Pomarancheva’ exhibited significantly lower activity in both FRAP and DPPH assays. Notably, A. kolomikta cultivars showed distinct radical-scavenging capacities, particularly for superoxide, wherein ‘Tallinn’ and ‘Pozdni’ achieved the highest values. Cell viability tests on Caco-2 and HT29-MTX cells revealed a dose-dependent reduction in viability, notably stronger in Caco-2 cells. Overall, this study underscores the therapeutic potential of Actinidia species. Full article
(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 5th Edition)
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18 pages, 3034 KiB  
Article
Antidiabetic Potential of Black Elderberry Cultivars Flower Extracts: Phytochemical Profile and Enzyme Inhibition
by Elżbieta Studzińska-Sroka, Magdalena Paczkowska-Walendowska, Justyna Kledzik, Agnieszka Galanty, Anna Gościniak, Piotr Szulc, Katarzyna Korybalska and Judyta Cielecka-Piontek
Molecules 2024, 29(23), 5775; https://doi.org/10.3390/molecules29235775 - 6 Dec 2024
Viewed by 1931
Abstract
Black elderberry (Sambucus nigra L.) flowers are rich in polyphenolic compounds, including chlorogenic acid and quercetin derivatives, which are known for their health benefits, particularly their antioxidant and antidiabetic properties. This study aimed to optimize the extraction conditions using the Box–Behnken model [...] Read more.
Black elderberry (Sambucus nigra L.) flowers are rich in polyphenolic compounds, including chlorogenic acid and quercetin derivatives, which are known for their health benefits, particularly their antioxidant and antidiabetic properties. This study aimed to optimize the extraction conditions using the Box–Behnken model to maximize polyphenol yields from different elderberry flower cultivars and to evaluate their potential for antidiabetic action. The extracts were analyzed for their phytochemical content and assessed for enzyme inhibition, specifically targeting enzymes critical in carbohydrate digestion and glucose regulation. The anti-inflammatory activity was also assessed. Results indicated that the Black Beauty, Obelisk, and Haschberg cultivars demonstrated significant inhibition of α-glucosidase, with a high inhibitory potential against α-amylase enzymes for the Obelisk cultivar. Additionally, high chlorogenic acid content was strongly correlated with enzyme inhibition and antioxidant activity, suggesting its substantial role in glucose regulation. This study underscores the potential of elderberry flower extracts, particularly those rich in chlorogenic acid, as natural agents for managing blood glucose levels, warranting further exploration of their use in antidiabetic applications. Full article
(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 5th Edition)
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17 pages, 1501 KiB  
Article
New Antioxidant Caffeate Esters of Fatty Alcohols Identified in Robinia pseudoacacia
by Ágnes M. Móricz, Márton Baglyas, András Darcsi, József Balla and Gertrud E. Morlock
Molecules 2024, 29(23), 5673; https://doi.org/10.3390/molecules29235673 - 30 Nov 2024
Cited by 2 | Viewed by 845
Abstract
The stem bark of black locust (Robinia pseudoacacia L.) was extracted, and nine antioxidant compounds (R1–R9) were detected by high-performance thin-layer chromatography combined with the radical scavenging 2,2-diphenyl-1-picrylhydrazyl (DPPH•) assay, multi-detection, and heated electrospray high-resolution mass spectrometry. For [...] Read more.
The stem bark of black locust (Robinia pseudoacacia L.) was extracted, and nine antioxidant compounds (R1–R9) were detected by high-performance thin-layer chromatography combined with the radical scavenging 2,2-diphenyl-1-picrylhydrazyl (DPPH•) assay, multi-detection, and heated electrospray high-resolution mass spectrometry. For structure elucidation, the methanolic crude extract was fractionated by solid-phase extraction, and the compounds were isolated by reversed-phase high-performance liquid chromatography with diode array detection. The structures of isolated compounds were elucidated by nuclear magnetic resonance and attenuated total reflectance Fourier-transform infrared spectroscopy as well as gas chromatography-mass spectrometry to determine the double bond position. 3-O-Caffeoyl oleanolic acid (R1), oleyl (R2), octadecyl (R3), gadoleyl (R4), eicosanyl (R5), (Z)-9-docosenyl (R6), docosyl (R7), tetracosyl (R8), and hexacosanyl (R9) caffeates were identified. While R1 has been reported in R. pseudoacacia stem bark, the known R3, R5, R7, R8, and R9 are described for the first time in this species, and the R2, R4, and R6 are new natural compounds. All nine caffeates demonstrated antioxidant activity. The antioxidant effects of the isolated compounds R1–R8 were quantified by a microplate DPPH• assay, with values ranging from 0.29 to 1.20 mol of caffeic acid equivalents per mole of isolate. Full article
(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 5th Edition)
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19 pages, 2143 KiB  
Article
Effect of Selenium Supplementation on Biotin and Selenobiotin Concentrations in Meyerozyma guilliermondii and Trichosporon cutaneum Cells
by Andrea Maria Patelski, Urszula Dziekońska-Kubczak, Agnieszka Nowak, Maciej Ditrych, Maria Balcerek, Katarzyna Pielech-Przybylska and Piotr Dziugan
Molecules 2024, 29(23), 5607; https://doi.org/10.3390/molecules29235607 - 27 Nov 2024
Viewed by 981
Abstract
Numerous studies have demonstrated the efficacy of selenium compounds in preventing and treating lifestyle-related diseases such as cancer and cardiovascular disorders. The formulation of selenium-enriched supplements for humans and animals, particularly those containing selenium yeast, is highly advantageous. These products are rich in [...] Read more.
Numerous studies have demonstrated the efficacy of selenium compounds in preventing and treating lifestyle-related diseases such as cancer and cardiovascular disorders. The formulation of selenium-enriched supplements for humans and animals, particularly those containing selenium yeast, is highly advantageous. These products are rich in organic selenium derivatives, showing significantly higher bioavailability than inorganic forms of selenium. A particularly promising selenium analogue of sulphur-containing compounds is selenobiotin. The literature indicates that Phycomyces blakesleeanus and Escherichia coli strains can synthesise this compound. This research aimed to evaluate the effect of selenium supplementation on the biosynthesis of biotin and selenobiotin in Trichosporon cutaneum and Meyerozyma guilliermondii. The results have the potential to advance biotechnological approaches for the production of selenobiotin for various applications. A method based on affinity chromatography was used to quantify selenobiotin. The results confirmed that both yeast strains could synthesise selenobiotin in addition to biotin. In M. guilliermondii cells, selenobiotin accounted for up to 17.3% of the total biotin vitamer fraction. In comparison, in T. cutaneum cells, it accounted for up to 28.4% of the sum of biotin and its analogues. The highest levels of selenobiotin were observed in cells cultured with selenomethionine. Full article
(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 5th Edition)
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18 pages, 6329 KiB  
Article
Enhancing Wound Healing with Nanohydrogel-Entrapped Plant Extracts and Nanosilver: An In Vitro Investigation
by Devadass Jessy Mercy, Anbazhagan Thirumalai, Saranya Udayakumar, Balasubramanian Deepika, Gopalarethinam Janani, Agnishwar Girigoswami and Koyeli Girigoswami
Molecules 2024, 29(21), 5004; https://doi.org/10.3390/molecules29215004 - 22 Oct 2024
Cited by 3 | Viewed by 2624
Abstract
Wound healing is a complex process that can be improved through advanced biomedical approaches. Incorporating nanopolymers and plant extracts into wound dressings offers a favorable strategy for promoting tissue repair. Nanopolymers provide a controlled environment for sustained drug release while also protecting the [...] Read more.
Wound healing is a complex process that can be improved through advanced biomedical approaches. Incorporating nanopolymers and plant extracts into wound dressings offers a favorable strategy for promoting tissue repair. Nanopolymers provide a controlled environment for sustained drug release while also protecting the wound from external contaminants. When combined with bioactive compounds from plant extracts, which possess antioxidant, anti-inflammatory, and antimicrobial properties, this hybrid approach can accelerate healing, reduce infection, and improve tissue regeneration. Hence, in this study, we have synthesized alginate/gelatin hydrogel blended with only nanosilver (Alg/gel-Ag) and with nanosilver and plant extracts like aloe vera, curcumin, plantain peel extract, and Calendula flower petal extract (Alg/gel-AgP). The synthesized hydrogels were characterized using different photophysical tools, and the cytotoxicity effect was studied using a fibroblast cell line (V79). The antibacterial effect of the hydrogels was also observed against E. coli and S. aureus, determining the MIC and MBC. The wound healing in vitro was also assessed using scratch assay which depicted a rapid wound closure for Alg/gel-AgP compared to the untreated control and Alg/gel-Ag. The combined effect between nanotechnology and natural extracts represents a novel and effective approach for enhancing the wound healing process. Full article
(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 5th Edition)
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11 pages, 1102 KiB  
Article
Isolation and Structure Determination of New Pyrones from Dictyostelium spp. Cellular Slime Molds Coincubated with Pseudomonas spp.
by Takehiro Nishimura, Takuya Murotani, Hitomi Sasaki, Yoshinori Uekusa, Hiromi Eguchi, Hirotaka Ishigaki, Katsunori Takahashi, Yuzuru Kubohara and Haruhisa Kikuchi
Molecules 2024, 29(9), 2143; https://doi.org/10.3390/molecules29092143 - 5 May 2024
Viewed by 1288
Abstract
Cellular slime molds are excellent model organisms in the field of cell and developmental biology because of their simple developmental patterns. During our studies on the identification of bioactive molecules from secondary metabolites of cellular slime molds toward the development of novel pharmaceuticals, [...] Read more.
Cellular slime molds are excellent model organisms in the field of cell and developmental biology because of their simple developmental patterns. During our studies on the identification of bioactive molecules from secondary metabolites of cellular slime molds toward the development of novel pharmaceuticals, we revealed the structural diversity of secondary metabolites. Cellular slime molds grow by feeding on bacteria, such as Klebsiella aerogenes and Escherichia coli, without using medium components. Although changing the feeding bacteria is expected to affect dramatically the secondary metabolite production, the effect of the feeding bacteria on the production of secondary metabolites is not known. Herein, we report the isolation and structure elucidation of clavapyrone (1) from Dictyostelium clavatum, intermedipyrone (2) from D. magnum, and magnumiol (3) from D. intermedium. These compounds are not obtained from usual cultural conditions with Klebsiella aerogenes but obtained from coincubated conditions with Pseudomonas spp. The results demonstrate the diversity of the secondary metabolites of cellular slime molds and suggest that widening the range of feeding bacteria for cellular slime molds would increase their application potential in drug discovery. Full article
(This article belongs to the Special Issue Discovery of Bioactive Ingredients from Natural Products, 5th Edition)
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