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Advances in the Mechanism of Action and the Therapeutic Role...
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Advances in the Mechanism of Action and the Therapeutic Role of Phytopharmaceuticals

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

Deadline for manuscript submissions: 20 August 2026 | Viewed by 17326

Special Issue Editors

Dr. Maria-Eleni Grafakou

E-Mail Website
Guest Editor
Faculty of Pharmacy and Chemistry, University of Regensburg, Regensburg, Germany
Interests: biotransformation; medicinal plants; phytochemistry; biological activity; specialized metabolites
Prof. Dr. Jörg Heilmann

E-Mail Website
Guest Editor
Faculty of Pharmacy and Chemistry, University of Regensburg, Regensburg, Germany
Interests: pharmaceutical biology; natural product chemistry; medicinal plants; metabolism

Special Issue Information

Dear Colleagues,

There is evidence supporting the therapeutic use of plants since prehistoric times. Today, herbal medicines play a pivotal role in preventing and treating diseases associated with modern civilization, while natural products remain a rich source of lead structures for drug development.

Through evolutionary processes, plants have developed sophisticated chemical defense mechanisms, producing diverse specialized bioactive compounds such as terpenoids, flavonoids, and alkaloids. These compounds are critical for plants' ecological fitness and survival, but they also exhibit significant pharmacological properties in humans. Understanding the mechanisms of action of these bioactive metabolites fosters innovation in drug discovery and provides deeper insights into the therapeutic potential of plant-derived compounds in addressing complex diseases, including cancer, neurodegenerative disorders, and metabolic syndromes.

In recent years, biotransformation studies have emerged, focusing on the structural modification of phytochemicals by biological systems, including interactions with the microbiome in various niches of the human body. These studies have provided new perspectives on the therapeutic roles of medicinal plants.

This Special Issue invites original research and review articles that explore these dimensions of phytochemicals and medicinal plants. Topics of interest include investigations of bioactive specialized metabolites, their molecular targets, biotransformation pathways, interactions with the microbiome, and innovative therapeutic applications. This issue aims to provide a comprehensive overview of the state-of-the-art in this field, highlight the latest discoveries, and elucidate future research directions.

Dr. Maria-Eleni Grafakou
Prof. Dr. Jörg Heilmann
Guest Editors

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

  • medicinal plants
  • natural products
  • phytochemistry
  • biological activities
  • mechanism of action
  • biotransformation
  • microbiome

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Published Papers (5 papers)

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Research

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26 pages, 4316 KB  
Article
Protective Effects of Licorice (Glycyrrhiza uralensis) Against Vancomycin-Induced Nephrotoxicity In Vivo and In Vitro
by Jianping Zhang, Yan Zhou, Ruirui Cui, Lijun Wang, Sijia Wang, Wenhan Rao and Xinan Wu
Pharmaceuticals 2026, 19(5), 728; https://doi.org/10.3390/ph19050728 - 4 May 2026
Abstract
Background: Vancomycin (VAN)-induced nephrotoxicity limits its clinical application. Licorice (Glycyrrhiza uralensis Fisch.) and its bioactive constituents have been reported to protect against nephrotoxicity induced by various nephrotoxic agents. This study aimed to evaluate the protective effects of licorice against VAN-induced nephrotoxicity and [...] Read more.
Background: Vancomycin (VAN)-induced nephrotoxicity limits its clinical application. Licorice (Glycyrrhiza uralensis Fisch.) and its bioactive constituents have been reported to protect against nephrotoxicity induced by various nephrotoxic agents. This study aimed to evaluate the protective effects of licorice against VAN-induced nephrotoxicity and to explore the underlying mechanisms both in vivo and in vitro. Methods: Seven groups of male C57BL/6 mice received different treatments for 7 consecutive days. Blood, fecal and renal tissue samples were collected for the assessment of serum creatinine, renal histopathology, mitochondrial ultrastructure, oxidative stress markers, kidney injury molecule-1 (Kim-1), short-chain fatty acids (SCFAs), and uremic toxins. In human proximal tubular epithelial cells (HK-2 cells), the effects of licorice on cell viability, oxidative stress, inflammatory markers, and mitochondrial membrane potential (MMP) were further investigated. Results: Licorice significantly attenuated VAN-induced nephrotoxicity and restored glutathione peroxidase (GSH-Px) activity while reducing malondialdehyde (MDA) levels. In addition, licorice markedly ameliorated VAN-induced renal histopathological injury, as demonstrated by hematoxylin and eosin staining and transmission electron microscopy. Licorice also reversed VAN-induced intestinal microbiota dysbiosis and increased the relative abundance of SCFA-producing bacteria, including Bacteroides. Moreover, licorice treatment increased fecal SCFA contents and modulated multiple uremic toxins in both serum and renal tissue. Consistently, licorice protected HK-2 cells against VAN-induced cytotoxicity by regulating GSH, interleukin-1β (IL-1β), interleukin-6 (IL-6), tumor necrosis factor-α (TNF-α), and MMP. Conclusions: These findings demonstrate that licorice exerts protective effects against VAN-induced nephrotoxicity in vivo and in vitro, suggesting the potential involvement of oxidative stress, mitochondrial structure and function, inflammation, intestinal microbiota-SCFAs and uremic toxins. Full article
(This article belongs to the Special Issue Advances in the Mechanism of Action and the Therapeutic Role of Phytopharmaceuticals)
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17 pages, 4704 KB  
Article
Ginsenoside Rg1 Ameliorates the Learning and Memory Deficits of 5xFAD Mice by Inhibiting CCR3 Activity: Insights from In Vivo and In Vitro Investigations
by Hui Lu, Ying Yu, Ying Yang, He Li, Yangyi Li, Tianhao Yu, Shixue Wang, Fengzhen Li and Xiaorui Cheng
Pharmaceuticals 2026, 19(5), 661; https://doi.org/10.3390/ph19050661 - 23 Apr 2026
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Abstract
Background/Objectives: Alzheimer’s disease (AD) is characterized by amyloid-beta accumulation and neuroinflammation, yet the molecular target of Ginsenoside Rg1 remains elusive. This study aimed to elucidate the neuroprotective mechanism of Ginsenoside Rg1, specifically investigating its interaction with C-C motif chemokine receptor 3 (CCR3). [...] Read more.
Background/Objectives: Alzheimer’s disease (AD) is characterized by amyloid-beta accumulation and neuroinflammation, yet the molecular target of Ginsenoside Rg1 remains elusive. This study aimed to elucidate the neuroprotective mechanism of Ginsenoside Rg1, specifically investigating its interaction with C-C motif chemokine receptor 3 (CCR3). Methods: We utilized 5xFAD transgenic mice and CCR3-overexpressing BV2 microglial cells. Behavioral assessments, enzyme-linked immunosorbent assays, quantitative real-time polymerase chain reaction, molecular docking, and surface plasmon resonance were employed to evaluate cognitive function and molecular pathways. Results: Ginsenoside Rg1 treatment significantly ameliorated spatial learning and memory deficits. Quantitatively, Rg1 reduced cortical amyloid-beta 1–40 levels (p < 0.05) and bound directly to CCR3 with a dissociation constant of 3.599 × 10−5 mol/L. This inhibition suppressed neuroinflammation and restored neurotrophic factors, including Brain-derived neurotrophic factor. Conclusions: CCR3 is a novel pharmacological target for Ginsenoside Rg1, providing a precise molecular basis for its neuroprotective effects. Future research should focus on clarifying the pharmacokinetic profile and brain bioavailability of Ginsenoside Rg1 to facilitate clinical translation. Full article
(This article belongs to the Special Issue Advances in the Mechanism of Action and the Therapeutic Role of Phytopharmaceuticals)
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21 pages, 11682 KB  
Article
Mechanism of Bao Jing Tablets in Chronic Prostatitis/Chronic Pelvic Pain Syndrome: Insights from Multi-Omics and Network Pharmacology
by Haitao Ge, Yan Zhang, Siqi Jin, Chen Wang and Fujiang Wang
Pharmaceuticals 2026, 19(4), 632; https://doi.org/10.3390/ph19040632 - 17 Apr 2026
Viewed by 362
Abstract
Background/Objectives: To investigate the therapeutic potential and mechanistic basis of Bao Jing Tablet (BJT) for chronic prostatitis/chronic pelvic pain syndrome (CP/CPPS) via an experimental autoimmune prostatitis (EAP) rat model, through integrating network pharmacology, metabolomics, proteomics, and animal experiments. Methods: UPLC-ZenoTOF 7600-MS/MS [...] Read more.
Background/Objectives: To investigate the therapeutic potential and mechanistic basis of Bao Jing Tablet (BJT) for chronic prostatitis/chronic pelvic pain syndrome (CP/CPPS) via an experimental autoimmune prostatitis (EAP) rat model, through integrating network pharmacology, metabolomics, proteomics, and animal experiments. Methods: UPLC-ZenoTOF 7600-MS/MS was used to analyze the chemical composition of BJT. The therapeutic effect of BJT was evaluated using an experimental autoimmune prostatitis (EAP) rat model. Lipid metabolomics, proteomics, and integrated network pharmacology analyses were performed to investigate the potential mechanisms and active components of BJT in treatment. Results: A total of 174 constituents were identified in BJT, among which 54 major active compounds were screened for further analysis. Network pharmacology and combined multi-omics analysis indicate that the protein targets of HIF-1α, Akt, and PI3K/Akt, as well as the Glycolysis pathway, play important roles in the improvement of CP/CPPS. Conclusions: Our results demonstrated that BJT was an effective drug to improve the development of CP/CPPS. This is associated with the PI3K/Akt–HIF-1α-Glycolysis pathways. Full article
(This article belongs to the Special Issue Advances in the Mechanism of Action and the Therapeutic Role of Phytopharmaceuticals)
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Review

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37 pages, 1748 KB  
Review
Pharmacological Insights and Technological Innovations in Curcuma longa L. and Echinacea purpurea (L.) Moench as Plant-Derived Immunomodulators
by Juan Pablo Espinoza, Valentina Guajardo, Maité Rodríguez-Díaz, Mabel Moreno, Carolina Klagges, Mario Castillo-Ruiz and María Carolina Otero
Pharmaceuticals 2026, 19(1), 93; https://doi.org/10.3390/ph19010093 - 3 Jan 2026
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Abstract
Immune dysregulation and chronic inflammation are central contributors to many diseases. Curcuma longa L. and Echinacea purpurea (L.) Moench are widely used medicinal plants with extensive preclinical evidence supporting immunomodulatory effects. Their key metabolites, curcuminoids, turmerones, alkamides, polysaccharides, and caffeic acid derivatives, engage [...] Read more.
Immune dysregulation and chronic inflammation are central contributors to many diseases. Curcuma longa L. and Echinacea purpurea (L.) Moench are widely used medicinal plants with extensive preclinical evidence supporting immunomodulatory effects. Their key metabolites, curcuminoids, turmerones, alkamides, polysaccharides, and caffeic acid derivatives, engage with critical pathways, including NF-κB, MAPK, JAK/STAT, and Nrf2. This interaction modulates cytokine production, oxidative stress responses, and both innate and adaptive immune activities. Although numerous mechanistic and early clinical studies support these actions, human evidence remains inconsistent, partly due to poor and variable oral bioavailability and substantial heterogeneity in extract composition, despite the existence of some standardized preparations. Recent technological strategies, including micelles, phytosomes, phospholipid complexes, nanoemulsions, polymeric nanoparticles, and liposomal systems, have improved solubility, stability, and systemic exposure of key metabolites, particularly curcuminoids. However, clinical results are still limited and often derived from small or heterogeneous trials. This review summarizes the ethnopharmacological background, mechanistic data, clinical findings, and formulation advances for both species and highlights the translational barriers that restrict their therapeutic application. Rigorous clinical studies using standardized and technologically optimized preparations are required to determine the true immunomodulatory potential of C. longa and E. purpurea. Full article
(This article belongs to the Special Issue Advances in the Mechanism of Action and the Therapeutic Role of Phytopharmaceuticals)
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Other

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12 pages, 1077 KB  
Systematic Review
Hawthorn (Crataegus spp.) Clinically Significantly Reduces Blood Pressure in Hypertension: A Meta-Analysis of Randomized Placebo-Controlled Clinical Trials
by Zsóka Szikora, Rebeka Olga Mátyus, Bettina Vargáné Szabó, Dezső Csupor and Barbara Tóth
Pharmaceuticals 2025, 18(7), 1027; https://doi.org/10.3390/ph18071027 - 10 Jul 2025
Cited by 5 | Viewed by 14576
Abstract
Background/Objectives: Hypertension affects over 1.3 billion people globally, and inadequate therapy is reported in 80% of cases. Patients increasingly turn to complementary therapies, including hawthorn (Crataegus spp.), a traditional remedy for cardiovascular diseases. Hawthorn has long been used in folk medicine [...] Read more.
Background/Objectives: Hypertension affects over 1.3 billion people globally, and inadequate therapy is reported in 80% of cases. Patients increasingly turn to complementary therapies, including hawthorn (Crataegus spp.), a traditional remedy for cardiovascular diseases. Hawthorn has long been used in folk medicine to lower blood pressure; however, its efficacy has not been fully established. This meta-analysis aimed to evaluate the antihypertensive effects and safety of hawthorn in randomized, placebo-controlled trials. Methods: A systematic review and meta-analysis were conducted, including six studies with a total of 428 participants. The trials focused on systolic (SBP) and diastolic blood pressure (DBP) changes over treatment periods of 10 weeks to 6 months. Literature searches were conducted in the Embase, PubMed, Cochrane, and Web of Science databases. Studies that met the predefined PICO criteria were included. Data analysis was performed using a random-effects model, and the risk of bias was assessed using the Cochrane Risk of Bias Tool. Results: Hawthorn statistically significantly decreased SBP (MD: −6.65 mmHg; 95% CI [−11.72; 1.59]) and non-significantly reduced DBP (MD: −7.19 mmHg; 95% CI [−15.17; 0.79]) after 2–6 months of treatment. Variations in dosage (250–1200 mg/day) and study protocols contributed to this heterogeneity. Conclusions: The effect of hawthorn on blood pressure is clinically significant. However, larger, well-designed trials are needed to establish optimal dosing, duration, and efficacy with greater reliability. Full article
(This article belongs to the Special Issue Advances in the Mechanism of Action and the Therapeutic Role of Phytopharmaceuticals)
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