Fitoterapia最新文献

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Zanthoxylum alkylamides improves hepatic glucose metabolism by regulating gut microbiota in STZ-induced T2DM rats 花青素烷基酰胺通过调节stz诱导的T2DM大鼠肠道微生物群改善肝脏糖代谢
IF 2.5 3区 医学
Fitoterapia Pub Date : 2025-05-15 DOI: 10.1016/j.fitote.2025.106623
Xiaowei Peng , Bing Yang , Xunyu Wei , Lu Wang , Jianquan Kan
{"title":"Zanthoxylum alkylamides improves hepatic glucose metabolism by regulating gut microbiota in STZ-induced T2DM rats","authors":"Xiaowei Peng ,&nbsp;Bing Yang ,&nbsp;Xunyu Wei ,&nbsp;Lu Wang ,&nbsp;Jianquan Kan","doi":"10.1016/j.fitote.2025.106623","DOIUrl":"10.1016/j.fitote.2025.106623","url":null,"abstract":"<div><div>The observed beneficial impact of <em>Zanthoxylum</em> alkylamides (ZA) in addressing Type 2 diabetes mellitus (T2DM) suggests a potential association with short-chain fatty acids (SCFAs) and gut microbial composition. This study systematically investigated the influence of ZA on the organ index, c-peptide and lipid levels, gut microbiota composition, SCFAs production, and hepatic glucose metabolism in T2DM rats. The results indicate the success of ZA in treating T2DM rats characterized by hepatomegaly, nephromegaly, elevated blood lipids, and suppressed c-peptide levels. Following ZA intervention, the capacity of T2DM rats to produce SCFAs was not only restored but exceeded normal levels. Additionally, there was an augmentation in gut bacteria diversity, with a heightened abundance of <em>Proteobacteria</em> and an elevated <em>Firmicutes</em>/<em>Bacteroidetes</em> ratio. Conversely, a reduction in <em>Actinobacteria</em> abundance was noted. Importantly, ZA demonstrated the ability to regulate insulin activity and alleviate T2DM by activating the PI3K/Akt/mTOR signaling pathway in the liver of rats. In summary, our research reveals promising avenues for managing T2DM, encompassing diagnostic, therapeutic, monitoring, and drug discovery methodologies.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"184 ","pages":"Article 106623"},"PeriodicalIF":2.5,"publicationDate":"2025-05-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144072769","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Combined network pharmacology and metabolomics reveal that Rubia cordifolia L. ameliorates exhaustive exercise-induced myocardial injury in rats via the BCAA degradation pathway. 网络药理学和代谢组学联合研究表明,芦花可通过BCAA降解途径改善运动性大鼠心肌损伤。
IF 2.5 3区 医学
Fitoterapia Pub Date : 2025-05-14 DOI: 10.1016/j.fitote.2025.106617
Xueyu Niu, Jia Deng, Yan Zhao, Yi Zhang, Ziqi Wang, Li Zhang, Kan Wang
{"title":"Combined network pharmacology and metabolomics reveal that Rubia cordifolia L. ameliorates exhaustive exercise-induced myocardial injury in rats via the BCAA degradation pathway.","authors":"Xueyu Niu, Jia Deng, Yan Zhao, Yi Zhang, Ziqi Wang, Li Zhang, Kan Wang","doi":"10.1016/j.fitote.2025.106617","DOIUrl":"https://doi.org/10.1016/j.fitote.2025.106617","url":null,"abstract":"<p><p>Rubia cordifolia L. (RCL) is a widely used medicinal and food-related product with a long history. It exhibits anti-inflammatory and antioxidant properties and prevents apoptosis. While there is growing evidence that exhausted exercise (EE) might cause cardiac damage, RCL has been shown to provide cardioprotective effects. The effects and mechanisms of RCL on exercise-induced myocardial injury remain unclear. In this study, we tested the RCL extract using a rat model of exhausted swimming. We evaluated the therapeutic effect of RCL on exercise-induced myocardial damage using PCR, ELISA, hematoxylin-eosin (H&E) staining, DHE staining, and other methods. UPLC-Q-TOF-MS was employed to identify the components of the RCL extract and its blood-entry components, and network pharmacology was constructed. LC-MS was utilized to investigate left ventricular metabolomics. The two were combined in order to predict the possible metabolic pathways regulated by RCL. Finally, the targets of the metabolic pathway were verified using molecular docking and western blot analysis. The findings suggest that rubioncolin B, 4-hydroxy-2-carbexyanthraquinone, and 9-Oxo-9H-xanthene-4-carboxylic acid may be the primary active compounds of RCL. RCL promotes the degradation pathway of branched-chain amino acids (BCAA), including valine, leucine, and isoleucine, regulates the proteins BCAT2 and BCKDK, reduces pathological injuries, inflammation, oxidative stress, and collagen deposition, and mitigates the effects of exhaustion-induced myocardial injuries by influencing the key target AKR1C1 and the metabolite L-Valine. This study provides a foundation for the development of RCL as a sports supplement to alleviate EE-induced myocardial injury.</p>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":" ","pages":"106617"},"PeriodicalIF":2.5,"publicationDate":"2025-05-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144086037","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Integrating serum pharmacochemistry and network pharmacology to explore the potential mechanisms of Xianshen formula in the prevention of exercise-induced fatigue. 结合血清药物化学和网络药理学,探讨仙参方预防运动性疲劳的可能机制。
IF 2.5 3区 医学
Fitoterapia Pub Date : 2025-05-13 DOI: 10.1016/j.fitote.2025.106621
Qiwen Xuan, Yi Ruan, Zifei Yin, Wei Gu, Changquan Ling
{"title":"Integrating serum pharmacochemistry and network pharmacology to explore the potential mechanisms of Xianshen formula in the prevention of exercise-induced fatigue.","authors":"Qiwen Xuan, Yi Ruan, Zifei Yin, Wei Gu, Changquan Ling","doi":"10.1016/j.fitote.2025.106621","DOIUrl":"https://doi.org/10.1016/j.fitote.2025.106621","url":null,"abstract":"<p><strong>Objective: </strong>On the basis of exploring the efficacy of XSF, the material basis and mechanism of XSF for the prevention of exercise-induced fatigue were clarified by network pharmacology using blood-absorbed components as the research object.</p><p><strong>Methods: </strong>UPLC-Q-TOF/MS was used to identify the blood components of XSF. On this basis, the target prediction of the blood-entering components was obtained from the Swiss Target Prediction and SuperPred database, and the target related to exercise-induced fatigue was acquired from OMIM, GeneCards, and other disease databases. The network model of \" components- targets-diseases\" of XSF was established by Cytoscape software. The String data analysis platform was used to build the PPI network to filter out the primary targets. The DAVID database was used for gene ontology (GO) enrichment analysis and the Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway enrichment analysis of the key targets.</p><p><strong>Results: </strong>Administration of XSF increased swimming time, decreased BLA, BUN, and MDA levels, and elevated SOD levels in swimming exhausted rats and mice. A total of 60 in vitro active ingredients, 45 blood-entry prototype ingredients, and 41 blood-entry metabolized ingredients were identified. Out of 717 possible targets of action between medication components and exercise exhaustion, network pharmacology identified 176 nodes with a maximum value of TP53 (Degree = 81) according to PPI analysis. The key targets were involved in 96 KEGG pathways including the PI3K-Akt signaling pathway, MAPK signaling pathway, HIF-1 signaling pathway TNF signaling pathway, and 170 GO pathways. The top 10 targets in the \"component-target-pathway\" network of XSF against EIF were predicted to be NFKB1, PIK3R1, GRIN1, CACNA1B, SLC6A5, NTRK3, GRIA2, TRIM24, TOP2A, TLR4 and RORB, TLR4 and RORB.</p><p><strong>Conclusion: </strong>XSF is effective in the prevention of EIF and its potential pharmacological mechanisms may be related to the improvement of energy metabolism, regulation of inflammatory response, and regulation of oxidative stress.</p>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":" ","pages":"106621"},"PeriodicalIF":2.5,"publicationDate":"2025-05-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144076862","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Antiviral activity against HSV-1 of triterpene saponins from Anagallis arvensis is related tothe fusion-inhibitory activity of desglucoanagalloside B 穿山甲三萜皂苷对HSV-1的抗病毒活性与去糖穿山甲苷B的融合抑制活性有关
IF 2.5 3区 医学
Fitoterapia Pub Date : 2025-05-13 DOI: 10.1016/j.fitote.2025.106620
Nica Classen , Jandirk Sendker , Diana Ulrich , Michael Schöfbänker , Eike R. Hrincius , Stephan Ludwig , Alexander Weng , Matthias Melzig , Joachim Kühn , Andreas Hensel
{"title":"Antiviral activity against HSV-1 of triterpene saponins from Anagallis arvensis is related tothe fusion-inhibitory activity of desglucoanagalloside B","authors":"Nica Classen ,&nbsp;Jandirk Sendker ,&nbsp;Diana Ulrich ,&nbsp;Michael Schöfbänker ,&nbsp;Eike R. Hrincius ,&nbsp;Stephan Ludwig ,&nbsp;Alexander Weng ,&nbsp;Matthias Melzig ,&nbsp;Joachim Kühn ,&nbsp;Andreas Hensel","doi":"10.1016/j.fitote.2025.106620","DOIUrl":"10.1016/j.fitote.2025.106620","url":null,"abstract":"<div><div>The identification of antiviral natural products as new lead structures has become a major task in medical science. Especially saponins have gained high interest for their antiviral activity. Antiviral effects of the saponin-containing plant <em>Anagallis arvensis</em>, widely used in traditional medicine, have been described, while mode of action or detailed phytochemical and functional investigations are still missing. A saponin enriched extract (AAS) from the aerial material of <em>A. arvensis</em> was characterized in detail by LC-HRMS, indicating the presence of a complex mixture of triterpene saponins and flavonoid glycosides. Plaque assays with <em>Herpes simplex</em> virus 1 (HSV-1) on Vero cells indicated strong inhibition of viral spread after infection of the host cells, resulting in reduced plaque size. The strongest effect was achieved by treating host cells post infection, which points towards an interference with the viral post-entry step. Using a specific HSV-1 fusion assay, AAS was shown to inhibit HSV-1 glycoprotein-mediated cell fusion at &gt;2 μg/mL. Bioassay-guided fractionation of AAS yielded one active subfraction, which significantly reduced HSV-1 plaque size on Vero cells. The membrane-fusion inhibiting effect was correlated to the presence of desglucoanagalloside B <strong>9</strong>. Interestingly, this compound was also detected in relevant amounts in herbal preparations from traditional medicine, which again could rationalize the use of <em>A. arvensis</em> as antiviral remedy in folk medicine. Relevant antiviral activity against SARS-CoV-2 was not detected.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"184 ","pages":"Article 106620"},"PeriodicalIF":2.5,"publicationDate":"2025-05-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143946744","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Two sesquiterpenoids and a steroid produced by an endophytic fungus Aspergillus sp. YUD20004 and their bioactivity. 内生真菌Aspergillus sp. YUD20004产生的两种倍半萜类和一种类固醇及其生物活性。
IF 2.5 3区 医学
Fitoterapia Pub Date : 2025-05-12 DOI: 10.1016/j.fitote.2025.106619
Dan-Dan Xia, Jing-Xin Chen, Fei Xie, Yan Geng, Hai-Xia Dong, Hao Zhou, Zhong-Tao Ding
{"title":"Two sesquiterpenoids and a steroid produced by an endophytic fungus Aspergillus sp. YUD20004 and their bioactivity.","authors":"Dan-Dan Xia, Jing-Xin Chen, Fei Xie, Yan Geng, Hai-Xia Dong, Hao Zhou, Zhong-Tao Ding","doi":"10.1016/j.fitote.2025.106619","DOIUrl":"https://doi.org/10.1016/j.fitote.2025.106619","url":null,"abstract":"<p><p>Two new sesquiterpenoids asperpenoids A-B (1-2) and one new ergostane-type steroid aspergteroid (3) were isolated from the fungus Aspergillus sp. YUD20004 which was derived from the tuber of Zingiber officinale Roscoe. Their structures and absolute configurations were elucidated by comprehensive spectroscopic analyses, electronic circular dichroism (ECD) spectra and consideration of the biogenetic origins. Especially, asperpenoid A was featured as a rare spiro[6-oxabicyclo[3.2.1]octane-2,2'-oxirane] 5/6/3 tricyclic skeleton. In vitro cytotoxic activity assays, aspergteroid (3) exhibited significant cytotoxic activities against five human cancer cell lines (SMMC-7721, HL-60, A549, SW480 and MDA-MB-231) with IC<sub>50</sub> values ranging from 0.40 to 34.24 μM. Most significantly, compound 3 reduced the viability of SMMC-7721 cells in a concentration-dependent manner with an IC<sub>50</sub> value of 0.40 μM.</p>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":" ","pages":"106619"},"PeriodicalIF":2.5,"publicationDate":"2025-05-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144076864","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Controlled fermentation of Arisaema cum bile with isolated Fungi strains and its antipyretic effects in a febrile mouse model 分离菌种对胆沙蒿的控制发酵及其对发热小鼠模型的解热作用
IF 2.5 3区 医学
Fitoterapia Pub Date : 2025-05-12 DOI: 10.1016/j.fitote.2025.106618
Ranqiao Jigu, Kongjie Zhang, Yi Li, Zhi Zhang, Xiaohong Jian, Zaixin Li
{"title":"Controlled fermentation of Arisaema cum bile with isolated Fungi strains and its antipyretic effects in a febrile mouse model","authors":"Ranqiao Jigu,&nbsp;Kongjie Zhang,&nbsp;Yi Li,&nbsp;Zhi Zhang,&nbsp;Xiaohong Jian,&nbsp;Zaixin Li","doi":"10.1016/j.fitote.2025.106618","DOIUrl":"10.1016/j.fitote.2025.106618","url":null,"abstract":"<div><div>Arisaema cum Bile (DNX, Dan Nanxing) is a traditional fermented Chinese medicine renowned for its antipyretic properties. Conventionally, DNX is produced through natural fermentation using indigenous microbial strains, which often results in an unstable microbial composition and susceptibility to contamination by harmful microorganisms. Additionally, inconsistencies in the fermentation process and outdated quality control methods further compromise the quality and safety of the final product. This study aimed to investigate the production of DNX using isolated fungal combinations under controlled conditions. Based on separation and high-throughput sequencing analyses, four dominant fungi were selected for restricted fermentation. When inoculated at a ratio of 1:1:2:2, the amylase activity of DNX reached its peak, with fermentation endpoints determined by both amylase activity and changes in calcium oxalate crystal structure. Metabolomic analysis revealed that among the top 30 compounds with the highest content, 24 exhibited consistent relative content changes between restricted fermentation and natural fermentation. In febrile mice, DNX produced by both fermentation methods demonstrated comparable antipyretic effects, significantly reducing body temperature and inflammatory cytokines (<em>p</em> &lt; 0.05), including IL-6 and TNF-α, to normal levels. Furthermore, inflammation-related signaling pathways, such as cAMP and PGE2 levels, were significantly downregulated following DNX treatment (<em>p</em> &lt; 0.01). These findings suggest that DNX produced through restricted fermentation exhibits therapeutic effects comparable to those achieved by natural fermentation. This study proposes a novel fermentation strategy for the industrial production of DNX, offering improved consistency and quality control.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"184 ","pages":"Article 106618"},"PeriodicalIF":2.5,"publicationDate":"2025-05-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143946745","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
FLEXA, a new herbal formulation, alleviates inflammation and cartilage degradation of osteoarthritis by inhibiting the activation of the MAPK/ NF-κB signaling pathways FLEXA是一种新型草药制剂,通过抑制MAPK/ NF-κB信号通路的激活,减轻骨关节炎的炎症和软骨降解。
IF 2.5 3区 医学
Fitoterapia Pub Date : 2025-05-11 DOI: 10.1016/j.fitote.2025.106590
Minwoo Song , You Yeon Choi , Seong Chul Jin , Hee Kyung Baek , Seungyob Yi , Eun Jung Kim , Woong Mo Yang
{"title":"FLEXA, a new herbal formulation, alleviates inflammation and cartilage degradation of osteoarthritis by inhibiting the activation of the MAPK/ NF-κB signaling pathways","authors":"Minwoo Song ,&nbsp;You Yeon Choi ,&nbsp;Seong Chul Jin ,&nbsp;Hee Kyung Baek ,&nbsp;Seungyob Yi ,&nbsp;Eun Jung Kim ,&nbsp;Woong Mo Yang","doi":"10.1016/j.fitote.2025.106590","DOIUrl":"10.1016/j.fitote.2025.106590","url":null,"abstract":"<div><h3>Background</h3><div>Osteoarthritis (OA) is a progressive musculoskeletal disorder marked by cartilage degradation and inflammation. FLEXA, a novel herbal formulation composed of <em>Ostericum koreanum</em> Maxim, <em>Cibotium barometz</em> J. Smith, and <em>Carthamus tinctorius</em> Linne, has traditionally been used to manage joint-related conditions. This study aimed to evaluate the therapeutic efficacy of FLEXA in an OA model by elucidating its molecular mechanisms and multi-target effects.</div></div><div><h3>Methods</h3><div>Network pharmacology analysis was performed to identify potential interactions between the active components of FLEXA and OA-related targets. Osteoarthritis was induced in rats via intra-articular injection of monosodium iodoacetate (MIA), followed by intramuscular administration of FLEXA at two doses (0.0094 and 0.094 mg/kg) twice weekly for four weeks. Cartilage integrity, proteoglycan content, bone mineral density, and inflammatory markers were assessed. Additionally, the effects of FLEXA on mitogen-activated protein kinase (MAPK) and nuclear factor-kappa B (NF-κB) pathways were evaluated in interleukin-1β-stimulated SW1353 chondrocytes.</div></div><div><h3>Results</h3><div>FLEXA improved cartilage integrity, increased proteoglycan levels, and enhanced bone mineral density in the femoral condyles of OA rats. Network pharmacology revealed that FLEXA modulated key targets associated with “Positive Regulation of Extracellular Matrix Assembly”. In SW1353 cells, FLEXA suppressed MAPK and NF-κB signaling, reducing pro-inflammatory cytokine production and extracellular matrix degradation.</div></div><div><h3>Conclusion</h3><div>These findings demonstrate that FLEXA exerts multi-target chondroprotective and anti-inflammatory effects, suggesting its potential as a complementary therapeutic option for OA management.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"184 ","pages":"Article 106590"},"PeriodicalIF":2.5,"publicationDate":"2025-05-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143980796","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Corrigendum to “Triterpenoids from Ganoderma cochlear against inflammation and renal fibrosis” [Fitoterapia 183 (2025) 106543] “灵芝三萜抗炎症和肾纤维化”的勘误表[Fitoterapia 183(2025) 106543]。
IF 2.5 3区 医学
Fitoterapia Pub Date : 2025-05-09 DOI: 10.1016/j.fitote.2025.106581
Jian-Biao Zhang , Sheng-Hong Li , Zhi-Yuan Li , Yong-Ming Yan , Yong-Xian Cheng
{"title":"Corrigendum to “Triterpenoids from Ganoderma cochlear against inflammation and renal fibrosis” [Fitoterapia 183 (2025) 106543]","authors":"Jian-Biao Zhang ,&nbsp;Sheng-Hong Li ,&nbsp;Zhi-Yuan Li ,&nbsp;Yong-Ming Yan ,&nbsp;Yong-Xian Cheng","doi":"10.1016/j.fitote.2025.106581","DOIUrl":"10.1016/j.fitote.2025.106581","url":null,"abstract":"","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"183 ","pages":"Article 106581"},"PeriodicalIF":2.5,"publicationDate":"2025-05-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143958242","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
New bis-norditerpene by biotransformation of favelines from Cnidoscolus quercifolius using Umbelopsis isabellina as biocatalyst 以深黄伞为生物催化剂,从槲皮刺槐中提取亚麻碱生物转化新的双北二萜
IF 2.5 3区 医学
Fitoterapia Pub Date : 2025-05-08 DOI: 10.1016/j.fitote.2025.106605
Sovannychloé Nai , Thomas Gaslonde , Julia Krystyańczuk , Séverine Amand , Laurent Picot , Carlos Arthur Gouveia Veloso , Didier Buisson , Marie-Christine Lallemand , Raimundo Gonçalves de Oliveira Junior
{"title":"New bis-norditerpene by biotransformation of favelines from Cnidoscolus quercifolius using Umbelopsis isabellina as biocatalyst","authors":"Sovannychloé Nai ,&nbsp;Thomas Gaslonde ,&nbsp;Julia Krystyańczuk ,&nbsp;Séverine Amand ,&nbsp;Laurent Picot ,&nbsp;Carlos Arthur Gouveia Veloso ,&nbsp;Didier Buisson ,&nbsp;Marie-Christine Lallemand ,&nbsp;Raimundo Gonçalves de Oliveira Junior","doi":"10.1016/j.fitote.2025.106605","DOIUrl":"10.1016/j.fitote.2025.106605","url":null,"abstract":"<div><div>Favelines, tricyclic benzylcycloheptene diterpenes predominantly found in <em>Cnidoscolus quercifolius</em>, have demonstrated significant cytotoxic activity against human cancer cell lines, including melanoma. In this study, we employed a combinatorial approach to screen microbial strains for biotransformation, focusing on regioselective oxidation of the cyclohexyl ring in the faveline core structure. This strategy, applied directly to the crude plant extract, enabled the rapid identification of <em>Umbelopsis isabellina</em> as the active strain. Subsequent preparative biotransformation yielded a novel <em>bis</em>-norditerpene, 14-hydroxy-isofavelol (<strong>3</strong>). The new compound exhibited moderate cytotoxic activity (IC₅₀ = 68.8 μM) against chemoresistant human melanoma A2058 cells, which are resistant to dacarbazine but sensitive to vemurafenib. Compound <strong>3</strong> enhanced the cytotoxic effect of vemurafenib, reducing its IC₅₀ from 24.8 to 9.63 μM. This work demonstrates the utility of microbial biotransformation for generating new bioactive natural product derivatives and highlights the potential of 14-hydroxy-isofavelol as a chemosensitizing agent in melanoma therapy.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"184 ","pages":"Article 106605"},"PeriodicalIF":2.5,"publicationDate":"2025-05-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143928997","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Study on the pharmacokinetics and brain tissue distribution of eight anti-inflammatory active components in normal and neuroinflammatory rats orally administered with extract of Tinospora sinensis (Lour.) Merr. using the UPLC-MS/MS method. 中药天螺提取物对正常大鼠和神经炎大鼠8种抗炎活性成分的药动学及脑组织分布研究稳定。采用UPLC-MS/MS法。
IF 2.5 3区 医学
Fitoterapia Pub Date : 2025-05-08 DOI: 10.1016/j.fitote.2025.106564
Liping Chen, Longhui Lu, Guoliang Xu, Zhihui Jiang, Qiujin Guo, Feijun Huang, Wenyan Yan, Hang Zhang, Yi Wu, Yongyan Xie, Liping Huang, Shuaikang Wang
{"title":"Study on the pharmacokinetics and brain tissue distribution of eight anti-inflammatory active components in normal and neuroinflammatory rats orally administered with extract of Tinospora sinensis (Lour.) Merr. using the UPLC-MS/MS method.","authors":"Liping Chen, Longhui Lu, Guoliang Xu, Zhihui Jiang, Qiujin Guo, Feijun Huang, Wenyan Yan, Hang Zhang, Yi Wu, Yongyan Xie, Liping Huang, Shuaikang Wang","doi":"10.1016/j.fitote.2025.106564","DOIUrl":"https://doi.org/10.1016/j.fitote.2025.106564","url":null,"abstract":"<p><p>Tinospora sinensis (Lour.) Merr. (Tinospora sinensis) is a traditional Chinese medicine commonly used by Tibetan people in China to prevent and treat diseases such as senile dementia, neuroinflammatory, and rheumatoid arthritis. However, the pharmacokinetic characteristics and tissue distribution of Tinospora sinensis active components in vivo, especially the distribution of brain regions, are unclear. Herein, a stable and accurate ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method was developed and validated to compare the pharmacokinetic patterns and differences in brain tissue distribution of eight anti-inflammatory active components in normal and neuroinflammatory rats after oral administration of extracts from Tinospora sinensis. ACE Excel 3 C18-AR (100 × 2.1 mm, 1.7 μm) column was used for gradient elution with 0.1 % formic acid water (A) and acetonitrile (B), rifampicin as an internal standard, electrospray ionization (ESI) positive and negative ion mode scanning, multiple reaction monitoring (MRM) determination, and DAS 2.0 software analysis. The UPLC-MS/MS method established through verification is accurate and reliable, and the methodology can meet the quantitative requirements. The pharmacokinetic results showed differences in the pharmacokinetic process and brain tissue distribution between normal rats and rats with neuroinflammation. All eight anti-inflammatory active components can be rapidly absorbed into the bloodstream (Tmax ≤ 2 h), but the plasma metabolism rate of rats with neuroinflammation is faster and the brain content is lower. Neuroinflammation has a significant impact on the in vivo process of oral administration of Tinospora sinensis in rats. The study provides experimental evidence for the quality control and clinical application of Tinospora sinensis.</p>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":" ","pages":"106564"},"PeriodicalIF":2.5,"publicationDate":"2025-05-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144004645","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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