Natural Products and Phytotherapy: Advances in Phytochemistry and Pharmacology

A special issue of Plants (ISSN 2223-7747). This special issue belongs to the section "Phytochemistry".

Deadline for manuscript submissions: 31 July 2024 | Viewed by 7245

Special Issue Editors


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Guest Editor
Department of Pharmacognosy, Faculty of Pharmacy, Medical University of Sofia, 100 Sofia, Bulgaria
Interests: natural product chemistry; medicinal plants and herbal drugs; chemical composition and biological activity of plant extracts and products
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Guest Editor
Department of Pharmacology, Pharmacotherapy and Toxicology, Faculty of Pharmacy, Medical University of Sofia, 100 Sofia, Bulgaria
Interests: experimental anticancer chemotherapy; anticancer drug design; antineoplastic metallodrugs; antimicrobials; ethnopharmacology; phytopharmacology; targeted drug delivery systems; drug discovery; medicinal chemistry; pharmacokinetics; natural product chemistry
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The term “phytotherapy” combines two Greek words, “phyton” (plant) and “therapy” (treatment), and it is used to describe a system of alternative methods of treatment based on the healing properties of medicinal plants. Since ancient times, medicinal plants have been explored as therapeutic agents, and a vast number of the medicinal ingredients accessible today have originated from natural resources. Plant-derived natural products have played a crucial role in the drug discovery process due to their well-known propensity to act on diverse molecular targets and modulate miscellaneous processes such as inflammation, oxidative stress, cellular proliferation, apoptosis, and angiogenesis on one hand, and due to the complex chemical scaffold characteristic for plant secondary metabolites, which it is not possible to generate in the lab. Undoubtedly, treating multifactorial diseases, such as cancer, chronic inflammatory conditions, metabolic diseases, etc., using pharmacological modalities targeting a single molecular entity is inevitably associated with limited success and unsatisfactory outcomes. On these grounds, natural products, in view of their multifaceted pharmacology and complex chemical composition, appear to still represent a vast and to a great extent unexplored source of potential pharmacological modalities. Much remains to be discovered, and as the phytochemical and pharmacological tools become more sophisticated and sensitive, our chances of more in-depth characterization of classical medicinal herbal drugs as well as these plants with pharmacological potential increase enormously. This Special Issue of Plants will focus on phytochemical and pharmacological studies on plants with current and potential employment in phytotherapy and traditional systems of medicine.

Dr. Paraskev T. Nedialkov
Prof. Dr. Georgi Momekov
Guest Editors

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Keywords

  • evidence-based phytotherapy
  • natural product pharmacology
  • ethnopharmacology
  • bioactivity-guided isolation
  • structure elucidation of new plant metabolites

Published Papers (6 papers)

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Research

15 pages, 3561 KiB  
Article
Regional Variations in Peucedanum japonicum Antioxidants and Phytochemicals
by Neil Patrick Uy, Hoon Kim, Jajung Ku and Sanghyun Lee
Plants 2024, 13(3), 377; https://doi.org/10.3390/plants13030377 - 27 Jan 2024
Cited by 1 | Viewed by 652
Abstract
Peucedanum japonicum has long been a staple in East Asian cuisine. In the context of traditional medicine, various members of the Peucedanum genus have been investigated for potential medicinal properties. In laboratory settings, some compounds derived from this plant have shown antioxidant and [...] Read more.
Peucedanum japonicum has long been a staple in East Asian cuisine. In the context of traditional medicine, various members of the Peucedanum genus have been investigated for potential medicinal properties. In laboratory settings, some compounds derived from this plant have shown antioxidant and anti-inflammatory properties—characteristics often associated with potential medicinal applications. This study aimed to determine which part of the P. japonicum plants cultivated on two Korean islands contains the most antioxidant compounds. This determination was made through assessments of total polyphenol content and total flavonoid content, coupled with evaluation of antioxidant activity via DPPH and ABTS assays. The results showed that the aerial parts contain a richer array of bioactive compounds and demonstrate superior antioxidant activity compared to their root counterparts in the plants from both islands. To characterize the phytochemicals underpinning this bioactivity, LC-MS/MS and HPLC analyses were carried out. These methods detected varying amounts of chlorogenic acid, peucedanol 7-O-glucoside, rutin, and peucedanol, with good separation and retention times. This study addresses the lack of research on the antioxidant activity of different parts of P. japonicum. The findings hold significance for traditional medicine, dietary supplements, and the development of functional foods. Understanding antioxidant distribution aids in the development of medicinal and nutritional applications, influences agricultural practices, and contributes to regional biodiversity-conservation efforts. The study’s geographical scope provides insights into how location impacts the concentration of bioactive compounds in plants. Overall, the results contribute valuable data for future research in plant biology, biochemistry, and related fields. Full article
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16 pages, 2019 KiB  
Article
Effect of Plant Extracts Combinations on TNF-α, IL-6 and IL-10 Levels in Serum of Rats Exposed to Acute and Chronic Stress
by Ilin Kandilarov, Petya Gardjeva, Maria Georgieva-Kotetarova, Hristina Zlatanova, Natalia Vilmosh, Ivanka Kostadinova, Mariana Katsarova, Kiril Atliev and Stela Dimitrova
Plants 2023, 12(17), 3049; https://doi.org/10.3390/plants12173049 - 24 Aug 2023
Cited by 1 | Viewed by 1540
Abstract
Oxydative stress, anxiety and depression are associated with changes in cytokine levels. Natural products, including individual and combined plant extracts, have the potential to be used in the treatment of neuropsychiatric disorders. The goal of this study is to investigate the effects of [...] Read more.
Oxydative stress, anxiety and depression are associated with changes in cytokine levels. Natural products, including individual and combined plant extracts, have the potential to be used in the treatment of neuropsychiatric disorders. The goal of this study is to investigate the effects of two combined plant extracts, rich in flavonoids, on the levels of the cytokines TNF-α, IL-6, and IL-10 in rats subjected to models of acute cold stress and chronic unpredictable stress. The study utilized common medicinal plants such as Valeriana officinalis, Melissa officinalis, Crataegus monogyna, Hypericum perforatum, and Serratula coronata, which were combined in two unique combinations—Antistress I and Antistress II. The compositions of the used extracts were determined by HPLC methods. Pro- and anti-inflammatory cytokines in rats’ serum were measured with Enzyme-linked immunosorbent assay. The results from the acute stress model revealed that the individual extract of Crataegus monogyna decreased levels of TNF-α, while Serratula coronata, Hypericum perforatum, and Valeriana officinalis effectively reduced IL-6 levels. Both combinations, Antistress I and Antistress II, were effective in reducing TNF-α and IL-6 levels, with Antistress II also increasing IL-10 levels. In the chronic stress model, Hypericum perforatum extract decreased the levels of the pro-inflammatory cytokines TNF-α and IL-6, whereas extracts of Serratula coronata and Valeriana officinalis only reduced TNF-α levels. The two combined extracts, Antistress I and Antistress II, decreased TNF-α and IL-6 levels, while Antistress I also reduced the levels of the anti-inflammatory cytokine IL-10. The combinations of plant extracts used in our experiment have not been previously studied or documented in the available literature. However, based on our own experimental results, we can draw the conclusion that the combinations exhibit a more pronounced effect in reducing cytokine levels compared to the individual plant extracts. Full article
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12 pages, 1039 KiB  
Article
Chemical Constituents from Ficus sagittifolia Stem Bark and Their Antimicrobial Activities
by Olayombo M. Taiwo, Olaoluwa O. Olaoluwa, Olapeju O. Aiyelaagbe and Thomas J. Schmidt
Plants 2023, 12(15), 2801; https://doi.org/10.3390/plants12152801 - 28 Jul 2023
Cited by 2 | Viewed by 1092
Abstract
The phytochemical investigation of the ethylacetate fraction of an ethanolic extract obtained from the stem bark of Ficus sagittifolia (Moraceae) led to the isolation of four flavonoids: (2R)-eriodictyol (1), 2′- hydroxygenistein (2), erycibenin A (3), [...] Read more.
The phytochemical investigation of the ethylacetate fraction of an ethanolic extract obtained from the stem bark of Ficus sagittifolia (Moraceae) led to the isolation of four flavonoids: (2R)-eriodictyol (1), 2′- hydroxygenistein (2), erycibenin A (3), and genistein (4); a dihydrobenzofuran: moracin P (5); a coumarin: peucedanol (6); and an apocarotenoid terpenoid: dihydrophaseic acid (7). These were identified via 1D and 2D nuclear magnetic resonance spectroscopy (NMR) and ultra-high-resolution liquid chromatography–quadrupole time-of-flight mass spectroscopy (UHPLC-QTOF MS). Moracin P (5) is being reported for the first time in the genus Ficus, while the others are known compounds (1–4 and 6–7) isolated previously from the genus but being reported for the first time from the species F. sagittifolia. Their antimicrobial activity against various pathogens (five bacteria: Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, Staphylococcus aureus, and Salmonella typhi; two fungi: Aspergillus niger and Candida albicans) was tested. The mixture of genistein and moracin P (4+5) exhibited strong activity against K. pneumoniae (MIC < 0.0039 mg/mL), whereas dihydrophaseic acid (7) was the most active against P. aeruginosa and A. niger (MIC = 0.0078 and <0.0039 mg/mL, respectively). These compounds might be considered potential antimicrobial agents with the potential to be starting points for the development of antimicrobial drugs. Full article
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11 pages, 1569 KiB  
Article
Exploring Phytochemical Composition and In Vivo Anti-Inflammatory Potential of Grape Seed Oil from an Alternative Source after Traditional Fermentation Processes: Implications for Phytotherapy
by Yancho Zarev, Lyubomir Marinov, Denitsa Momekova and Iliana Ionkova
Plants 2023, 12(15), 2795; https://doi.org/10.3390/plants12152795 - 28 Jul 2023
Cited by 1 | Viewed by 955
Abstract
This study aimed to analyze the composition of grape seed oil (GSO) derived from an alternative source after traditional fermentation processes and its potential anti-inflammatory effects using an in vivo model of carrageenan-induced inflammation in mice. Gas chromatography high-resolution electron ionization mass spectrometry [...] Read more.
This study aimed to analyze the composition of grape seed oil (GSO) derived from an alternative source after traditional fermentation processes and its potential anti-inflammatory effects using an in vivo model of carrageenan-induced inflammation in mice. Gas chromatography high-resolution electron ionization mass spectrometry (GC-HR-EIMS) analysis identified eight main components in the GSO extract, including myristic acid methyl ester, palmitoleic acid methyl ester, methyl isoheptadecanoate, cis-linoleic acid, oleic acid methyl ester, linoleic acid stereoisomer, linoleic acid ethyl ester, and methyl (6E, 9E, 12E, 15E)-docose-6,9,12,15-tetraenoate. No significant differences were observed in the main fatty acids between commercially available grape seed oil and GSO extract obtained from fermented grape seeds. In the carrageenan-induced inflammation model, treatment with GSO resulted in a significant reduction in paw edema at 180 min, as in the reduction observed with diclofenac treatment. Combined treatment with GSO and diclofenac showed enhanced anti-inflammatory effects. Additionally, GSO exhibited antioxidative effects by decreasing the levels of glutathione (GSH) and malondialdehyde (MDA) in the serum. Chronic treatment with GSO for ten days did not provide a protective effect on inflammation. These findings suggest that GSO could be used as an alternative raw material and could possess anti-inflammatory and antioxidative properties. Further studies are needed to explore its potential therapeutic applications. Full article
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27 pages, 2068 KiB  
Article
Phytochemical Profiling, Antioxidant and Cognitive-Enhancing Effect of Helichrysum italicum ssp. italicum (Roth) G. Don (Asteraceae)
by Reneta Gevrenova, Ivanka Kostadinova, Alexandra Stefanova, Vessela Balabanova, Gokhan Zengin, Dimitrina Zheleva-Dimitrova and Georgi Momekov
Plants 2023, 12(15), 2755; https://doi.org/10.3390/plants12152755 - 25 Jul 2023
Cited by 2 | Viewed by 981
Abstract
This study aimed at the evaluation of the antioxidant and cognitive-enhancing effect of methanol–aqueous extract from Helichrysum italicum ssp. italicum aerial parts. Significant radical scavenging activity (110.33 ± 3.47 and 234.70 ± 5.21 mg TE/g for DPPH and ABTS) and reducing power (354.23 [...] Read more.
This study aimed at the evaluation of the antioxidant and cognitive-enhancing effect of methanol–aqueous extract from Helichrysum italicum ssp. italicum aerial parts. Significant radical scavenging activity (110.33 ± 3.47 and 234.70 ± 5.21 mg TE/g for DPPH and ABTS) and reducing power (354.23 ± 17.51 and 210.24 ± 8.68 mg TE/g for CUPRAC and FRAP) were observed. The extract showed average acetylcholinesterase and low butyrylcholinesterase inhibitory potential. H. italicum extract (200 mg/kg/po) administered in combination with galantamine (3 mg/kg/po) for 12 days significantly improved the memory and learning process compared with galantamine alone in the passive avoidance test. The effect was comparable to that of Ginkgo biloba extract (100 mg/kg/po). In deep secondary metabolite annotation of the extract by UHPLC-HRMS, more than 90 hydroxybenzoic and hydroxicinnamic acid-glycosides, phenylethanoid glycosides, a series of acylquinic and caffeoylhexaric acids, methoxylated derivatives of scutellarein, quercetagetin and 6-hydroxyluteolin, and prenylated phloroglucinol-α-pyrones were reported for the first time in H. italicum. Fragmentation patterns of four subclasses of heterodimer-pyrones were proposed. In-depth profiling of the pyrones revealed 23 compounds undescribed in the literature. Pyrones and acylphloroglucinols together with acylquinic acids could account for memory improvement. The presented research advanced our knowledge of H. italicum, highlighting the species as a rich source of secondary metabolites with cognitive-enhancing potential. Full article
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11 pages, 7118 KiB  
Article
Molecular Docking of Cryptoconcatones to α-Tubulin and Related Pironetin Analogues
by Gérard Vergoten and Christian Bailly
Plants 2023, 12(2), 296; https://doi.org/10.3390/plants12020296 - 08 Jan 2023
Cited by 5 | Viewed by 1397
Abstract
Cryptoconcatones A-L represent a series of 12 dihydropyrone derivatives isolated from the evergreen tree Cryptocarya concinna Hance, which is well distributed in southeast Asia. The lead compound in the series, cryptoconcatone L, has revealed antiproliferative activity against cultured cancer cells but its mechanism [...] Read more.
Cryptoconcatones A-L represent a series of 12 dihydropyrone derivatives isolated from the evergreen tree Cryptocarya concinna Hance, which is well distributed in southeast Asia. The lead compound in the series, cryptoconcatone L, has revealed antiproliferative activity against cultured cancer cells but its mechanism of action remains unknown. Based on a structural analogy with the anticancer natural product pironetin, which is well known for binding covalently to α-tubulin and for functioning as a microtubule polymerization inhibitor, we investigated the interaction of cryptoconcatones with tubulin dimers using molecular docking. The α-tubulin binding capacity of each compound was quantified (through calculation of the empirical energy of interaction ΔE) and structure–binding relationships were delineated. Two compounds were found to interact with α-tubulin much more potently than pironetin: cryptoconcatones F and L. In both cases, the facile formation of a covalent bond with Cys316 was evidenced, as observed with the parent compound pironetin. A few other pironetin analogues were investigated, including spicigerolide, which is an analogue of another known α-tubulin binder. Altogether, this study points to the identification of a series of 5,6-dihydro-α-pyrones as α-tubulin-binding agents. The study contributes to a better understanding of the mechanism of action of cryptoconcatones and should help the design of analogues targeting the pironetin site of α-tubulin. Full article
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