{"title":"Obeticholic Acid and Other Farnesoid-X-Receptor (FXR) Agonists in the Treatment of Liver Disorders.","authors":"Stefano Fiorucci, Ginevra Urbani, Eleonora Distrutti, Michele Biagioli","doi":"10.3390/ph18091424","DOIUrl":"10.3390/ph18091424","url":null,"abstract":"<p><p>The Farnesoid-X-receptor (FXR) is a bile sensor involved in the regulation of bile acid homeostasis, fibrosis, inflammation, and metabolism. Obeticholic acid (OCA), a semisynthetic derivative of chenodeoxycholic acid (CDCA), initially named 6-ethyl-CDCA or INT-747, is the first in a class of FXR ligands that have been approved for clinical use for the treatment of patients with primary biliary cholangitis (PBC) who are unresponsive or intolerant to ursodeoxycholic acid. In this narrative review, we will examine the current status and future perspective of clinical use of OCA. Based on results from phase 2 and 3 clinical trials, OCA received a conditional market approval for its use as a second-line treatment for the management of PBC in 2016. However, concerns over drug (OCA)-induced liver injury (DILI), including hepatic decompensation in cirrhotic and non-cirrhotic PBC patients, have led to discontinuation of OCA commercialization in the EU, but not in North America and the UK, in 2024. Based on positive results from preclinical models, OCA has been investigated also for the treatment of metabolic dysfunction-associated steatohepatitis (MASH). Results from phase 2 and 3 trials, however, have shown that while OCA reduces liver fibrosis, the beneficial effects on steatosis are marginal, thus preventing its clinical approval under the current regulatory guidelines. Here, we review potential applications of OCA in PBC patients in the context of a highly competitive therapeutic landscape, generated by the approval for clinical use of safer and effective second-line therapies, including PPARs agonists such as elafibranor and seladelapar and increased off-label use of fibrates. The current status of development of second-generation FXR agonists such as cilofexor, tropifexor, and vonafexor and their potential in the treatment of liver fibrosis in MASH will be discussed and compared to recently approved therapies, resmetirom, and semaglutide, a GLP-1 agonist. Finally, since some of the novel candidates for treating MASH, have shown limited efficacy on liver fibrosis, we suggest that development of combinatorial therapies based on FXR ligands and agents acting on different molecular targets might offer the opportunity for the repositioning of drug candidates whose development has been abandoned for insufficient efficacy, minimizing/recovering costs linked to drug development.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":"18 9","pages":""},"PeriodicalIF":4.8,"publicationDate":"2025-09-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12472620/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145177683","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Jan Siwiec, Kornelia Kuźnik-Trocha, Katarzyna Winsz-Szczotka, Katarzyna Komosińska-Vassev, Andrzej Siwiec, Krystyna Olczyk
{"title":"The Impact of 24-Month Etanercept Therapy on Changes in Adiponectin, Leptin and Tenascin C Levels in the Blood of Children with Juvenile Idiopathic Arthritis.","authors":"Jan Siwiec, Kornelia Kuźnik-Trocha, Katarzyna Winsz-Szczotka, Katarzyna Komosińska-Vassev, Andrzej Siwiec, Krystyna Olczyk","doi":"10.3390/ph18091423","DOIUrl":"10.3390/ph18091423","url":null,"abstract":"<p><p><b>Background/Objectives</b>: The most commonly diagnosed group of rheumatic diseases in children is juvenile idiopathic arthritis. It is characterized by a chronic inflammatory process that leads to the degradation of the bone and joint system and increased secretion of pro-inflammatory cytokines such as TNF-α, IL-1, and IL-6. These cytokines contribute to the dysregulation of adipocytokine metabolism, including adiponectin and leptin, as well as extracellular matrix components, such as tenascin C. While it is known that children with JIA exhibit TNF-α-stimulated degradation of most ECM cartilage components, the effect of TNF-α antagonists, such as etanercept, on these processes has not yet been evaluated. Therefore, the aim of our study was to assess the dynamics of changes in tenascin C, adiponectin, and leptin levels in the blood of children with JIA, both before and during therapy. <b>Methods</b>: The study material consisted of blood samples collected from 66 children of both sexes, including 40 girls and 26 boys diagnosed with juvenile idiopathic arthritis and treated with etanercept, as well as from 40 healthy children (22 girls and 18 boys). The quantitative assessment of adiponectin, leptin, and tenascin C levels was performed using commercial ELISA tests. <b>Results</b>: The conducted study revealed that untreated children with JIA exhibit altered plasma levels of all examined parameters-adiponectin, leptin, and tenascin C. Specifically, there was an increase in adiponectin concentration and a decrease in leptin as well as TNC levels compared to healthy children. The results demonstrated the beneficial effects of the TNF-α antagonist, i.e., etanercept, which not only improved the clinical condition of children with JIA but also positively influenced the metabolism of both adipokines and tenascin C. <b>Conclusions</b>: The obtained results suggest the potential use of adiponectin, leptin, and tenascin C as biochemical markers of the effectiveness of etanercept therapy in inhibiting the progression of degenerative joint changes in children with JIA treated with TNF-α inhibitors.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":"18 9","pages":""},"PeriodicalIF":4.8,"publicationDate":"2025-09-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12472541/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145177837","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Ada Radu, Andrei-Flavius Radu, Gabriela S Bungau, Delia Mirela Tit, Paul Andrei Negru
{"title":"Tracing Five Decades of Psoriasis Pharmacotherapy: A Large-Scale Bibliometric Investigation with AI-Guided Terminology Normalization.","authors":"Ada Radu, Andrei-Flavius Radu, Gabriela S Bungau, Delia Mirela Tit, Paul Andrei Negru","doi":"10.3390/ph18091422","DOIUrl":"10.3390/ph18091422","url":null,"abstract":"<p><p><b>Background/Objectives</b>: Large-scale bibliometric assessments of psoriasis pharmacotherapy research remain limited despite significant research output in this rapidly evolving field. This study aimed to map the evolution of systemic psoriasis therapy research over five decades and demonstrate how systematic analysis of research trajectories can illuminate the transformation of specialized medical fields into central components of precision medicine. <b>Methods</b>: A comprehensive bibliometric analysis was conducted using Web of Science Core Collection as the single data source, examining 19,284 publications spanning 1975-2025. The methodology employed AI-enhanced terminology normalization for standardizing pharmaceutical nomenclature, VOSviewer version 1.6.20 for network visualization, and Bibliometrix package for temporal trend analysis and thematic evolution mapping. International collaboration networks, thematic evolution across three distinct periods (1975-2000, 2001-2010, 2011-2025), and citation impact patterns were systematically analyzed. <b>Results</b>: Four distinct developmental phases were identified, with publications growing from 9 articles in 1975 to 1638 in 2024. The United States dominated research output with 5959 documents, while Canada achieved the highest citation efficiency at 62.65 citations per document. Global collaboration encompassed 70 countries organized into four regional clusters, with a 28-nation Asia-Pacific-Africa-Middle East alliance representing the largest collaborative group. Citation impact peaked during 2001-2008, coinciding with revolutionary biological therapy introduction. Thematic evolution demonstrated systematic transformation from two foundational themes to nine specialized domains, ultimately consolidating into four core areas focused on targeted therapeutics and evidence-based methodologies. Keyword analysis demonstrated progression from basic immunological studies to sophisticated targeted interventions, evolving from tumor necrosis factor alpha inhibitors to contemporary interleukin-17/interleukin-23 pathway targeting and Janus kinase inhibitors. <b>Conclusions</b>: Over five decades, psoriasis therapeutics research has shifted from a niche dermatological discipline to a central model for innovation in immune-mediated diseases. This evolution illustrates how bibliometric approaches can capture the dynamics of scientific transformation, offering strategic insights for guiding pharmaceutical innovation, shaping research priorities, and informing precision medicine strategies across inflammatory conditions.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":"18 9","pages":""},"PeriodicalIF":4.8,"publicationDate":"2025-09-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12473059/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145177713","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"In Vivo Antihypertensive and Ex Vivo Vasodilatory Studies of Taxifolin.","authors":"Xuye Wang, Xiangyang Xu, Wan Yin Tew, Liyun Ouyang, Xiaoning Yang, Hui Wei Loh, Wen Xu, Wei Xu, Mun Fei Yam","doi":"10.3390/ph18091420","DOIUrl":"10.3390/ph18091420","url":null,"abstract":"<p><p><b>Background</b>: Hypertension is a leading cause of cardiovascular morbidity and mortality. Taxifolin has shown cardiovascular benefits, but its antihypertensive mechanisms remain poorly defined. This study aimed to comprehensively elucidate the molecular mechanisms underlying Taxifolin's blood pressure-lowering effects by integrating network pharmacology, molecular docking, ex vivo functional studies, and in vivo validation. <b>Methods</b>: Network pharmacology and molecular docking prioritized targets. Ex vivo thoracic aortas were obtained from healthy male Sprague-Dawley (SD) rats, and rings (3-4 mm) were prepared for vasorelaxation studies. Pathway-specific inhibitors, Western blotting, and ELISA were used to investigate mechanisms. In vivo, spontaneously hypertensive rats (SHRs) received oral Taxifolin 15, 30, or 60 mg/kg once daily for 28 days; propranolol (80 mg/kg) served as the positive control. <b>Results</b>: Taxifolin produced robust vasorelaxation in endothelium-intact rings (Rmax ≈ 121%), falling to ~72% after denudation. Relaxation was attenuated by LY294002, ODQ, indomethacin, and glibenclamide. In SHR aorta, Taxifolin increased NO by ~132% and cGMP by ~1.9-fold and upregulated p-Akt and eNOS; LY294002 abolished these effects. In vivo, Taxifolin reduced systolic blood pressure by ≈60 mmHg without adverse changes in hematology, biochemistry, or body weight. <b>Conclusions</b>: Taxifolin lowers blood pressure through multiple vascular mechanisms consistent with PI3K/Akt/eNOS, NO-sGC-cGMP, COX-2/PGI<sub>2</sub> and calcium-handling pathways, supporting its potential as a safe antihypertensive candidate.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":"18 9","pages":""},"PeriodicalIF":4.8,"publicationDate":"2025-09-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12473947/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145177674","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Damian Łomankiewicz, Barbara Pilawa, Ewa Chodurek, Magdalena Zdybel
{"title":"Interactions of Extracts from Selected Plant Materials Supporting the Treatment of Alzheimer's Disease with Free Radicals-EPR and UV-Vis Studies.","authors":"Damian Łomankiewicz, Barbara Pilawa, Ewa Chodurek, Magdalena Zdybel","doi":"10.3390/ph18091421","DOIUrl":"10.3390/ph18091421","url":null,"abstract":"<p><p><b>Background/objectives</b>: Interactions of infusions of <i>Ginkgo biloba</i>, ginseng, Yerba Mate, and green tea, with free radicals, were examined. The aim of these studies was to determine quenching of free radicals by the extracts from the selected plant raw materials that are useful in the treatment of Alzheimer's disease. <b>Methods</b>: The interactions were tested by an X-band (9.3 GHz) EPR spectroscopy and UV-Vis spectrophotometry. The model DPPH free radicals were used. The magnitude and changes with time of EPR and UV-Vis spectra of DPPH by the tested extracts were measured. <b>Results</b>: EPR and UV-Vis lines of DPPH free radicals decrease with increasing time of interactions of the extracts with DPPH, and after reaching the minimum value, it does not change with time. Ginseng infusion quenched free radicals the least. <i>Ginkgo biloba</i> extract quenches free radicals a little stronger than ginseng extract. Taking into account the tested extracts, <i>Ginkgo biloba</i> and ginseng extracts interact with free radicals less effectively compared to extracts of Yerba mate and green tea. <i>Ginkgo biloba</i> and ginseng extracts quench free radicals weaker than Yerba Mate and green tea extracts. <b>Conclusions</b>: Yerba Mate extract definitely had the strongest antioxidant properties. This extract quenches free radicals most effectively, what can be useful in the case of Alzheimer's disease. Given its strong antioxidant properties, green tea extract can also be particularly recommended in the case of Alzheimer's disease.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":"18 9","pages":""},"PeriodicalIF":4.8,"publicationDate":"2025-09-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12472563/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145177365","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"An Overview of Target Membrane Proteins for Near-Infrared Photoimmunotherapy.","authors":"Motofumi Suzuki, Hirofumi Hanaoka","doi":"10.3390/ph18091419","DOIUrl":"10.3390/ph18091419","url":null,"abstract":"<p><p>Near-infrared photoimmunotherapy (NIR-PIT) is a recently developed cancer treatment that utilizes antibody-photoabsorber (IRDye700DX [IR700]) conjugates and NIR light. Necrotic cell death associated with lethal membrane damage is induced when this conjugate binds to an antigen on cancer cells, and it is exposed to NIR light. Therefore, various membrane proteins are potential therapeutic targets for NIR-PIT, and many studies have described various target molecules and specific antibodies. To develop future drugs for NIR-PIT, the selection of appropriate target membrane proteins and monoclonal antibodies will be important. In this review, we summarize the membrane targets and antibodies for NIR-PIT used in previous studies, focusing on the characteristics of each molecule.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":"18 9","pages":""},"PeriodicalIF":4.8,"publicationDate":"2025-09-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12472690/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145177611","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Comprehensive Identification and Mechanistic Evaluation of Novel DHODH Inhibitors as Potent Broad-Spectrum Antiviral Agents.","authors":"Chao Zhang, Shiyang Sun, Huiru Xie, Yongzhao Ding, Chun Hu, Jialin Guo, Junhai Xiao","doi":"10.3390/ph18091416","DOIUrl":"10.3390/ph18091416","url":null,"abstract":"<p><p><b>Background/Objectives</b>: This study identifies novel dihydroorotate dehydrogenase (DHODH) inhibitors exhibiting potent broad-spectrum antiviral agents, particularly against influenza A virus (A/PR/8/34(H1N1)) and SARS-CoV-2. <b>Methods</b>: Structure-based virtual screening of 1.6 million compounds (ChemDiv and TargetMol databases) yielded 10 candidates, with compounds <b>6</b>, <b>9</b>, and <b>10</b> demonstrating significant anti-influenza activity (IC<sub>50</sub> = 4.85 ± 0.58, 7.35 ± 1.65, and 1.75 ± 0.28 μM, respectively). Building on these, molecular hybridization principles and scaffold hopping principles were applied to design and synthesize six novel compounds (<b>11</b>-<b>16</b>) through cyclization, coupling, and carboxylate deprotection. Prior to subsequent biological assays, the molecular structures of each compound were elucidated by NMR spectroscopy and MS. Their antiviral activities were subsequently assessed against both influenza virus and SARS-CoV-2. The compound <b>11</b>, demonstrating the most potent antiviral activity, was further subjected to surface plasmon resonance (SPR) analysis to assess its binding affinity for human DHODH. <b>Results</b>: Compound <b>11</b> emerged as the most potent DHODH inhibitor (<i>K</i><sub>D</sub> = 6.06 μM), exhibiting superior broad-spectrum antiviral activities (IC<sub>50</sub> = 0.85 ± 0.05 μM, A/PR/8/34(H1N1); IC<sub>50</sub> = 3.60 ± 0.67 μM, SARS-CoV-2) to the reported DHODH inhibitor (Teriflunomide<b>,</b> IC<sub>50</sub> = 35.02 ± 3.33 μM, A/PR/8/34(H1N1); IC<sub>50</sub> = 26.06 ± 4.32 μM, SARS-CoV-2). Mechanistic evaluations via 100 ns MD simulations and QM/MM calculations revealed stable binding interactions, particularly hydrogen bonds with GLN47 and ARG136, while alanine scanning mutagenesis confirmed these residues' critical roles in binding stability. <b>Conclusions</b>: This work identifies compound <b>11</b> as a potent broad-spectrum antiviral compound, offering a promising strategy for broad-spectrum antiviral therapy against RNA viruses by depleting pyrimidine pools essential for viral replication.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":"18 9","pages":""},"PeriodicalIF":4.8,"publicationDate":"2025-09-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12472551/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145177654","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Márton Kalabay, Zsófia Szász, Eszter Lajkó, Bálint Bagu, Éva Pállinger, Cintia Duró, Tamás Jernei, Antal Csámpai, Angéla Takács, László Kőhidai
{"title":"Comparative Study of Ferrocene- and Indene-Based Tamoxifen Derivatives of Different Molecular Flexibility on High-Mortality Cancer Cell Lines.","authors":"Márton Kalabay, Zsófia Szász, Eszter Lajkó, Bálint Bagu, Éva Pállinger, Cintia Duró, Tamás Jernei, Antal Csámpai, Angéla Takács, László Kőhidai","doi":"10.3390/ph18091417","DOIUrl":"10.3390/ph18091417","url":null,"abstract":"<p><p>Tamoxifen is a well-established selective estrogen receptor modulator (SERM) widely used in breast cancer treatment, yet its efficacy varies across tumor types. To enhance its antitumor potential, we previously synthesized and investigated novel ferrocene-linked (T5, T15) derivatives. This publication is a close continuation of this work, introducing a new indene-based (T6) derivative. <b>Objectives</b>: The main aim of this study was to further broaden our knowledge of the mechanism behind the increased antitumor effect of the ferrocene-linked drugs (T5 and T15) and compare it with a new, indene-based tamoxifen derivative, T6. The indene moiety was selected as a rigid, hydrophobic aromatic unit to probe pharmacological effects independent of ferrocene's redox activity. <b>Methods</b>: The compounds were tested on MCF7, MDA-MB231 and PANC1 cells. Cell viability was assessed with the AlamarBlue assay and the xCELLigence SP system. Reactive oxygen species (ROS) production was measured with the ROS Glo assay. Flow cytometry and RT-qPCR experiments were conducted to assess apoptosis and ROS regulation as well. <b>Results</b>: The modified compounds demonstrated an increased cell-viability-decreasing effect in breast (MCF7, MDA-MB-231) and pancreatic (PANC1) cancer cell lines, influencing both estrogen-receptor-dependent and -independent pathways. T6 led to G2/M phase arrest in PANC1 cells. Beyond cell cycle disruption, these derivatives significantly elevated ROS levels, contributing to apoptosis. <b>Conclusions</b>: Our findings suggest that these structural modifications retain tamoxifen's pharmacophore properties while expanding its mechanism of action, particularly through universal interactions independent of the ER status of tumor cells. The enhanced antitumor effects highlight the potential of these derivatives as promising candidates for improved cancer therapies.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":"18 9","pages":""},"PeriodicalIF":4.8,"publicationDate":"2025-09-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12472596/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145177506","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Jun-Ho Song, Yun-Soo Seo, Yeseul Kim, Sohee Jeong, Sungyu Yang, Goya Choi, Joong-Sun Kim, Inkyu Park
{"title":"Integrative Study of Dipsaci Radix and Phlomidis Radix: Nomenclature, Morphology, DNA-Based Authentication, and Comparative Effects on Osteoclastogenesis.","authors":"Jun-Ho Song, Yun-Soo Seo, Yeseul Kim, Sohee Jeong, Sungyu Yang, Goya Choi, Joong-Sun Kim, Inkyu Park","doi":"10.3390/ph18091418","DOIUrl":"10.3390/ph18091418","url":null,"abstract":"<p><p><b>Background/Objectives</b>: Dipsaci Radix (<i>Dipsacus asper</i>) and Phlomidis Radix (<i>Phlomoides umbrosa</i>) are both traditional medicines used in Korea and China for various bone-associated diseases. However, the two are misused due to similarities in name and appearance. Additionally, <i>D. japonicus</i> root frequently contaminates Dipsaci Radix in Korean herbal markets. <b>Methods</b>: We examined morphological plant traits and performed a DNA barcoding analysis using ITS2 and <i>matK</i> sequences to differentiate between these three species. The effects of root extracts on bone resorption and osteoclast differentiation, measured as tartrate-resistant acid phosphatase (TRAP)-positive cell formation, were evaluated using mouse (5 weeks male ICR mice) bone marrow-derived macrophages. Cytotoxicity assays were conducted to assess extract safety. <b>Results</b>: <i>Phlomoides umbrosa</i> is easily distinguished by its verticillaster inflorescences and 2-labiate corollas. <i>Dipsacus asper</i> and <i>D. japonicus</i>, which share globose inflorescences, are distinguishable by flower color and leaf lobation. The ITS2 and <i>matK</i> sequences clearly differentiated the three species, with haplotype analysis supporting their genetic distinctiveness, enabling robust species discrimination. All three extracts decreased osteoclastic bone resorption and inhibited TRAP-positive cell formations in a dose-dependent manner. Only the <i>D. japonicus</i> extract demonstrated toxicity. <b>Conclusions</b>: This integrative study provides the current scientific names of the original species and proposes their use in the Korean Herbal Pharmacopoeia. Moreover, a reasonable molecular method for authenticating medicinal materials is suggested. <i>Dipsacus japonicus</i> shows promise as an additional origin species in the Korean Pharmacopoeia. However, processing methods that reduce toxicity must be discovered.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":"18 9","pages":""},"PeriodicalIF":4.8,"publicationDate":"2025-09-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12472938/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145177318","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Biosynthesized Silver Nanoparticles and Their Antidiabetic Potential.","authors":"Angélica Sofía González-Garibay, Omar Ricardo Torres-González, Iván Moisés Sánchez-Hernández, Eduardo Padilla-Camberos","doi":"10.3390/ph18091412","DOIUrl":"10.3390/ph18091412","url":null,"abstract":"<p><p><b>Background/Objectives</b>: Recent advances in nanotechnology have enabled the use of biosynthesized silver nanoparticles (AgNPs) in healthcare, including the management of diabetes mellitus, a metabolic disorder characterized by impaired glucose homeostasis. AgNPs have shown promising effects on enzymes, insulin signaling, gut hormones, and in vivo models. Despite the availability of oral treatments, challenges persist, prompting interest in novel therapies such as AgNPs, which are currently under investigation in various in vitro and in vivo studies. <b>Methods</b>: This narrative review was conducted through a PubMed search using the terms \"antidiabetic + activity + AgNPs\" in April 2025. Relevant articles published in English were selected and analyzed, with emphasis on studies employing biosynthesized AgNPs from plants in in vitro and in vivo models. Information was extracted regarding the experimental approaches used to evaluate antidiabetic activity, the plant sources employed, nanoparticle characteristics, concentrations tested, and corresponding outcomes. <b>Results</b>: The biosynthesis of AgNPs employs bioactive compounds from plants, making it an environmentally friendly green synthesis method. Plant extracts are the most common biomaterial for AgNPs biosynthesis. Most of the in vitro studies evaluated the inhibitory effect of AgNPs on α-glucosidase or α-amylase; meanwhile, in animal studies, the main parameter evaluated is blood glucose level. <b>Conclusions</b>: The antidiabetic potential of AgNPs is becoming increasingly evident as ongoing research continues to explore their effects through both in vitro and in vivo studies. In this review, the current state of research regarding the potential use of AgNPs for diabetes management and treatment is presented, highlighting recent findings and discussing future perspectives in the field.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":"18 9","pages":""},"PeriodicalIF":4.8,"publicationDate":"2025-09-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12472463/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145177424","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}