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Medicinal Value of Natural Bioactive Compounds and Plant Extracts, 3rd Edition

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

Deadline for manuscript submissions: closed (31 March 2026) | Viewed by 30411

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Prof. Dr. Magdalena Wójciak

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Department of Analytical Chemistry, Medical University of Lublin, Chodzki 4a, 20-093 Lublin, Poland
Interests: secondary plant metabolites; plant extracts; biological activity of natural compounds; polyphenols; chromatography
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Dr. Marcin Feldo

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Department of Vascular Surgery, Medical University of Lublin, Staszica 11 St., 20-081 Lublin, Poland
Interests: flavonoids; diosmin; biological activity of plant metabolites chronic venous insufficiency; cardiovascular diseases
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Prof. Dr. Ireneusz Sowa

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Department of Analytical Chemistry, Medical University of Lublin, Lublin, Poland
Interests: chemical structure; phytochemical analysis; chromatography; trace analysis
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Special Issue Information

Dear Colleagues,

The importance of plants and plant-derived compounds continues to increase due to their broad range of activity, including anti-inflammatory, antioxidant, immunostimulating, protective, antimicrobial, and antifungal properties, alongside health-promoting effects and protection against the development of cardiovascular and neurodegenerative disorders. However, their potential for pharmaceutical, medicinal, and cosmetological applications is still unexplored. As such, this Special Issue aims to present new achievement in these fields.

Studies on the isolation, structural elucidation, and biological activity of natural constituents from plants, fungi, and algae, as well as on the activity and utility of well-characterized plant extracts, are appreciated.

Prof. Dr. Magdalena Wójciak
Dr. Marcin Feldo
Prof. Dr. Ireneusz Sowa
Guest Editors

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Keywords

secondary plant metabolites
plant extracts
biological activity
polyphenols
alkaloids
in vitro, in vivo and study
cosmetology
ethnopharmacology
isolation and structure elucidation of plant metabolites

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Related Special Issues

Medicinal Value of Natural Bioactive Compounds and Plant Extracts in Molecules (16 articles)
Medicinal Value of Natural Bioactive Compounds and Plant Extracts II in Molecules (15 articles)
Medicinal Value of Natural Bioactive Compounds and Plant Extracts, 4th Edition in Molecules

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Research

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24 pages, 4186 KB

Open AccessArticle

Chemical Characteristics and Antimicrobial Activity of Arctostaphylos uva-ursi (L.) Spreng. Extracts Against Skin-Associated Bacteria

by Danuta Sugier, Aleksandra Nurzyńska, Małgorzata Miazga-Karska, Łukasz Sęczyk and Piotr Sugier

Molecules 2026, 31(8), 1267; https://doi.org/10.3390/molecules31081267 - 12 Apr 2026

Viewed by 587

Abstract

The interest in the use of phytochemicals and herbal medicines for the treatment of acne vulgaris has grown steadily over recent decades. The research on the secondary metabolites and biological properties of bearberry (Arctostaphylos uva-ursi (L.) Spreng.) has been intensified in recent years, but the range of bacterial strains tested, many of which are highly relevant to human health, remains very limited. Therefore, the aim of this study was to evaluate the chemical composition and the antioxidant, antimicrobial, and cytotoxic activities of water and ethanolic bearberry leaf extracts. Compared with the ethanolic extract, the water extract was characterized by higher concentrations of arbutin, hydroquinone, corilagin, and hyperoside and the absence of ursolic acid and oleanolic acid. However, it exhibited lower total phenolic content and reduced levels of penta-O-galloyl-β-d-glucose (PGG). The ethanolic extract of bearberry leaves showed higher antioxidant activity and the most favorable overall biological properties. The therapeutic index (TI) values for the water and ethanolic extracts, respectively, were as follows: Cutibacterium acnes ATCC 11827 (10.70; 21.57), Propionibacterium acnes PCM 2334 (10.70; 43.13), P. acnes PCM (5.33; 21.57), Staphylococcus aureus ATCC 25923 (10.70; 21.57), and S. epidermidis ATCC 12228 (5.33; 10.78). The present findings further support the medicinal and cosmetic use of A. uva-ursi and highlight its potential as a source of natural antibacterial agents for acne treatment. Full article

(This article belongs to the Special Issue Medicinal Value of Natural Bioactive Compounds and Plant Extracts, 3rd Edition)

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19 pages, 6411 KB

Open AccessArticle

Viniferin-Rich Phytocomplex from Vitis vinifera L. Plant Cell Culture Mitigates Neuroinflammation in BV2 Microglia Cells

by Giacomina Videtta, Chiara Sasia, Sofia Quadrino, Oriana Bertaiola, Chiara Guarnerio, Elisa Bianchi, Giacomo Biagiotti, Barbara Richichi, Stefano Cicchi, Giovanna Pressi and Nicoletta Galeotti

Molecules 2026, 31(1), 196; https://doi.org/10.3390/molecules31010196 - 5 Jan 2026

Cited by 1 | Viewed by 802

Abstract

Activation of microglia and resulting neuroinflammation are central processes that significantly contribute to neurodegenerative disease progression. Treatments capable of attenuating neuroinflammation are therefore an urgent medical need. Vitis vinifera L., cultivated since ancient times for its fruits, is known for its antioxidant and anti-inflammatory activities. However, polyphenols, the main bioactive molecules in V. vinifera extracts, exhibit considerable variability due to numerous hard-to-control factors, which complicates the production of standardized extracts with consistent biological activity. To address this issue, plant cell culture biotechnology was used to produce a highly standardized V. vinifera phytocomplex (VP), and its anti-neuroinflammatory profile was investigated in LPS-stimulated microglial cells, an in vitro model of neuroinflammation. VP reduced the LPS-induced pro-inflammatory phenotype, improved cell viability and cell number, attenuated NF-κB activation and ERK1/2 phosphorylation, and increased SIRT1 levels. To overcome VP’s poor water solubility, water-soluble cellulose nanocrystal (CNC)-based formulations were developed and tested. VP-CNC formulations markedly reduced the BV2 pro-inflammatory phenotype and increased cell viability under both basal and LPS-stimulated conditions. The nanoformulations also decreased pERK1/2 levels and increased SIRT1 expression, exhibiting biological activities comparable to VP alone. V. vinifera phytocomplex derived from plant cell cultures represents an innovative and standardized product with promising anti-neuroinflammatory properties. Full article

(This article belongs to the Special Issue Medicinal Value of Natural Bioactive Compounds and Plant Extracts, 3rd Edition)

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20 pages, 984 KB

Open AccessArticle

Unlocking the Functional Value of European-Originated Chrysanthemum Hybrids: Phytochemical and Bioactivity Assessment

by Natalia Miler, Maciej Balcerek, Jakub Gębalski, Anita Woźny, Magdalena Wójciak, Ireneusz Sowa and Daniel Załuski

Molecules 2026, 31(1), 172; https://doi.org/10.3390/molecules31010172 - 1 Jan 2026

Viewed by 1006

Abstract

Chrysanthemums are appreciated not only for their ornamental and medicinal attributes but also as edible plants long incorporated into teas, infusions, and culinary traditions. Yet, hybrid cultivars specifically adapted to European growing conditions remain poorly characterized with respect to their medicinal potential. In this study, we investigated the phytochemical composition, antioxidant properties, and enzyme-inhibitory activities of inflorescences of four field-grown Chrysanthemum × morifolium ‘Donna’ × C. rubellum ‘Clara Curtis’ hybrids of European origin (CD 7, DC 19, DC 26, CD 46). Their profiles were compared with those of a Chinese tea cultivar (C. morifolium CHR18) and a commercial herbal product (CH B). Chemical constituents were analyzed using GC–MS and LC–MS, while antioxidant activity was evaluated by FRAP, CUPRAC, DPPH, ABTS, and iron-chelating assays; hyaluronidase (HYAL) and butyrylcholinesterase (BChE) inhibition were also assessed. A total of 61 volatile compounds were identified, with several terpenoids—such as chrysanthenone and verbenone—occurring exclusively in the European hybrids. CHR 18 possessed the highest flavonoid and phenolic acid levels, whereas hybrid CD 46 exhibited the most pronounced overall antioxidant performance. Hyaluronidase inhibition was strongest in DC 26 and CD 46 (60–62%), surpassing both reference samples, while BChE inhibition remained generally low. Overall, the results highlight that C. morifolium × C. rubellum hybrids developed for cultivation in the temperate European climate offer a unique combination of phytochemical richness, robust antioxidant activity, and noteworthy enzyme inhibition. These traits underscore their promise as emerging functional chrysanthemum resources and support future applications in European herbal products, nutraceutical development, and region-specific functional food innovation. Full article

(This article belongs to the Special Issue Medicinal Value of Natural Bioactive Compounds and Plant Extracts, 3rd Edition)

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23 pages, 2361 KB

Open AccessFeature PaperArticle

Tyrosinase Inhibitors Among Flora of Lubelskie Region—Application of Bio-Chromatographic Approach and Zebrafish Model in Bioactivity Screening of Plant Material

by Kamila Kusio-Targońska, Nataliia Kosheva, Krzysztof Kamil Wojtanowski, Katarzyna Gaweł-Bęben, Dimitris Beis and Wirginia Kukula-Koch

Molecules 2025, 30(9), 1979; https://doi.org/10.3390/molecules30091979 - 29 Apr 2025

Cited by 3 | Viewed by 2242

Abstract

The whitening potential of natural products is commonly assessed through spectrophotometric assays that colorimetrically measure the inhibitory effects on tyrosinase, a key enzyme in pigment formation. However, these assays fail to provide evidence about the input of individual components into the total activity of a mixture like plant extracts. This study introduced chromatographic methods to identify active natural products without isolating them from their mixtures. In this study, various plant extracts of differing polarities (EtOH, 50% EtOH, and HOH) from species growing in the Lubelskie region of Poland were evaluated for their ability to inhibit tyrosinase. The most active extract identified through spectrophotometric assays was a 50% EtOH extract from Matricaria recutita L. (Chamomilla recutita (L.) Rauschert). Subsequent HPLC-MS analysis allowed for the identification of several active compounds from different classes, including organic acids, glycosylated phenolics, and phenolic acids that interacted with the enzyme. The bioactivity of individual components was confirmed through classical spectrophotometric assays, highlighting ferulic acid (IC₅₀ = 0.484 µM), quinic acid (IC₅₀ = 22.90 µM), and citric acid (IC₅₀ = 24.18 µM) as three representatives of different classes of molecules with inhibitory potential. Furthermore, the whitening capacity of the chamomile extract was investigated in a zebrafish model, demonstrating effective pigmentation inhibition in Danio rerio larvae and validating the proposed chromatographic approach. Full article

(This article belongs to the Special Issue Medicinal Value of Natural Bioactive Compounds and Plant Extracts, 3rd Edition)

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26 pages, 26334 KB

Open AccessArticle

Exploring the Structural Characteristics and Antioxidant Capacity of Pectins from Adenophora tetraphylla (Thunb.) Fisch.

by Su Yan, Shuo Zhang, Yuxuan Liu, Hao Zang, Lihui Zhang and Duo Liu

Molecules 2025, 30(6), 1301; https://doi.org/10.3390/molecules30061301 - 13 Mar 2025

Cited by 2 | Viewed by 1232

Abstract

This research explores the structural composition and antioxidant abilities of pectins extracted from Adenophora tetraphylla (Thunb.) Fisch. Pectins, which are a complex group of acidic polysaccharides, exhibit various biological activities due to their unique structural domains. Following aqueous extraction, the pectins underwent sequential purification using ion exchange and gel permeation chromatography techniques. FT-IR and NMR techniques were used to elucidate their structural characteristics. The structural investigation was enhanced through the application of multiple characterization methods: Congo red binding analysis, circular dichroism measurements, and scanning electron microscopy imaging. Among the isolated pectins, WATP-A2b (22.5 kDa) and WATP-A3b (49.8 kDa) demonstrated significant variations in their structural domain organization, comprising different ratios of homogalacturonan, rhamnogalacturonan I, and rhamnogalacturonan II. WATP-A3b displayed the most potent antioxidant performance among the tested pectins, effectively scavenging all three free radical species, which may be correlated with its higher galacturonic acid proportion and substantial rhamnogalacturonan I domain presence. These experimental results provide valuable insights into the correlation between structural characteristics and biological functions of pectins derived from Adenophora tetraphylla and their potential applications in healthcare. Full article

(This article belongs to the Special Issue Medicinal Value of Natural Bioactive Compounds and Plant Extracts, 3rd Edition)

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17 pages, 10367 KB

Open AccessArticle

Metabolite Profiling and Anti-Inflammatory Activities of Fritillaria cirrhosa D. Don Bulbs Derived from Tissue Culture

by Yu Wang, Jiamin Liu, Enhao Zhang, Yixi Yang, Qiuxia Lu, Ziwei Zhu and Rui Li

Molecules 2025, 30(3), 623; https://doi.org/10.3390/molecules30030623 - 31 Jan 2025

Cited by 3 | Viewed by 3086

Abstract

Fritillaria cirrhosa D. Don (known as Chuan-Bei-Mu in Chinese) is a prominent medicinal plant utilized in traditional medicine for chronic respiratory ailments. It has garnered global acknowledgment because of its incorporation in many herbal preparations, resulting in a significant increase in demand and, consequently, leading to the decimation of wild populations. The study aimed to obtain regenerated plantlets of F. cirrhosa using in vitro propagation techniques and evaluate the accumulation of active metabolites and anti-inflammatory properties from in vitro and natural plant bulbs. UHPLC-Q-TOF/MS analysis identified 267 metabolites. Notably, 118 metabolites showed significantly different intensities between the wild bulbs (WBs) and in vitro tissue culture-regenerated bulbs (RBs). Higher edpetiline amounts were obtained from the RBs, and 14 steroid-related metabolites were elevated in RBs. Both RB and WB extracts had comparable anti-inflammatory abilities and significantly inhibited TNF-α-induced epithelial cell TSLP release. Subsequent mechanistic studies revealed that the efficacy of WB and RB extracts depended on the regulation of the TRPV1/NFAT pathway. These findings highlight the viability of in vitro regeneration and medicinal part replacement as sustainable alternatives to the existing detrimental overharvesting of wild Chuan-Bei-Mu populations. Full article

(This article belongs to the Special Issue Medicinal Value of Natural Bioactive Compounds and Plant Extracts, 3rd Edition)

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Review

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74 pages, 5599 KB

Open AccessReview

An Updated and Comprehensive Review of Phellodendri amurensis Cortex: Ethnobotany, Geographical Distribution, Phytochemistry, Quality Control, and Pharmacology

by Kang Li, Chunqi Song, Xin Tan, Yang Zhang, Hao Zang and Xingzun Zhu

Molecules 2026, 31(8), 1318; https://doi.org/10.3390/molecules31081318 - 17 Apr 2026

Viewed by 234

Abstract

Phellodendri amurensis Cortex is the dried bark of the cork tree (Phellodendron amurense Rupr.) from the Rutaceae family, and possesses traditional efficacy in clearing heat, drying dampness, purging fire, relieving steaming sensations, detoxifying, and healing sores. Clinically, it is commonly used for treating symptoms such as damp-heat diarrhea and dysentery, jaundice with reddish urine, leukorrhea with vaginal itching, painful and difficult urination due to heat strangury, flaccidity and weakness of the lower limbs, bone-steaming and consumptive fever, night sweats and seminal emission, sores, ulcers, swellings, and toxins, eczema, damp sores, and urinary tract infections. Modern pharmacological studies have further revealed its diverse bioactivities, including antioxidant, antibacterial, anti-inflammatory, immunosuppressive, and anticancer effects. To provide an updated and comprehensive review of the research into Phellodendri amurensis Cortex, this study conducted a thorough literature search and analysis based on databases such as SciFinder, Web of Science, and China National Knowledge Infrastructure. The review integrates information on the plant’s botanical characteristics, geographical distribution, traditional applications, chemical components, quality control methods, and pharmacological effects to present a current and holistic overview of its research status. To date, approximately 170 compounds have been isolated and identified from Phellodendri amurensis Cortex, primarily including alkaloids, phenolics, terpenoids, sterols, lignans, flavonoids, and others. Among these, alkaloids exhibit significant antioxidant and anti-inflammatory activities and demonstrate potential pharmacological value in antibacterial, anticancer, hypoglycemic, and multi-organ protective effects. Although substantial foundational research exists, the mechanisms of action and quality control of Phellodendri amurensis Cortex require further in-depth exploration. Future efforts should focus on clarifying its pharmacodynamic material basis, uncovering new targets and pathways, and improving analytical methods for component analysis and quality control to advance the scientific development and rational utilization of this medicinal material. Full article

(This article belongs to the Special Issue Medicinal Value of Natural Bioactive Compounds and Plant Extracts, 3rd Edition)

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29 pages, 1093 KB

Open AccessReview

Polyphenols and Bone Health: A Comprehensive Review of Their Role in Osteoporosis Prevention and Treatment

by Pasquale Perrone, Chiara De Rosa and Stefania D’Angelo

Molecules 2025, 30(21), 4154; https://doi.org/10.3390/molecules30214154 - 22 Oct 2025

Cited by 6 | Viewed by 3824

Abstract

Osteoporosis is a progressive bone disorder characterized by decreased bone mineral density and structural deterioration, leading to increased fracture risk. Conventional treatments, although effective, are limited by adverse effects and low long-term adherence. In recent years, polyphenols, plant-derived bioactive compounds, have emerged as promising candidates for bone health promotion due to their antioxidant, anti-inflammatory, and osteo-regulatory properties. This review synthesizes the current preclinical and clinical evidence on the potential of polyphenols, including quercetin, resveratrol, curcumin, isoflavones, and epigallocatechin gallate, to modulate bone metabolism and prevent or mitigate osteoporosis. Mechanistically, polyphenols enhance osteoblastogenesis, inhibit osteoclast differentiation, regulate the RANKL/OPG axis, and activate key osteogenic pathways such as Wnt/β-catenin and MAPKs. Additionally, their estrogen-like activity and ability to modulate gut microbiota offer further therapeutic potential. Preclinical models consistently demonstrate improvements in bone mass, architecture, and turnover markers, while clinical trials, although limited, support their role in preserving bone density, particularly in postmenopausal women. Despite promising outcomes, variability in bioavailability, dosage, and study design limits current translational application. Further large-scale clinical studies and standardized formulations are needed. Polyphenols represent a compelling adjunct or alternative approach in the integrated management of osteoporosis. Full article

(This article belongs to the Special Issue Medicinal Value of Natural Bioactive Compounds and Plant Extracts, 3rd Edition)

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24 pages, 1055 KB

Open AccessReview

Potential of Quercetin as a Promising Therapeutic Agent Against Type 2 Diabetes

by Przemysław Niziński, Anna Hawrył, Paweł Polak, Adrianna Kondracka, Tomasz Oniszczuk, Jakub Soja, Mirosław Hawrył and Anna Oniszczuk

Molecules 2025, 30(15), 3096; https://doi.org/10.3390/molecules30153096 - 24 Jul 2025

Cited by 9 | Viewed by 5928

Abstract

Quercetin (QE) is a naturally occurring flavonoid found in many fruits, vegetables, and other plant-based foods. It is recognized for its diverse pharmacological activities. Among its many therapeutic potentials, its antidiabetic properties are of particular interest due to the growing worldwide prevalence of diabetes mellitus. QE improves glycemic control by enhancing insulin sensitivity, stimulating glucose uptake, and preserving pancreatic beta cell function. These effects are mediated by the modulation of key molecular pathways, including AMPK, PI3K/Akt, and Nrf2/ARE, as well as by the suppression of oxidative stress and pro-inflammatory cytokines, such as TNF-α and IL-6. Furthermore, QE mitigates the progression of diabetic complications such as nephropathy, retinopathy, and vascular dysfunction, reducing lipid peroxidation and protecting endothelial function. However, the clinical application of quercetin is limited by its low water solubility, poor bioavailability, and extensive phase II metabolism. Advances in formulation strategies, including the use of nanocarriers, co-crystals, and phospholipid complexes, have shown promise in improving its pharmacokinetics. This review elucidates the mechanistic basis of QE quercetin antidiabetic action and discusses strategies to enhance its therapeutic potential in clinical settings. Full article

(This article belongs to the Special Issue Medicinal Value of Natural Bioactive Compounds and Plant Extracts, 3rd Edition)

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23 pages, 1607 KB

Open AccessReview

Hamamelis virginiana L. in Skin Care: A Review of Its Pharmacological Properties and Cosmetological Applications

by Magdalena Wójciak, Wiktoria Pacuła, Ireneusz Sowa, Marcin Feldo, Filip Graczyk and Daniel Załuski

Molecules 2025, 30(13), 2744; https://doi.org/10.3390/molecules30132744 - 26 Jun 2025

Cited by 2 | Viewed by 10078

Abstract

Hamamelis virginiana L. (witch hazel) is a traditionally used medicinal plant, well-known for its dermatological applications. The plant’s bark and leaves contain a rich array of bioactive compounds, including phenolic acids, flavonoids, catechins, proanthocyanidins, and tannins, many of which exhibit antimicrobial, anti-inflammatory, antioxidant, and wound-healing properties. These activities have been verified by numerous in vitro and in vivo studies, as well as limited clinical trials. The H. virginiana extracts have demonstrated effectiveness against bacteria, fungi, and some viruses. Moreover, the extracts exert anti-inflammatory effects by modulating cytokine expression and NF-κB signaling, improve skin regeneration, and protect against UV-induced damage and pollution. This review highlights H. virginiana as a complex botanical resource to be used in dermatology and cosmetology and shows that current research offers encouraging results for its future therapeutic use, especially in skin treatment. Full article

(This article belongs to the Special Issue Medicinal Value of Natural Bioactive Compounds and Plant Extracts, 3rd Edition)

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