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Plant-Based Extracts and the Therapeutic Potential of Bioactive Compounds, 2nd...
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Plant-Based Extracts and the Therapeutic Potential of Bioactive Compounds, 2nd Edition

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Natural Products".

Deadline for manuscript submissions: 31 August 2026 | Viewed by 12567

Special Issue Editor

Dr. Grażyna Zgórka

E-Mail Website1 Website2
Guest Editor
Department of Pharmacognosy with the Medicinal Plant Garden, Faculty of Pharmacy, Medical University of Lublin, 20-093 Lublin, Poland
Interests: plant polyphenols; chemoprevention; advanced phytochemical analysis; herbal medicinal products
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The safety, efficacy, and quality of modern herbal medicinal products are determined by the valuable plant extracts used in their production. The quality of herbal substances must be consistent, and the multi-stage process (which involves achieving the maximum compliance of the chemical composition with that found in the plant material during the herbal preparation stage) must be standardized. Specific high-quality physicochemical tests are carried out on the final herbal extract, including the control of biologically active components or active chemical markers and the validation of developed analytical methods. This leads to valuable extracts that can be assessed in preclinical and clinical studies due to their therapeutic properties.This Special Issue showcases submissions that present a variety of preparative methods used to obtain liquid and solid herbal extracts and their phytochemical standardization procedures using validated analytical methods.

We welcome article submissions that present coupled chromatographic, spectroscopic, and spectrometric analytical techniques. Detailed phytochemical profiling should be combined with an evaluation of the biological properties (in vitro and in vivo studies or preliminary clinical evaluation) of herbal preparations and isolated bioactive phytoconstituents, especially regarding their ability to inhibit degenerative processes in the human body.

Dr. Grażyna Zgórka
Guest Editor

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 250 words) can be sent to the Editorial Office for assessment.

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. Pharmaceuticals is an international peer-reviewed open access monthly 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 2900 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

  • plant extracts
  • herbal medicinal products
  • standardization
  • phytochemical profiling
  • bioactive plant compounds
  • therapeutic effects

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Related Special Issue

Published Papers (8 papers)

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Research

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19 pages, 1473 KB  
Article
Phytochemical Composition and Bioactivity of Acanthus dioscoridis var. perringii: An Integrated Analysis of Antioxidant Activity, Enzyme Inhibition, and Phenolic–Bioactivity Correlations
by Bedrettin Selvi
Pharmaceuticals 2026, 19(3), 512; https://doi.org/10.3390/ph19030512 - 20 Mar 2026
Viewed by 342
Abstract
Objectives: Plant organs often allocate phenolic metabolites unevenly, resulting in organ-specific bioactivities. This study aimed to characterize the organ-specific phenolic profile of Acanthus dioscoridis var. perringii and determine how this chemical segregation is associated with antioxidant capacity and enzyme inhibitory activities. Materials and [...] Read more.
Objectives: Plant organs often allocate phenolic metabolites unevenly, resulting in organ-specific bioactivities. This study aimed to characterize the organ-specific phenolic profile of Acanthus dioscoridis var. perringii and determine how this chemical segregation is associated with antioxidant capacity and enzyme inhibitory activities. Materials and Methods: Organ-specific extracts (roots, stems, leaves, bracts, and flowers) were evaluated for total phenolic and flavonoid contents, targeted LC-MS analysis of individual phenolics, antioxidant activity by multiple assays, enzyme inhibition [acetylcholinesterase (AChE), butyrylcholinesterase (BChE), α-amylase, and α-glucosidase], and the relationships between phenolic composition and biological activities. Antioxidant performance was also assessed using the Relative Antioxidant Capacity Index (RACI). Results and Discussion: Roots showed the highest total phenolic content, whereas bracts had the highest total flavonoid level. Verbascoside was the dominant compound in all organs, with the highest levels in leaves, roots, and bracts. Roots exhibited the strongest reducing and radical-scavenging activities, while flowers showed the best metal-chelating capacity. Enzyme inhibition was organ-dependent and generally moderate, with stems showing the strongest cholinesterase inhibition, leaves the strongest α-amylase inhibition, and bracts together with roots the strongest α-glucosidase inhibition. Statistical analysis revealed close associations between phenolic richness, antioxidant responses, and cholinesterase inhibition. Conclusions: These findings demonstrate a clear organ-dependent distribution of phenolic compounds in A. dioscoridis var. perringii, reflected in distinct antioxidant and enzyme inhibitory profiles. Overall, the study provides a biochemical and bioactivity-based characterization of the species at the organ level. Full article
(This article belongs to the Special Issue Plant-Based Extracts and the Therapeutic Potential of Bioactive Compounds, 2nd Edition)
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38 pages, 5024 KB  
Article
Improving Sexual Dysfunction with Cinnamon Leaf Extract and Nanoemulsion by Using a Rat Model
by Yi-No Wu, Jin-Wei Lee, Han-Sun Chiang, Baskaran Stephen Inbaraj, Wen-Jhen Chen and Bing-Huei Chen
Pharmaceuticals 2026, 19(2), 284; https://doi.org/10.3390/ph19020284 - 7 Feb 2026
Viewed by 1082
Abstract
Background/Objectives: Taiwan cinnamon leaves have been reported to be effective in improving chronic diseases. Herein, cinnamon leaf extract (CLE) and nanoemulsion (CLEN) were prepared to explore their effects in improving sexual dysfunction in rats. Methods: Following extraction with 80% ethanol and analysis by [...] Read more.
Background/Objectives: Taiwan cinnamon leaves have been reported to be effective in improving chronic diseases. Herein, cinnamon leaf extract (CLE) and nanoemulsion (CLEN) were prepared to explore their effects in improving sexual dysfunction in rats. Methods: Following extraction with 80% ethanol and analysis by UPLC-MS/MS, CLEN was prepared using an optimal ratio of soybean oil, lecithin, Tween 80, deionized water, and CLE. A total of 48 male rats and 48 female rats were used, with the former being induced with erectile dysfunction, followed by treatment with CLEN or CLE at two doses (100 mg/kg and 50 mg/kg) for 4 weeks. After conducting the penile reflex test, male rats were paired with female rats for measurement of sexual behavior and ICP/MAP. Following sacrifice, α-SMA, nNOS, and β-III tubulin expression areas were measured by histochemical analyses; SMC/collagen ratio by Masson’s trichrome staining; and NO, cGMP, and PDE5 levels by ELISA kits. Results: CLEN was more effective than CLE in increasing intromission frequency, decreasing intromission and ejaculation latency, and recovering erectile response for improving copulatory and ejaculatory performances. A higher maximum ICP/MAP ratio was shown for CLEN through elevation of neurovascular function and erectile capacity. Additionally, CLEN efficiently reduced fibrosis, enhanced neuronal marker expression, and increased the SMC/collagen ratio, leading to penile tissue protection and neural regeneration. Both treatments showed elevated levels of NO and cGMP with a reduction in PDE5, probably through modulation of the NO-cGMP signaling pathway. Conclusions: CLEN was more effective than CLE in restoring erectile function in rats. Some more clinical trials are needed to verify this finding. Full article
(This article belongs to the Special Issue Plant-Based Extracts and the Therapeutic Potential of Bioactive Compounds, 2nd Edition)
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17 pages, 1421 KB  
Article
Bassia indica Attenuates Cardiotoxicity in a Rat Model via Anti-Inflammatory, Antioxidant, and Keap1/Nrf2 Modulation
by Fayyaz Anjum, Saad Touqeer, QurratUlAin Jamil, Ayesha Rida, Hafiz Muhammad Zubair, Adeel Sarfraz, Saleh Alfuraih, Waad Alrohily, Ali F. Almutairy, Ashfaq Ahmad, Mohammed Aufy and Shahid Muhammad Iqbal
Pharmaceuticals 2025, 18(12), 1907; https://doi.org/10.3390/ph18121907 - 18 Dec 2025
Cited by 1 | Viewed by 571
Abstract
Background: Drug-induced cardiotoxicity is a primary concern in clinical practice, especially in the context of oxidative stress induced by anti-cancer, antiviral, and antidiabetic drugs. Several strategies are devised to limit cardiotoxicity, which are supportive and provide symptomatic relief. This highlights the need [...] Read more.
Background: Drug-induced cardiotoxicity is a primary concern in clinical practice, especially in the context of oxidative stress induced by anti-cancer, antiviral, and antidiabetic drugs. Several strategies are devised to limit cardiotoxicity, which are supportive and provide symptomatic relief. This highlights the need to develop cardioprotective agents that circumvent the oxidative stress. Bassia indica is a cardiotonic plant with antioxidant properties traditionally used in Africa, South Asia, and China. We investigated its cardioprotective effects against doxorubicin-induced cardiotoxicity (DIC). Methods: B. indica extract (BiE) was analyzed by GC-MS and HPLC. Several antioxidant assays, including DPPH, FRAP, CUPRAC, NO, and H2O2 scavenging, were performed. In vivo attenuation of DIC was assessed in a rat model. Results: BiE contained several bioactive flavonoids, including 2-methoxy-4-vinylphenol, ferulic acid, gallic acid, kaempferol, and coumaric acid. Antioxidant assays demonstrated potent free-radical scavenging and antioxidant activity of BiE, providing mechanistic evidence for its in vivo amelioration of DIC. BiE treatment reduced myocardial oxidative stress by increasing endogenous antioxidant levels (p < 0.01), including SOD, CAT, and GSH. It upregulated Nrf2 and lowered Keap1 levels. This was also reflected in the restoration of cardiac tissue architecture and modulation of inflammatory markers, including IL-1β and TNF-α (p < 0.01). Cardiac tissue biomarkers were also improved. Conclusions: These findings conclude that BiE exerts cardiac protection by reducing oxidative stress and inflammation through modulation of the Keap1/Nrf2 pathway and decreasing the expression of IL-1β and TNF-α. Full article
(This article belongs to the Special Issue Plant-Based Extracts and the Therapeutic Potential of Bioactive Compounds, 2nd Edition)
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25 pages, 3418 KB  
Article
Nanovesicles from Rosa canina: A Treasure Trove of Antioxidant Potential for Oxidative Stress, Inflammation, and Gut Microbiota Modulation
by Gaia Cusumano, Agnese Bertoldi, Eleonora Calzoni, Husam B. R. Alabed, Laura Dorina Dinu, Emanuel Vamanu, Florentina Matei, Gokhan Zengin and Carla Emiliani
Pharmaceuticals 2025, 18(11), 1672; https://doi.org/10.3390/ph18111672 - 5 Nov 2025
Viewed by 1240
Abstract
Background/Objectives: Extracellular vesicles (EVs) have become key facilitators of communication between cells, significantly influencing various physiological functions. Although EVs originating from mammalian cells have been heavily researched for their therapeutic applications, there is a growing interest in extracellular vesicles derived from edible plants [...] Read more.
Background/Objectives: Extracellular vesicles (EVs) have become key facilitators of communication between cells, significantly influencing various physiological functions. Although EVs originating from mammalian cells have been heavily researched for their therapeutic applications, there is a growing interest in extracellular vesicles derived from edible plants (PDEVs) because of their unique bioactive characteristics. These nanovesicles (NVs) exhibit remarkable biocompatibility, low immunogenicity, and the ability to overcome biological barriers, making them promising candidates for biomedical applications. This study aimed to evaluate the antioxidant and anti-inflammatory properties of NVs isolated from Rosa canina berries. Methods: Antioxidant activity was assessed through in vitro assays, confirming their ability to fight oxidative stress. Additionally, enzymatic inhibition tests were conducted to explore their potential role in regulating key metabolic pathways associated with inflammation and oxidative damage. The antioxidant and anti-inflammatory activity of Rosa canina NVs was further tested on a THP-1 cell-based inflammation model, demonstrating their ability to modulate the inflammatory response at the cellular level. Moreover, the impact of these NVs on gut microbiota was investigated to assess their protective effects on antibiotic-induced dysbiosis. Results: The results demonstrated their ability to modulate oxidative stress, regulate enzymatic pathways, reduce inflammation in THP-1 cells, and influence gut microbiota in a positive manner. Full article
(This article belongs to the Special Issue Plant-Based Extracts and the Therapeutic Potential of Bioactive Compounds, 2nd Edition)
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19 pages, 6106 KB  
Article
Therapeutic Potential of Bioactive Compounds in Edible Mushroom-Derived Extracellular Vesicles: Isolation and Characterization of EVs from Pleurotus eryngii
by Gaia Cusumano, Agnese Bertoldi, Eleonora Calzoni, Husam B. R. Alabed, Roberto Maria Pellegrino, Lorena Urbanelli, Gokhan Zengin, Giancarlo Angeles Flores, Roberto Venanzoni, Paola Angelini and Carla Emiliani
Pharmaceuticals 2025, 18(9), 1362; https://doi.org/10.3390/ph18091362 - 12 Sep 2025
Viewed by 1561
Abstract
Background/Objectives: Over the past twenty years, there has been a rapid increase in studies aimed at comprehending how cells communicate with each other via Extracellular Vesicles (EVs), accompanied by a heightened interest in plant-derived extracellular vesicles due to their potential relevance in [...] Read more.
Background/Objectives: Over the past twenty years, there has been a rapid increase in studies aimed at comprehending how cells communicate with each other via Extracellular Vesicles (EVs), accompanied by a heightened interest in plant-derived extracellular vesicles due to their potential relevance in dietary supplementation and therapeutic applications. However, there is a limited amount of research on extracellular vesicles derived from mushrooms (MDEVs). Among edible mushrooms, Pleurotus eryngii is peculiar due to its flavor and interesting nutritional profiling. It also produces a wide array of secondary metabolites including biologically active compounds with many health-promoting benefits such as anticancer, antioxidant, antitumor, antiviral, antibacterial, antidiabetic, and anti-hypercholesteremic activities. The aim of this work has been to isolate EVs from the fruiting body and mycelium of P. eryngii in order to investigate their potential applications as nutraceuticals. Methods: MDEVs were isolated by differential and density gradient centrifugation, characterized by Nanoparticle Tracking Analysis (NTA), Scanning Electron Microscopy (SEM) and immunoblotting, and subjected to metabolomic and phenolic profiling. Their antioxidant potential was assessed through in vitro radical scavenging (DPPH, ABTS) and metal-reducing (CUPRAC, FRAP) assays. Results: The findings suggest that mycelium-derived EVs may represent a valuable source of high-quality MDEVs, which exhibited promising antioxidant properties in all assays conducted, particularly in radical scavenging assays. Conclusions: These results highlight the potential of P. eryngii mycelium-derived EVs as a novel natural source of bioactive compounds, paving the way for future applications in nutraceutical and therapeutic fields. Full article
(This article belongs to the Special Issue Plant-Based Extracts and the Therapeutic Potential of Bioactive Compounds, 2nd Edition)
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20 pages, 1780 KB  
Article
Exploring the Impact of Ultrasound-Assisted Extraction on the Phytochemical Composition and Bioactivity of Tamus communis L. Fruits
by Irene Gouvinhas, Maria José Saavedra, Maria José Alves and Juliana Garcia
Pharmaceuticals 2025, 18(9), 1342; https://doi.org/10.3390/ph18091342 - 6 Sep 2025
Cited by 2 | Viewed by 1541
Abstract
Background/Objectives: The health benefits of Tamus communis fruits have been associated with their high phenolic content, which comprises several flavonoids. However, the extraction methods might significantly impact these valuable compounds’ bioactivity. Therefore, the current study assesses how different extraction techniques affect T. [...] Read more.
Background/Objectives: The health benefits of Tamus communis fruits have been associated with their high phenolic content, which comprises several flavonoids. However, the extraction methods might significantly impact these valuable compounds’ bioactivity. Therefore, the current study assesses how different extraction techniques affect T. communis extracts’ antioxidant, anti-aging, antimicrobial, cytotoxic, anti-inflammatory, and phenolic contents. Methods: Conventional method (TCE-CM) and ultrasound-assisted extraction (TCE-UM) were the methods employed. Results: The increased phenolic content of TCE-UM, particularly flavonoids and phenolic acids, was demonstrated to be a contributing factor to its higher biological activity. Key enzymes linked to dermatological conditions, such as elastase, collagenase, hyaluronidase, and tyrosinase, were significantly inhibited by both extracts at 1 mg/mL; TCE-UM showed the highest tyrosinase inhibition (65.61  ±  5.21%) compared to TCE-CM (21.78  ±  2.19%). TCE-UM also demonstrated exceptional antibacterial performance, showing notable antibiofilm and metabolic inactivation effects and potent activity against pathogens such as Staphylococcus aureus, Escherichia coli, and Candida albicans. Both extracts showed concentration-dependent anti-inflammatory properties; TCE-UM had a lower IC50 value (26.46 ± 2.30%) in nitric oxide inhibition tests, suggesting stronger anti-inflammatory capabilities. Conclusions: These findings underscore the superior bioactivity of TCE-UM and suggest that ultrasonic extraction is a more efficient method for isolating bioactive phenolic compounds from T. communis fruits, presenting promising applications in anti-aging and antimicrobial formulations. Full article
(This article belongs to the Special Issue Plant-Based Extracts and the Therapeutic Potential of Bioactive Compounds, 2nd Edition)
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25 pages, 1710 KB  
Article
Phytochemical Profiling, Antioxidant Activity, and In Vitro Cytotoxic Potential of Mangrove Avicennia marina
by Federico Cerri, Beatrice De Santes, Francesca Spena, Lucia Salvioni, Matilde Forcella, Paola Fusi, Stefania Pagliari, Henrik Stahl, Paolo Galli, Miriam Colombo, Marco Giustra and Luca Campone
Pharmaceuticals 2025, 18(9), 1308; https://doi.org/10.3390/ph18091308 - 31 Aug 2025
Cited by 6 | Viewed by 2596
Abstract
Background: Avicennia marina (Forsk.) Vierh., a widely distributed mangrove species, is known for its diverse secondary metabolites with potential pharmacological applications. Despite its dominance in the Arabian Gulf, where A. marina may have adapted to extreme environmental conditions with a distinct set [...] Read more.
Background: Avicennia marina (Forsk.) Vierh., a widely distributed mangrove species, is known for its diverse secondary metabolites with potential pharmacological applications. Despite its dominance in the Arabian Gulf, where A. marina may have adapted to extreme environmental conditions with a distinct set of bioactive molecules, research in this region remains limited. Methods: This study investigates the phytochemical composition, antioxidant activity, and in vitro cytotoxicity of extracts from different plant parts, including roots, leaves, propagules, pericarps, and cotyledons, collected in the United Arab Emirates (UAE). Extracts were analyzed using ultra-pressure liquid chromatography coupled with high-resolution mass spectrometry (UPLC-HRMS). Antioxidant activity was assessed using DPPH and ABTS assays, while cytotoxicity was evaluated against human cancer and normal cell lines. Results: Analysis revealed 49 compounds, including iridoid glycosides, hydroxycinnamic acids, phenylethanoid glycosides, flavonoid glycosides, and triterpene saponins, several reported for the first time in A. marina and mangroves. The pericarp and root extracts exhibited the highest scavenging activity (DPPH: 187.14 ± 2.87 and 128.25 ± 1.12; ABTS: 217.16 ± 2.67 and 147.21 ± 2.42 μmol TE/g, respectively), correlating with phenylethanoid content. The root extract also displayed the highest cytotoxicity, with IC50 values of 58.46, 81.98, and 108.10 μg/mL against MDA-MB-231, SW480, and E705, respectively. In silico analysis identified triterpene saponins as potential contributors. Conclusions: These findings highlight the root extract of A. marina as a promising source of bioactive compounds with potential antioxidant and anticancer applications, supporting further exploration for novel therapeutic candidates. Full article
(This article belongs to the Special Issue Plant-Based Extracts and the Therapeutic Potential of Bioactive Compounds, 2nd Edition)
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Review

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35 pages, 3451 KB  
Review
Beyond Traditional Use: The Scientific Evidence for the Role of Astragali radix in Organ Protection via Modulating Oxidative Stress, Cell Death, and Immune Responses
by Chuan Lin, Huiqiang Liu, Siyi Dong, Le Yang, Ling Kong, Yu Guan, Hui Sun, Guangli Yan, Ye Sun, Ying Han and Xijun Wang
Pharmaceuticals 2025, 18(10), 1448; https://doi.org/10.3390/ph18101448 - 26 Sep 2025
Cited by 4 | Viewed by 2693
Abstract
Astragali radix (AR) is a traditional Chinese herbal medicine derived from the roots of Astragalus membranaceus and A. mongholicus. AR exhibits a wide range of pharmacological activities, such as cardioprotective, hypoglycemic, antitumor, antiviral, and multi-organ restorative effects. Nearly 400 bioactive compounds have [...] Read more.
Astragali radix (AR) is a traditional Chinese herbal medicine derived from the roots of Astragalus membranaceus and A. mongholicus. AR exhibits a wide range of pharmacological activities, such as cardioprotective, hypoglycemic, antitumor, antiviral, and multi-organ restorative effects. Nearly 400 bioactive compounds have been identified in AR by phytochemical investigations, with astragalus polysaccharides (APS), astragalosides (I–IV), formononetin (FMN), and calycosin (CA) established as principal bioactive constituents. These components exhibit multifunctional mechanisms encompassing antioxidative stress, apoptotic suppression, autophagy regulation, anti-inflammation, and immune regulation, thereby exerting significant protective effects on critical organ systems such as the cardiovascular, renal, neural, hepatic, gastrointestinal, and immune systems. This review synthesized research over the past three decades, elucidating the organ protective mechanisms of AR through phytochemical profiling. Key findings demonstrated that FMN-mediated Nrf2 pathway activation could attenuate reactive oxygen species (ROS) generation, while astragaloside IV (AS-IV) could suppress endoplasmic reticulum stress by inactivating the PERK/ATF6/CHOP axis to ameliorate apoptosis. Additionally, comprehensive safety assessment and pharmacokinetic analysis also substantiated favorable bioavailability and toxicological profiles. To sum up, these findings provide a comprehensive theoretical basis and offer innovative strategies for preventing and treating complex diseases associated with multi-organ dysfunction, thereby facilitating future clinical applications. Full article
(This article belongs to the Special Issue Plant-Based Extracts and the Therapeutic Potential of Bioactive Compounds, 2nd Edition)
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