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Medicinal food plants of Sabah (Eastern Malaysia): a source of potential natural products and nutraceuticals for the fight against cancer. 沙巴(马来西亚东部)的药用食品植物:抗癌的潜在天然产品和营养药品的来源。
IF 6 3区 医学
Pharmaceutical Biology Pub Date : 2026-12-01 Epub Date: 2026-05-07 DOI: 10.1080/13880209.2026.2663269
Carynn Tanbuda, Mazdida Sulaiman, Pauline Yong Pau Lin, Fiffy Hasnidah Saikim, Nor Azizun Ruzdi, Mogana Rajagopal, Nicholas Pang Tze Ping, Nor Hayati Abdullah, Jhonnel Villegas, Sanen Marshall, Mukesh Singh Sikarwar, Veeranoot Nissapatorn, Prapairat Seephonkai, Marcelo Iriti, Mark S Butler, Christophe Wiart
{"title":"Medicinal food plants of Sabah (Eastern Malaysia): a source of potential natural products and nutraceuticals for the fight against cancer.","authors":"Carynn Tanbuda, Mazdida Sulaiman, Pauline Yong Pau Lin, Fiffy Hasnidah Saikim, Nor Azizun Ruzdi, Mogana Rajagopal, Nicholas Pang Tze Ping, Nor Hayati Abdullah, Jhonnel Villegas, Sanen Marshall, Mukesh Singh Sikarwar, Veeranoot Nissapatorn, Prapairat Seephonkai, Marcelo Iriti, Mark S Butler, Christophe Wiart","doi":"10.1080/13880209.2026.2663269","DOIUrl":"10.1080/13880209.2026.2663269","url":null,"abstract":"<p><strong>Context: </strong>The pharmaceutical and nutraceutical industries are seeking structurally and pharmacologically novel anticancer molecules, as well as onco-protective nutraceuticals. One approach to achieving this goal is to study traditional pharmacopoeias, particularly those from regions where cancers are less common. Certain ethnic groups in Sabah (East Malaysia) appear to have a low incidence of cancer, and the study of their pharmacopeia could lead to the discovery of original anticancer molecules or nutraceuticals.</p><p><strong>Objectives: </strong>This review presents a selection of 64 plants used for medicinal food in Sabah their potential for clinical uses.</p><p><strong>Methods: </strong>The data for this focused narrative review were gathered from Google Scholar, PubMed, ScienceDirect, Web of Science, PubMed, the Internet Archive, and Google books. For each plant the search string included the binomial denomination and the words \"cytotoxic\" or \"tumors.\" of the binomial denomination of each plant and \"cytotoxic\" and \"tumors\" was employed. Each result was examined and articles that did not contain information relevant to the topic or coming from non-peer-reviewed journals were excluded.</p><p><strong>Results: </strong>Eight plant species, of which <i>Helminthostachys zeylanica</i> (L.) Hook., <i>Pycnarrhena tumefacta</i> Miers, <i>Myrmecodia platytyrea</i> Becc., and <i>Mangifera pajang</i> Kosterm, demonstrate activities <i>in vitro</i> and <i>in vivo</i>, which call for further research. Others constitute a source of cytotoxic natural products that warrant further investigation.</p><p><strong>Conclusion: </strong>There is currently a need to find oncopreventive nutraceuticals as well as original natural products for developing anticancer drugs. Such products could potentially be found among the medicinal and edible plants of Sabah. Further studies are needed.</p>","PeriodicalId":19942,"journal":{"name":"Pharmaceutical Biology","volume":"64 1","pages":"668-724"},"PeriodicalIF":6.0,"publicationDate":"2026-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC13159609/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147841265","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}
引用次数: 0
Sauchinone attenuates UVB-induced photoaging by suppressing oxidative stress and ferroptosis through activation of the Keap1-Nrf2 pathway in dermal fibroblasts. Sauchinone通过激活真皮成纤维细胞的Keap1-Nrf2通路,抑制氧化应激和铁下垂,从而减轻uvb诱导的光老化。
IF 6 3区 医学
Pharmaceutical Biology Pub Date : 2026-12-01 Epub Date: 2026-05-21 DOI: 10.1080/13880209.2026.2668138
Xinyi Zhang, Jing Wang, Ying Zhou, Chenye Shen, Minjia Yuan, Qi Li, Wei Li
{"title":"Sauchinone attenuates UVB-induced photoaging by suppressing oxidative stress and ferroptosis through activation of the Keap1-Nrf2 pathway in dermal fibroblasts.","authors":"Xinyi Zhang, Jing Wang, Ying Zhou, Chenye Shen, Minjia Yuan, Qi Li, Wei Li","doi":"10.1080/13880209.2026.2668138","DOIUrl":"10.1080/13880209.2026.2668138","url":null,"abstract":"<p><strong>Context: </strong>Skin photoaging induced by chronic ultraviolet B (UVB) exposure is primarily driven by oxidative stress. Emerging evidence suggests that ferroptosis contributes to UVB-induced skin damage. Sauchinone, a phenolic lignan derived from <i>Saururus chinensis</i>, possesses potent antioxidant and anti-inflammatory properties; however, its protective effects and underlying mechanisms against UVB-induced skin damage remain unclear.</p><p><strong>Objective: </strong>This study aimed to investigate the potential photoprotective effects and underlying mechanisms of sauchinone against UVB-induced skin damage in dermal fibroblasts.</p><p><strong>Materials and methods: </strong>UVB-induced HFFs were used as an <i>in vitro</i> model of photoaging. Cellular senescence, extracellular matrix (ECM) degradation, oxidative stress, and ferroptosis were evaluated using fluorescence staining, flow cytometry, qPCR, ELISA, and western blot analysis.</p><p><strong>Results: </strong>Sauchinone significantly attenuated cellular senescence and ECM degradation in UVB-induced HFFs, as evidenced by reduced SA-β-gal activity and decreased expression of p16 and p21, increased COL1A1 levels, and decreased MMP1 levels. Sauchinone also alleviated oxidative stress by reducing intracellular ROS and MDA levels while restoring GSH content and antioxidant enzyme activity. In addition, sauchinone attenuated ferroptosis-related features, including reduced lipid ROS and Fe<sup>2+</sup> accumulation, and normalized ACSL4, GPX4, FTH1, and SLC7A11 expression. Mechanistically, sauchinone was associated with activation of the Keap1-Nrf2 pathway, as evidenced by decreased Keap1 levels, enhanced nuclear translocation of Nrf2, and upregulation of downstream antioxidant genes. Importantly, pharmacological inhibition of Nrf2 using ML385 partially reversed the protective effects of sauchinone on oxidative stress, ferroptosis, cellular senescence, and ECM degradation.</p><p><strong>Discussion and conclusions: </strong>Our findings revealed that sauchinone protected fibroblasts against UVB-induced photoaging by inhibiting oxidative stress and ferroptosis, potentially through activation of the Keap1-Nrf2 pathway.</p>","PeriodicalId":19942,"journal":{"name":"Pharmaceutical Biology","volume":"64 1","pages":"764-782"},"PeriodicalIF":6.0,"publicationDate":"2026-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC13195707/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147982591","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}
引用次数: 0
Cardioprotective effect of hydroalcoholic extract stem bark of Xeroderris stuhlmannii on cadmium chloride-induced hypertension and its possible vasorelaxant mechanism on isolated aortic rats. 干皮水醇提取物对氯化镉致高血压大鼠的心脏保护作用及其可能的血管松弛机制。
IF 6 3区 医学
Pharmaceutical Biology Pub Date : 2026-12-01 Epub Date: 2026-04-15 DOI: 10.1080/13880209.2026.2651482
Jacquy Joyce Wanche Kojom, Willifred Dongmo Tekapi Tsopgni, Russelle Camelie Nguemnang Tchatchouang, Anatole Guy Blaise Azebaze, Timo D Stark, Alain Bertrand Dongmo
{"title":"Cardioprotective effect of hydroalcoholic extract stem bark of <i>Xeroderris stuhlmannii</i> on cadmium chloride-induced hypertension and its possible vasorelaxant mechanism on isolated aortic rats.","authors":"Jacquy Joyce Wanche Kojom, Willifred Dongmo Tekapi Tsopgni, Russelle Camelie Nguemnang Tchatchouang, Anatole Guy Blaise Azebaze, Timo D Stark, Alain Bertrand Dongmo","doi":"10.1080/13880209.2026.2651482","DOIUrl":"10.1080/13880209.2026.2651482","url":null,"abstract":"<p><strong>Background: </strong><i>Xeroderris stuhlmannii</i> is a medicinal plant, widely used in Cameroonian folk medicine to treat hypertension.</p><p><strong>Objective: </strong>This study aimed to investigate the beneficial effect of <i>X. stuhlmannii</i> in hypertensive rats and to explore the vasorelaxant mechanisms of its hydroalcoholic extract and to determine the compounds responsible of the activities.</p><p><strong>Materials and methods: </strong>Hydroalcoholic extract, fractions, subfractions and isolated compounds were screened for the antihypertensive activity in Wistar rat of either sex using a noninvasive method to record blood pressure (BP) and heart rate (HR). At the end of the treatment, the level of nitrite in the tissues and the histological analysis of the heart and aorta were determined. Vasorelaxant activity of the plant was carried out <i>in vitro</i>, on the contractile responses of aortic rings induced by phenylephrine (10<sup>-6</sup> M) or KCl (60 mM). Mechanisms involved vasorelaxation effect of <i>X. stuhlmannii</i> were assessed using various antagonists.</p><p><strong>Results: </strong>Treatment of Cadmium-hypertensive rats with extract significantly (<i>p</i> ˂ 0.001) reduced BP and HR, improved nitrite level, ameliorated heart and aorta alterations. Moreover, the hydroalcoholic extract, fractions, subfraction and odoratin-induced vasorelaxant effect. The preincubation with N<sub>G</sub>-nitro-L-arginine methyl ester, methylene blue and tetraethylammonium partially inhibited hydroalcoholic extract/fraction-induced relaxation. The extract completely inhibited the effects on CaCl<sub>2</sub>-induced contracted rings and reduced the contraction induced by phenylephrine in a Ca<sup>2+</sup>-free solution.</p><p><strong>Conclusion: </strong>These results support the traditional use of <i>X. stuhlmannii</i> in the treatment of hypertension. This effect may be due in part to the plant's vasorelaxant activity and the presence of compounds such as phenol in plant extracts.</p>","PeriodicalId":19942,"journal":{"name":"Pharmaceutical Biology","volume":"64 1","pages":"556-574"},"PeriodicalIF":6.0,"publicationDate":"2026-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC13084835/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147691617","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}
引用次数: 0
Ginger-based formulations for allergic rhinitis disease: a systematic review and meta-analysis of experimental studies in animals and humans. 基于姜的过敏性鼻炎配方:动物和人类实验研究的系统回顾和荟萃分析。
IF 6 3区 医学
Pharmaceutical Biology Pub Date : 2026-12-01 Epub Date: 2026-05-25 DOI: 10.1080/13880209.2026.2667560
Ratchanon Inpan, Tattiya Kantasa, Nutthiya Hanprasertpong, Mingkwan Na Takuathung, Nut Koonrungsesomboon
{"title":"Ginger-based formulations for allergic rhinitis disease: a systematic review and meta-analysis of experimental studies in animals and humans.","authors":"Ratchanon Inpan, Tattiya Kantasa, Nutthiya Hanprasertpong, Mingkwan Na Takuathung, Nut Koonrungsesomboon","doi":"10.1080/13880209.2026.2667560","DOIUrl":"10.1080/13880209.2026.2667560","url":null,"abstract":"<p><strong>Background: </strong>Allergic rhinitis is a chronic non-communicable disease that adversely affects respiratory health and quality of life. Ginger-based formulations, owing to their anti-inflammatory and immunomodulatory properties, may offer a promising alternative therapeutic option.</p><p><strong>Objective: </strong>To systematically review and meta-analyze evidence from animal studies and human randomized controlled trials assessing the efficacy of ginger-based formulations in allergic rhinitis.</p><p><strong>Methods: </strong>A systematic search of the Cochrane Library, Embase, PubMed, and Scopus (April 2025) identified studies comparing ginger-based formulations with control interventions. Outcomes included clinical symptoms and relevant biomarkers. Risk of bias was assessed using the SYRCLE tool for animal studies and RoB2 for human studies. Meta-analyses were conducted using random-effects models, with results expressed as standardized mean difference (SMD) and 95% confidence intervals (CIs).</p><p><strong>Results: </strong>Twenty-one studies (6 animal and 15 human studies) were included. In rodents, ginger-based formulations significantly reduced nasal rubbing (SMD = -1.99; 95%CI, -3.15 to -0.83), sneezing (SMD = -1.99; 95%CI, -2.78 to -1.20), and biomarkers (IL-4, IL-5, and OVA-specific IgE). In humans, ginger-based formulations significantly improved itching (SMD = -0.51; 95%CI, -0.79 to -0.24), runny nose (SMD = -0.59; 95%CI, -0.87 to -0.30), sneezing (SMD = -0.56; 95%CI, -0.75 to -0.37), total nasal symptom scores (SMD = -0.63; 95%CI, -1.00 to -0.26), and quality of life (SMD = -0.56; 95%CI, -0.87 to -0.24), and eosinophil levels.</p><p><strong>Conclusion: </strong>Ginger-based formulations improve symptoms and biomarkers of allergic rhinitis in both animal and human studies. As many interventions are multi-component, the observed effects are more appropriately attributed to the overall formulations rather than ginger alone. Further research is needed to explore mechanisms and clarify clinical applications.</p>","PeriodicalId":19942,"journal":{"name":"Pharmaceutical Biology","volume":"64 1","pages":"749-763"},"PeriodicalIF":6.0,"publicationDate":"2026-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC13202703/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148016781","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}
引用次数: 0
Profiling of euphane and tirucallane triterpenes from Euphorbia systyloides on antichagasic activity reveals antileukemia and immunomodulatory effects. 从大戟中提取的大戟烷和三聚丙烯三萜的抗肿瘤活性分析揭示了其抗白血病和免疫调节作用。
IF 6 3区 医学
Pharmaceutical Biology Pub Date : 2026-12-01 Epub Date: 2026-08-28 DOI: 10.1080/13880209.2026.2722390
Mohamed Abakar Maaz, Anita Barta, Dragana Markovic, Simon Singer, Jürg Gertsch, Róbert Berkecz, Peter Waweru Mwangi, Judit Hohmann, Andrea Vasas
{"title":"Profiling of euphane and tirucallane triterpenes from <i>Euphorbia systyloides</i> on antichagasic activity reveals antileukemia and immunomodulatory effects.","authors":"Mohamed Abakar Maaz, Anita Barta, Dragana Markovic, Simon Singer, Jürg Gertsch, Róbert Berkecz, Peter Waweru Mwangi, Judit Hohmann, Andrea Vasas","doi":"10.1080/13880209.2026.2722390","DOIUrl":"10.1080/13880209.2026.2722390","url":null,"abstract":"<p><strong>Background: </strong><i>Euphorbia</i> is one of the largest genera in the spurge family and is rich in bioactive secondary metabolites, especially triterpenoids and diterpenoids. <i>Euphorbia systyloides</i> Pax. (Euphorbiaceae) is native to tropical Africa, and its leaf decoction has traditionally been used to treat tapeworm infections. Its chemistry has not been previously investigated.</p><p><strong>Objective: </strong>This study aimed to investigate the terpenoid constituents of <i>E. systyloides</i> and evaluate the bioactivity of the compounds against <i>Trypanosoma cruzi</i> and tumor cells.</p><p><strong>Materials and methods: </strong>Compounds were isolated by multistep chromatography and structurally elucidated using HRMS and 1D/2D NMR. Biological activity was assessed against <i>T. cruzi</i> epimastigotes (XTT assay), and host cell infection and amastigote replication assays, while cytotoxicity was evaluated in HL60, U937, and PBMCs (MTT assay). Immunomodulatory effects were assessed by ELISA measurement of TNF-α and IL-10 in infected macrophages.</p><p><strong>Results: </strong>Six new euphane and tirucallane triterpenes and six known triterpenes were isolated. None were selectively active against <i>T. cruzi</i>. One ergostane triterpene exhibited nanomolar cytotoxicity against HL60 and U937 cell lines, with moderate toxicity toward PBMCs. Unexpectedly, kansenonol enhanced amastigote replication in host cells, likely through macrophage immunomodulation.</p><p><strong>Discussion and conclusions: </strong>Our results indicate that the ergostane triterpene represents an unexplored scaffold for antileukemic drug discovery. Based on an unexpected observation in a cellular <i>T. cruzi</i> trypomastigote infection assay, kansenonol was found to exert significant immunomodulatory effects <i>in vitro</i>. Overall, this study shows that triterpenoids from <i>E. systyloides</i> primarily exert cytotoxic and immunomodulatory effects rather than selective antiparasitic activity.</p>","PeriodicalId":19942,"journal":{"name":"Pharmaceutical Biology","volume":"64 1","pages":"949-966"},"PeriodicalIF":6.0,"publicationDate":"2026-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC13528120/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148841115","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}
引用次数: 0
Triptolide in renal disorders: dual roles of therapeutic potential and nephrotoxicity: a narrative review. 雷公藤甲素在肾脏疾病中的双重作用:治疗潜力和肾毒性:叙述性回顾。
IF 6 3区 医学
Pharmaceutical Biology Pub Date : 2026-12-01 Epub Date: 2026-01-21 DOI: 10.1080/13880209.2026.2616270
Lan Yan, Lulu Zhang, Xiaomeng Zhang, Changqi Shi, Qi Geng, Lin Lin, Ning Zhao, Li Li, Xiaojuan He, Yong Tan, Xinyu Ji, Cheng Lu
{"title":"Triptolide in renal disorders: dual roles of therapeutic potential and nephrotoxicity: a narrative review.","authors":"Lan Yan, Lulu Zhang, Xiaomeng Zhang, Changqi Shi, Qi Geng, Lin Lin, Ning Zhao, Li Li, Xiaojuan He, Yong Tan, Xinyu Ji, Cheng Lu","doi":"10.1080/13880209.2026.2616270","DOIUrl":"10.1080/13880209.2026.2616270","url":null,"abstract":"<p><strong>Background: </strong>Triptolide (TP), derived from <i>Tripterygium wilfordii</i>, exhibits anti-inflammatory, immunosuppressive, and antifibrotic properties with potential for treating renal diseases, but its clinical use is restricted by dose-dependent nephrotoxicity.</p><p><strong>Objective: </strong>The aim of this review is to comprehensively summarize the dual roles of TP, elucidate its therapeutic mechanisms and nephrotoxic pathways, and to explore strategies to mitigate its toxicity.</p><p><strong>Methods: </strong>A literature search was performed using the PubMed and Web of Science databases. The search covered publications from the earliest available date until November 2025. The key search terms included 'triptolide', 'renal', 'kidney' and their combinations.</p><p><strong>Results: </strong>TP exerts dose-dependent dual effects in renal models. Therapeutic doses (typically ≤200 μg/kg <i>in vivo</i>) demonstrate efficacy in modulating immune responses, protecting podocytes, promoting apoptosis in hyperproliferative cells and inhibiting renal fibrosis. Conversely, its nephrotoxicity manifests at supratherapeutic doses (often >400 μg/kg <i>in vivo</i>) through oxidative stress, inflammation, metabolic dysregulation, and direct damage to renal tubular cells. The therapeutic efficacy and toxicity of TP are critically contingent on both dose and temporal parameters.</p><p><strong>Conclusion: </strong>TP holds significant but challenging potential for renal therapy. Future research should define its therapeutic window and advance strategies such as structural analogs, targeted delivery systems, and combination therapies to effectively separate efficacy from toxicity for clinical translation.</p>","PeriodicalId":19942,"journal":{"name":"Pharmaceutical Biology","volume":"64 1","pages":"257-278"},"PeriodicalIF":6.0,"publicationDate":"2026-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12825603/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146011554","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}
引用次数: 0
Dual anti-pseudomonal and resistance-modulatory actions of Sida acuta (Malvaceae) via BamB-OprM targeting: insights from integrated metabolomics, computational, and in vitro analyses. 通过BamB-OprM靶向的双重抗假单胞菌和耐药调节作用:来自综合代谢组学、计算和体外分析的见解
IF 6 3区 医学
Pharmaceutical Biology Pub Date : 2026-12-01 Epub Date: 2026-01-08 DOI: 10.1080/13880209.2025.2611594
Armel Jackson Seukep, Helene Gueaba Mbuntcha, Cromwel Tepap Zemnou, Arnaud Fondjo Kouam, Victor Kuete, Mingquan Guo
{"title":"Dual anti-pseudomonal and resistance-modulatory actions of <i>Sida acuta</i> (Malvaceae) via BamB-OprM targeting: insights from integrated metabolomics, computational, and <i>in vitro</i> analyses.","authors":"Armel Jackson Seukep, Helene Gueaba Mbuntcha, Cromwel Tepap Zemnou, Arnaud Fondjo Kouam, Victor Kuete, Mingquan Guo","doi":"10.1080/13880209.2025.2611594","DOIUrl":"10.1080/13880209.2025.2611594","url":null,"abstract":"<p><strong>Context: </strong>The growing multidrug resistance (MDR) of <i>Pseudomonas aeruginosa</i> presents a pressing global health challenge and demands novel solutions. Medicinal plants offer a largely untapped reservoir of structurally diverse compounds with promising antibacterial and adjuvant potential.</p><p><strong>Objective: </strong>This study investigated <i>Sida acuta</i> Burm.f. (Malvaceae) as a reservoir of dual-target phytochemicals capable of modulating resistance.</p><p><strong>Materials and methods: </strong>An integrated workflow combining LC/Q-TOF-MS metabolomic profiling, molecular docking (MD), dynamics simulations (MDS), and microbiological assays was applied to the ethyl acetate fraction of the aerial parts (SAAP-EA).</p><p><strong>Results: </strong>Metabolomic analysis identified 35 compounds, including biochanin A (BCA), resveratrol (RSV), methyl gallate (MG), 3-hydroxycinnamic acid (3-HCA), and azelaic acid (AZA), with favorable drug-likeness. Their toxicity predictions indicated low risks of acute toxicity (LD<sub>50</sub> >900 mg/kg), mutagenicity, and carcinogenicity, but flagged a potential nephrotoxicity risk requiring further investigation. MD and MDS revealed stable RSV and BCA binding to both BamB (outer membrane biogenesis) and OprM (efflux), while 3-HCA and AZA preferentially targeted OprM with higher affinities than reference inhibitors. Hydrogen-bonding supported specificity and complex stability. Experimentally, SAAP-EA showed potent bactericidal activity against clinical MDR <i>P. aeruginosa</i> (MIC 32-256 µg/mL) and synergized with β-lactams, fluoroquinolones, and tetracyclines, achieving up to 64-fold MIC reductions at sub-inhibitory doses. The dual inhibition of membrane assembly and efflux likely underlies the observed resistance-breaking effects, facilitating intracellular antibiotic accumulation.</p><p><strong>Discussion and conclusions: </strong>These findings establish a mechanistic basis for translating ethnopharmacology into therapeutic strategies against MDR Gram-negative pathogens. Future work should prioritize <i>in vivo</i> validation and preclinical optimization of lead dual-target adjuvants.</p>","PeriodicalId":19942,"journal":{"name":"Pharmaceutical Biology","volume":"64 1","pages":"205-233"},"PeriodicalIF":6.0,"publicationDate":"2026-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12784639/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145918147","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}
引用次数: 0
Identification and characterization of five anti-mitotic sesquiterpene lactones from Arnica cordifolia. 山金车五种抗有丝分裂倍半萜内酯的鉴定与表征。
IF 4.8 3区 医学
Pharmaceutical Biology Pub Date : 2026-12-01 Epub Date: 2026-01-03 DOI: 10.1080/13880209.2025.2610026
Tanner C Lockwood, David E Williams, Layla Molina, Raymond J Andersen, Roy M Golsteyn
{"title":"Identification and characterization of five anti-mitotic sesquiterpene lactones from <i>Arnica cordifolia</i>.","authors":"Tanner C Lockwood, David E Williams, Layla Molina, Raymond J Andersen, Roy M Golsteyn","doi":"10.1080/13880209.2025.2610026","DOIUrl":"10.1080/13880209.2025.2610026","url":null,"abstract":"<p><strong>Context: </strong>Unique ecozones, such as those in Canada, play an important role in the production of distinct natural product chemicals that help plants survive highly variable abiotic conditions and herbivory. Extracts prepared from <i>Arnica cordifolia</i> Hook. (heartleaf arnica), a North American species related to the European medicinal plant <i>Arnica montana</i> L., induce mitotic arrest in human cancer cell lines with a mitotic spindle morphology distinct from other mitotic inhibitors isolated from prairie plant species.</p><p><strong>Objective: </strong>This study aimed to identify the anti-mitotic compound(s) of <i>A. cordifolia</i>.</p><p><strong>Materials and methods: </strong>The cytotoxic and anti-mitotic activities of <i>A. cordifolia</i> extracts and their active compounds on human cancer cells were characterized by MTT assays, light microscopy, flow cytometry, and immunofluorescence microscopy. The active compounds were isolated by bioassay-guided HPLC fractionation and identified by NMR.</p><p><strong>Results: </strong>Five anti-mitotic sesquiterpene lactones were isolated from <i>A. cordifolia</i>: three previously unidentified structures, and the known compounds aromaticin and pulchellin-2α-<i>O</i>-isovalerate. These compounds induced rounded cells positive for the mitotic marker phospho-histone H3 at concentrations of 5 µM, yet had distinct effects on mitotic spindle morphology. Furthermore, aromaticin treatment induced ubiquitin foci in cells, indicating that it may target the ubiquitin-proteasome pathway.</p><p><strong>Discussion and conclusion: </strong>This is the first report of mitotic inhibitors from <i>Arnica cordifolia</i>. Of these five compounds, three have previously undescribed chemical structures, whereas new anti-mitotic activities have been identified for aromaticin and pulchellin-2α-<i>O</i>-isovalerate. Differences in their biological activities suggest that they possess distinct cellular targets. These findings support continued exploration of Canadian botanical species as sources of structurally diverse bioactive compounds.</p>","PeriodicalId":19942,"journal":{"name":"Pharmaceutical Biology","volume":"64 1","pages":"185-204"},"PeriodicalIF":4.8,"publicationDate":"2026-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12777910/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145896554","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}
引用次数: 0
Assessment of sub-chronic toxicity and anti-aging effects of a solid self-microemulsifying drug delivery system of Kaempferia parviflora extract in a D-galactose-induced rat model. 小山奈提取物固体自微乳化给药系统对d -半乳糖诱导大鼠模型的亚慢性毒性和抗衰老作用的评价。
IF 4.8 3区 医学
Pharmaceutical Biology Pub Date : 2026-12-01 Epub Date: 2026-01-05 DOI: 10.1080/13880209.2025.2606956
Somsuda Somintara, Waraporn Sakaew, Sarunya Tuntiyasawasdikul, Peera Tabboon, Catheleeya Mekjaruskul, Jenjiralai Phanphak, Choowadee Pariwatthanakun, Bungorn Sripanidkulchai, Tawut Rudtanatip
{"title":"Assessment of sub-chronic toxicity and anti-aging effects of a solid self-microemulsifying drug delivery system of <i>Kaempferia parviflora</i> extract in a D-galactose-induced rat model.","authors":"Somsuda Somintara, Waraporn Sakaew, Sarunya Tuntiyasawasdikul, Peera Tabboon, Catheleeya Mekjaruskul, Jenjiralai Phanphak, Choowadee Pariwatthanakun, Bungorn Sripanidkulchai, Tawut Rudtanatip","doi":"10.1080/13880209.2025.2606956","DOIUrl":"10.1080/13880209.2025.2606956","url":null,"abstract":"<p><strong>Context: </strong>The pharmacological effects of <i>Kaempferia parviflora</i> have been extensively documented. A solid self-microemulsifying drug delivery system (SMEDDS) has been developed to address limitations such as poor water solubility and low bioavailability.</p><p><strong>Objective: </strong>This study evaluated the safety and anti-aging efficacy of the solid SMEDDS containing <i>K. parviflora</i> extract (KPS-SMEDDS) in rats.</p><p><strong>Materials and methods: </strong>A sub-chronic toxicity study was performed to assess the safety of KPS-SMEDDS. Healthy rats (<i>n</i> = 10/group) received oral doses of 125, 250, or 500 mg/kg body weight daily for 90 days. Clinical signs, body weight, hematological and biochemical parameters, and major organ histopathology were evaluated. Separately, the anti-aging effects of KPS-SMEDDS were investigated in a different cohort of rats (<i>n</i> = 9/group) with D-galactose-induced aging. Rats received intraperitoneal D-galactose (50 mg/kg/day) and oral KPS-SMEDDS at the same doses for 60 days. Oxidative stress markers, hormone levels, histopathology, and the expression of proteins related to aging, apoptosis, and inflammation were assessed.</p><p><strong>Results: </strong>No significant changes were observed in clinical signs, body weight, organ weights, hematological or biochemical parameters, or histopathology in KPS-SMEDDS-treated rats, indicating its safety. KPS-SMEDDS treatment significantly improved testicular weight, reduced malondialdehyde levels, normalized hormone levels, and restored testicular structure in rats with D-galactose-induced aging. Additionally, it upregulated SIRT-1 and Bcl-2, downregulated SA-β-gal, p53, and caspase-3, and modulated inflammatory cytokines (TNF-α, IL-6, and IL-10).</p><p><strong>Discussion and conclusion: </strong>KPS-SMEDDS was well-tolerated in rats and exerted protective effects against D-galactose-induced aging. These findings support its potential as a safe, natural anti-aging agent and highlight the value of formulation enhancement in traditional herbal medicine.</p>","PeriodicalId":19942,"journal":{"name":"Pharmaceutical Biology","volume":"64 1","pages":"143-167"},"PeriodicalIF":4.8,"publicationDate":"2026-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12777754/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145900876","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}
引用次数: 0
Graveoumarins A-C: chiral resolution, absolute configuration, and anticoagulant/anti-inflammatory activities of 3'-methyl-3'-butenyl coumarins from ruta graveolens L. 丁香香豆素A-C:丁香香豆素3′-甲基-3′-丁烯基的手性拆分、绝对构型和抗凝/抗炎活性。
IF 4.8 3区 医学
Pharmaceutical Biology Pub Date : 2026-12-01 Epub Date: 2025-12-13 DOI: 10.1080/13880209.2025.2599599
Zhihao Wu, Xiaolin Liao, Yuxin Wang, Jian Yin, Xu Feng, Lingfei Tong, Hao Huang, Yueping Jiang, Xiongjun Hou
{"title":"Graveoumarins A-C: chiral resolution, absolute configuration, and anticoagulant/anti-inflammatory activities of 3'-methyl-3'-butenyl coumarins from <i>ruta graveolens</i> L.","authors":"Zhihao Wu, Xiaolin Liao, Yuxin Wang, Jian Yin, Xu Feng, Lingfei Tong, Hao Huang, Yueping Jiang, Xiongjun Hou","doi":"10.1080/13880209.2025.2599599","DOIUrl":"10.1080/13880209.2025.2599599","url":null,"abstract":"<p><strong>Context: </strong>Several coumarins have been isolated from <i>Ruta graveolens</i> L., but the chirality of many remains uncharacterized or their absolute configurations unresolved.</p><p><strong>Objective: </strong>This study aimed to comprehensively separate and characterize the chirality of 3'-methyl-3'-butenylcoumarins from <i>R. graveolens</i> extracts, determine their absolute configurations, and evaluate their anticoagulant and anti-inflammatory activities.</p><p><strong>Materials and methods: </strong>Comprehensive chromatographic separation and chiral HPLC analysis were employed on the <i>R. graveolens</i> extract. The structures of isolated compounds were elucidated using extensive spectroscopic data analysis (HR-ESI-MS, NMR) and by comparing experimental circular dichroism (CD) spectra with calculated electronic circular dichroism (ECD) spectra. The anticoagulant and anti-inflammatory (specifically inhibition of nitric oxide (NO) production in lipopolysaccharide (LPS)-induced RAW 264.7 macrophages) activities of the isolated compounds were evaluated.</p><p><strong>Results: </strong>The study led to the isolation of two pairs of enantiomeric 3'-methyl-3'-butenylcoumarins, present in both equivalent and inequivalent ratios. This included two previously undescribed chiral 3'-methyl-3'-butenylcoumarins with specific absolute configurations [(+)-2'<i>R</i>-<b>2</b> and (-)-2'<i>S</i>-<b>3</b>] and one undescribed achiral 3'-methyl-3'-butenylcoumarin (<b>1</b>). Among the tested compounds, only the racemic mixture (±)-<b>3</b> exhibited moderate inhibition of NO production in the anti-inflammatory assay. No significant anticoagulant activity was reported for the compounds.</p><p><strong>Conclusions: </strong>This study successfully characterized the chirality and determined the absolute configurations of specific 3'-methyl-3'-butenylcoumarins from <i>R. graveolens</i>, including the discovery of three new compounds. While most isolated compounds lacked significant anticoagulant or anti-inflammatory activity in the tested models, racemic (±)-<b>3</b> showed moderate anti-inflammatory potential by inhibiting NO production. These findings provide new insights for the future development and utilization of coumarins from <i>R. graveolens</i>.</p>","PeriodicalId":19942,"journal":{"name":"Pharmaceutical Biology","volume":"64 1","pages":"17-26"},"PeriodicalIF":4.8,"publicationDate":"2026-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12704130/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145743325","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}
引用次数: 0
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