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Pharmacological Activity of Natural Bioactive Compounds for Better Human Health

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

Deadline for manuscript submissions: 31 October 2026 | Viewed by 1204

Editors


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Guest Editor
Department of Biology, Faculty of Pharmacy, Medical University of Varna, 9000 Varna, Bulgaria
Interests: pharmacognosy; phytochemistry; phytotherapy

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Guest Editor
Department of Pharmacology, Toxicology and Pharmacotherapy, Faculty of Pharmacy, Medical University of Varna, 9000 Varna, Bulgaria
Interests: pharmacology; pharmacokinetics; drug–drug interactions
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Nature has been a major source of medicinal compounds for centuries, offering us a wide selection of bioactive substances with significant pharmacological potential. This is reflected in traditional medical systems across various cultures around the world, which primarily use medicines derived from natural sources, many of which have subsequently been confirmed by scientific research. The diverse chemical composition of natural sources—plants, animals, microorganisms, fungi, and many others—contributes to the wide spectrum of therapeutic effects they possess. Driven by the idea of ​​improving all aspects of human health, modern medicine, faced with challenges such as chronic diseases and adverse drug reactions, antibiotic resistance, and many others, is particularly interested in the search for new and better plant-based medicinal products.

It is precisely such natural compounds, their identification, isolation, purification, and even modification, both of pure components and of mixtures and even fractions of groups of substances, that this issue of the journal is aimed at. The special issue of Molecules also welcomes submissions on the analysis of cellular and molecular mechanisms of natural compounds or characterized extracts, as well as their absorption, distribution, metabolism, excretion, pharmacokinetics, pharmacodynamics, and therapeutic mechanisms.

Dr. Ilia Slavov
Prof. Dr. Kaloyan Georgiev
Guest Editors

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Keywords

  • natural products
  • pharmacologically active substances
  • chemical analysis
  • therapeutic effects
  • molecular mechanisms

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Published Papers (3 papers)

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Research

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18 pages, 1758 KB  
Article
Corosolic Acid Induces Endothelium-Dependent Vasorelaxation in Isolated Rat Aortic Rings
by Fangying Chen, Wan Yin Tew, Ming Thong Ong and Mun Fei Yam
Molecules 2026, 31(16), 2822; https://doi.org/10.3390/molecules31162822 - 13 Aug 2026
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Abstract
The effect of Corosolic acid (CA) on vascular tone and the possible mecha-nisms involved remain unclear. The SPF-grade male Sprague-Dawley rats (Animal Ethics Approval ID: USM/IACUC/2025/(155)(1406)) were used. The vasorelaxant effects of CA were evaluated in endothelium-intact and endothelium-denuded rings precontracted with phenylephrine [...] Read more.
The effect of Corosolic acid (CA) on vascular tone and the possible mecha-nisms involved remain unclear. The SPF-grade male Sprague-Dawley rats (Animal Ethics Approval ID: USM/IACUC/2025/(155)(1406)) were used. The vasorelaxant effects of CA were evaluated in endothelium-intact and endothelium-denuded rings precontracted with phenylephrine (PE), and in endothelium-intact rings precontracted with KCl. Possible mechanisms were examined using L-NAME, ODQ, methylene blue, indomethacin, atropine, propranolol, and potassium channel blockers (glibenclamide, TEA, BaCl2, and 4-AP). The effects of CA on voltage-operated calcium channels (VOCCs) and IP3 receptor (IP3R)-mediated sarcoplasmic reticulum calcium release were also assessed. CA concentration-dependently relaxed endothelium-intact aortic rings precontracted with PE (RMAX = 90.08 ± 7.33%; pD2 = 4.21 ± 0.08). The relaxation response was markedly reduced after endothelial removal and in KCl-precontracted rings. EDRF pathway inhibitors (L-NAME, ODQ, methylene blue, and indomethacin) and GPCR-related antagonists (atropine and propranolol) attenuated CA-induced relaxation. Among potassium channel blockers, glibenclamide and TEA showed stronger inhibitory effects. CA did not significantly inhibit VOCC-mediated CaCl2-induced contraction but partially reduced PE-induced contraction under calcium-free conditions. The mechanisms for CA treating hypertension may involve NO/cGMP signalling, COX-related prostanoid pathways, GPCR-related mechanisms, potassium channel modulation, and partial inhibition of IP3R-mediated calcium release. Full article
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19 pages, 1605 KB  
Article
Biologically Active Compounds and Antioxidant and DNA-Protective Potential of Rhodope Avens (Geum rhodopaeum Stoj.&Stef.) Dry Tinctures
by Ivanka Dimitrova-Dyulgerova, Silviya Mladenova, Elena Apostolova, Vasil Georgiev, Samir Naimov, Tsvetelina Mladenova, Ivayla Dincheva, Atanas Pavlov, Iliya Slavov and Rumen Mladenov
Molecules 2026, 31(10), 1643; https://doi.org/10.3390/molecules31101643 - 13 May 2026
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Abstract
This article is the first report highlighting Rhodope avens as a natural source of bioactive compounds with potential pharmaceutical applications. Dry tinctures obtained from herba (HDT) and rhizoma (RDT) from the Balkan Peninsula endemic plant Geum rhodopaeum were analyzed and tested for antioxidant [...] Read more.
This article is the first report highlighting Rhodope avens as a natural source of bioactive compounds with potential pharmaceutical applications. Dry tinctures obtained from herba (HDT) and rhizoma (RDT) from the Balkan Peninsula endemic plant Geum rhodopaeum were analyzed and tested for antioxidant activity (DPPH, ABTS, FRAP, CUPRAC assays) and DNA nicking protection potential. The tinctures were characterized by a high total polyphenol content (total the polyphenols in RDT were more than twice that of HDT, i.e., 516.6 mg GAE/g dt; p < 0.01). HPLC analysis revealed the presence of 14 phenolics, with the main one being (over 3 mg/g dt) (+)-catechin (28.21 mg/g dt for RDT; 9.67 mg/g dt HDT), followed by protocatechuic acid, salicylic acid, and rutin. Rosmarinic acid content is herein first reported for the genus Geum. GC/MS analysis identified 41 compounds, among which monosaccharides predominated (with the highest fructose content), followed by gluconic acid, glucose-1-phosphate, mannitol, sorbitol, and glycerol in HDT, along with xylitol in RDT. The tinctures exhibited strong antioxidant potential as evaluated by the methods used, with the most pronounced effect found in the CUPRAC assay (5 458.87 μM TE/g dt for HDT; 10 073.99 μM TE/g dt for RDT; p < 0.01), as confirmed in comparison to proven antioxidants such as BHT and vitamin C. DNA-protective activity against oxidative damage was established and microscopic identification of the herbal substances was also performed. Full article
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Review

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16 pages, 578 KB  
Review
Mechanistic Insights into the Antihypertensive and Cardioprotective Actions of Corosolic Acid: A Narrative Review
by Fangying Chen, Wan Yin Tew, Ming Thong Ong and Mun Fei Yam
Molecules 2026, 31(16), 2841; https://doi.org/10.3390/molecules31162841 - 14 Aug 2026
Viewed by 223
Abstract
Background: The specific mechanisms underlying the antihypertensive actions of corosolic acid (CA) have not been systematically elucidated. Methods: Evidence was categorized according to major signaling and physiological pathways, including the renin–angiotensin system (RAS), oxidative and inflammatory responses, endothelial and smooth muscle regulation (NO/cGMP [...] Read more.
Background: The specific mechanisms underlying the antihypertensive actions of corosolic acid (CA) have not been systematically elucidated. Methods: Evidence was categorized according to major signaling and physiological pathways, including the renin–angiotensin system (RAS), oxidative and inflammatory responses, endothelial and smooth muscle regulation (NO/cGMP and H2S/KATP), and kinase-mediated signaling (AMPK, NF-κB, JAK/STAT, PKC). Results: Consistent with in vitro and animal studies, CA has been reported to attenuate pro-hypertensive signaling through multiple pathways: (i) downregulating renin–angiotensin system-related cascades; (ii) reduction in reactive oxygen species and inflammatory mediators through activation of AMPK and inhibition of NF-κB and JAK/STAT pathways; (iii) improved vascular tone by enhancing NO/cGMP signaling, partly involving the H2S/KATP pathway, and inhibiting PKC. CA may indirectly contribute to blood pressure reduction by improving glucose and lipid metabolism and adipose tissue inflammation, thereby affecting metabolic risk factors. The existing evidence gaps include: lack of direct studies on voltage-gated, receptor-gated and store-regulated calcium channels; the specific effects on the isoforms of nitric oxide synthase (eNOS/iNOS/nNOS) and PKC are not known; limited human data on the antihypertensive efficacy, dose effect and safety of CA in humans are available. Conclusions: CA may have multi-targeted blood-pressure-lowering potential. Its clinical efficacy and safety require further confirmation. Full article
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