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The anti-inflammatory mechanism of a new skeleton alkaloid isolated from Portulaca oleracea L. 马齿苋骨架生物碱的抗炎机制研究。
IF 2.5 3区 医学
Fitoterapia Pub Date : 2025-07-26 DOI: 10.1016/j.fitote.2025.106760
Xiaoqian Zhang , Yingdai Zhao , Jinpeng Liu , Hongzhe Zhang , Junjie Yao , Jing Liu , Yujuan Niu , Xixiang Ying
{"title":"The anti-inflammatory mechanism of a new skeleton alkaloid isolated from Portulaca oleracea L.","authors":"Xiaoqian Zhang ,&nbsp;Yingdai Zhao ,&nbsp;Jinpeng Liu ,&nbsp;Hongzhe Zhang ,&nbsp;Junjie Yao ,&nbsp;Jing Liu ,&nbsp;Yujuan Niu ,&nbsp;Xixiang Ying","doi":"10.1016/j.fitote.2025.106760","DOIUrl":"10.1016/j.fitote.2025.106760","url":null,"abstract":"<div><div>A new skeleton alkaloid was isolated from <em>Portulaca oleracea</em> L., which was identified as ethyl (2<em>Z</em>,4<em>E</em>,6<em>E</em>)-3-amino-7-(4-amino-6-ethyl-3-glycyl-5-methylpyridin-2-yl)-2-methylocta-2,4,6-trienoate, trivial named, olerapyridin and the structure was clarified through IR, UV, 1D and 2D NMR as well as UHPLC-ESI-Q-TOF/MS methods. Moreover, the bioactivities of anti-inflammation of the compound were investigated via testing RAW 264.7 macrophage cell stimulated by lipopolysaccharide. The results showed that olerapyridin at 5 μ<em>M</em> remarkably downregulated the levels of inflammatory mediators, including IL-1<em>β</em>, the proteins expression levels of iNOS and the mRNA expression levels of COX-2, Additionally, at 15 μ<em>M</em>, olerapyridin effectively reduced the levels of NO and TNF-<em>a</em>, as well as the proteins expression levels of COX-2 and mRNA expression levels of iNOS.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"185 ","pages":"Article 106760"},"PeriodicalIF":2.5,"publicationDate":"2025-07-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144714530","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
Promorphinan and bisaporphine alkaloids from Alseodaphne peduncularis 山茱萸中原吗啡苷和双吗啡碱类生物碱
IF 2.5 3区 医学
Fitoterapia Pub Date : 2025-07-23 DOI: 10.1016/j.fitote.2025.106745
Sayed Mohammadhossein Modaresi , Premanand Krishnan , Wei-Meng Lim , Ling-Wei Hii , Kooi-Yeong Khaw , Chee-Onn Leong , Donald K.F. Chen , Brian K. Kennedy , Shou-Ping Guan , Jan Gruber , Ee-Soo Lee , Yi-Sheng Tan , Soon-Kit Wong , Yun-Yee Low , Kien-Thai Yong , Kuan-Hon Lim
{"title":"Promorphinan and bisaporphine alkaloids from Alseodaphne peduncularis","authors":"Sayed Mohammadhossein Modaresi ,&nbsp;Premanand Krishnan ,&nbsp;Wei-Meng Lim ,&nbsp;Ling-Wei Hii ,&nbsp;Kooi-Yeong Khaw ,&nbsp;Chee-Onn Leong ,&nbsp;Donald K.F. Chen ,&nbsp;Brian K. Kennedy ,&nbsp;Shou-Ping Guan ,&nbsp;Jan Gruber ,&nbsp;Ee-Soo Lee ,&nbsp;Yi-Sheng Tan ,&nbsp;Soon-Kit Wong ,&nbsp;Yun-Yee Low ,&nbsp;Kien-Thai Yong ,&nbsp;Kuan-Hon Lim","doi":"10.1016/j.fitote.2025.106745","DOIUrl":"10.1016/j.fitote.2025.106745","url":null,"abstract":"<div><div>Five previously undescribed benzylisoquinoline alkaloids were isolated from the leaves and stem-bark of <em>Alseodaphne peduncularis</em>. Among these, alseodaphnine (<strong>1</strong>) was characterized as a tetracyclic rearranged promorphinan alkaloid. Alseodaphnilarines A, B, and C (<strong>2</strong>–<strong>4</strong>) were identified as promorphinan-amine conjugates, while alseodaphnidine (<strong>5</strong>) represents a bisaporphine alkaloid. Additionally, (−)-9,10-dihydrocepharatine A (<strong>6</strong>) was isolated from a natural source for the first time, although it was previously reported as a byproduct from a total synthesis to cepharatine A. Twelve other known benzylisoquinoline alkaloids (<strong>7</strong>–<strong>18</strong>) were also identified. The chemical structures and absolute configurations of compounds <strong>1</strong>–<strong>5</strong> were elucidated through comprehensive spectroscopic analyses. In vitro cytotoxic assays revealed that alkaloid <strong>14</strong> showed moderate anti-cancer activity against pancreatic and breast cancer cell lines (IC<sub>50</sub> 12.6–21.7 μM). Compound <strong>5</strong> demonstrated selective butyrylcholinesterase inhibition (IC<sub>50</sub> 21.2 μM), with no activity against acetylcholinesterase. Furthermore, alkaloids <strong>1</strong>, <strong>7</strong>–<strong>9</strong>, <strong>14</strong>, and <strong>17</strong> significantly extended the lifespan of <em>Caenorhabditis elegans</em> by up to 12 % compared to the control group.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"185 ","pages":"Article 106745"},"PeriodicalIF":2.5,"publicationDate":"2025-07-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144703831","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
Efficacy of Chi-Huang cream as an anti-inflammatory and anti-pruritic agent in treating chronic pruritus 赤黄膏抗炎止痒治疗慢性瘙痒症的疗效观察
IF 2.5 3区 医学
Fitoterapia Pub Date : 2025-07-22 DOI: 10.1016/j.fitote.2025.106751
Wei-Hsin Wang , Tong Xie , Deng-Shan Shiau , Sherrie Xie , Di Zhang , Jiahao Lin
{"title":"Efficacy of Chi-Huang cream as an anti-inflammatory and anti-pruritic agent in treating chronic pruritus","authors":"Wei-Hsin Wang ,&nbsp;Tong Xie ,&nbsp;Deng-Shan Shiau ,&nbsp;Sherrie Xie ,&nbsp;Di Zhang ,&nbsp;Jiahao Lin","doi":"10.1016/j.fitote.2025.106751","DOIUrl":"10.1016/j.fitote.2025.106751","url":null,"abstract":"<div><div>Pruritus is the main clinical symptom of skin diseases in animals and humans. Treatment outcomes from current conventional medicine are often unsatisfactory, since the same pruritus mediator may play multiple roles in different pruritus-associated diseases. Chi-Huang formula is the experiential traditional Chinese medicine formula for canine atopic dermatitis (CAD), and Chi-Huang solution for topical use has been shown to exhibit significant anti-inflammatory and anti-pruritic effects. This study aims to assess the anti-inflammatory and antipruritic effects of Chi-Huang cream in a squaric acid dibutyl ester (SADBE)-induced allergic contact dermatitis (ACD) chronic pruritus murine model in vivo. Thirty C57BL/6 N mice were randomly divided into six groups to evaluate the therapeutic effects of Chi-Huang cream on SADBE-induced allergic contact dermatitis (ACD). Except for the control group, all mice underwent ACD induction and received different treatments for eight days. The high-dose Chi-Huang (CH-H) group showed significantly improved skin lesions, reduced scratching behavior, and decreased skin thickness compared to the saline group, with efficacy comparable to hydrocortisone butyrate (HBC). Histological analysis confirmed reduced epidermal thickness and mast cell counts in CH-H treated mice. Moreover, Chi-Huang cream treatment showed fewer adverse effects, with better spleen and thymus indices than the HBC group. In a conclusion, Chi-Huang cream exhibits significant anti-inflammatory and anti-pruritic effects under a SADBE-induced ACD condition, with minimal impact on spleen and thymus indices. These findings suggest Chi-Huang cream may serve as a promising therapeutic agent in treating chronic pruritus.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"185 ","pages":"Article 106751"},"PeriodicalIF":2.5,"publicationDate":"2025-07-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144703830","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
Chemical profiling of Lycium shawii via RP-HPLC-QTOF-MS and MS/MS: unveiling its in-vivo wound-healing potential supported by molecular docking investigations 利用RP-HPLC-QTOF-MS和MS/MS对枸杞进行化学分析:通过分子对接研究揭示其体内伤口愈合潜力
IF 2.5 3区 医学
Fitoterapia Pub Date : 2025-07-21 DOI: 10.1016/j.fitote.2025.106749
Mahmoud Moustafa , Walaa S. Aboelmaaty , Weaam Ebrahim , Reham Hassan Mekky , Mohamed A. Tammam , Amr El-Demerdash , Ahmed M. Zaghloul
{"title":"Chemical profiling of Lycium shawii via RP-HPLC-QTOF-MS and MS/MS: unveiling its in-vivo wound-healing potential supported by molecular docking investigations","authors":"Mahmoud Moustafa ,&nbsp;Walaa S. Aboelmaaty ,&nbsp;Weaam Ebrahim ,&nbsp;Reham Hassan Mekky ,&nbsp;Mohamed A. Tammam ,&nbsp;Amr El-Demerdash ,&nbsp;Ahmed M. Zaghloul","doi":"10.1016/j.fitote.2025.106749","DOIUrl":"10.1016/j.fitote.2025.106749","url":null,"abstract":"<div><div><em>Lycium shawii</em> Roem. &amp; Schult., traditionally used across arid regions for treating various ailments, was investigated for its wound-healing potential using integrated metabolomic, computational, and in- vivo approaches. Methanolic extract profiling via RP-HPLC-QTOF-MS/MS identified 62 metabolites, including terpenes, fatty acids, and phenolics. Six key compounds were selected for molecular docking and in silico pharmacokinetic/toxicity analysis, showing strong predicted activity and drug-likeness. In vivo evaluation using a rat excision wound model revealed that treatment with a 2 % extract cream significantly enhanced wound closure (88.63 % by day 14), re-epithelialization, collagen deposition, and VEGF expression compared to controls. The findings suggest that <em>L. shawii</em> promotes wound healing through angiogenesis and tissue regeneration mechanisms. This study supports its traditional use and highlights its pharmaceutical potential.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"185 ","pages":"Article 106749"},"PeriodicalIF":2.5,"publicationDate":"2025-07-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144694356","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
Baicalein, a major component of the root of Oroxylum indicum (L.) Kurz (Bignoniaceae), inhibits phosphodiesterase 5 and vasodilates isolated pulmonary arteries through endothelium-independent mechanisms 黄芩素是黄芩根的主要成分。Kurz (Bignoniaceae),通过内皮独立机制抑制磷酸二酯酶5和血管扩张离体肺动脉。
IF 2.5 3区 医学
Fitoterapia Pub Date : 2025-07-21 DOI: 10.1016/j.fitote.2025.106753
Nattiya Chaichamnong , Corine Girard , Céline Demougeot , Nitra Nuengchamnong , Samjhana Bhandari , Prapapan Temkitthawon , Kornkanok Ingkaninan , Perle Totoson
{"title":"Baicalein, a major component of the root of Oroxylum indicum (L.) Kurz (Bignoniaceae), inhibits phosphodiesterase 5 and vasodilates isolated pulmonary arteries through endothelium-independent mechanisms","authors":"Nattiya Chaichamnong ,&nbsp;Corine Girard ,&nbsp;Céline Demougeot ,&nbsp;Nitra Nuengchamnong ,&nbsp;Samjhana Bhandari ,&nbsp;Prapapan Temkitthawon ,&nbsp;Kornkanok Ingkaninan ,&nbsp;Perle Totoson","doi":"10.1016/j.fitote.2025.106753","DOIUrl":"10.1016/j.fitote.2025.106753","url":null,"abstract":"<div><div><em>Oroxylum indicum</em> (L.) Kurz root has been traditionally used as an aphrodisiac. This study aimed to elucidate the phosphodiesterase (PDE) 5 inhibition and vasodilatory effects of <em>O. indicum</em> root extract and its main constituent. LC-QTOF-MS/MS analysis identified twenty constituents within the extract, including baicalein, biochanin A, and chrysin, detected in both positive and negative modes. HPLC analysis confirmed baicalein as the major constituent of <em>O. indicum</em> root extract. The extract exhibited potential for PDE5 inhibition, with an IC<sub>50</sub> value of 1.96 μg/mL. Among the three compounds, biochanin A demonstrated the highest PDE5 inhibition, with an IC<sub>50</sub> value of 6.16 μM, followed by baicalein (IC<sub>50</sub> = 20.54 μM) and chrysin (IC<sub>50</sub> = 42.18 μM). The vascular effects and mechanisms of <em>O. indicum</em> extract (0.01–300 μg/mL) and compounds (10<sup>−11</sup>–10<sup>−6</sup> M) were evaluated in rat-isolated pulmonary artery (PA) and aorta. Both <em>O. indicum</em> extract and baicalein exhibited potent vasodilatory effects, with greater efficacy in the PA compared to the aorta. E<sub>max</sub> values for PA versus aorta were 84.8 % versus 24.8 % (<em>p</em> &lt; 0.001) for <em>O. indicum</em> extract and 85.3 % versus 31.9 % (<em>p</em> &lt; 0.001) for baicalein. <em>O. indicum</em>-induced PA relaxation was endothelium-dependent, involving eNOS activation, COX pathways, and EDHF production. Conversely, baicalein-induced PA relaxation was endothelium-independent, mediated by inhibition of K<sub>v</sub> channels, intracellular calcium release, and blockade of alpha-1 adrenergic receptors. Taken together, these findings expand the biological profile of <em>O. indicum</em> root and highlight baicalein as a promising candidate for cardiovascular disease treatment.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"185 ","pages":"Article 106753"},"PeriodicalIF":2.5,"publicationDate":"2025-07-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144697975","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
Exploring the molecular mechanism of Chinese herbal extracts used to improve skin wound healing 探讨中药提取物促进皮肤创面愈合的分子机制。
IF 2.5 3区 医学
Fitoterapia Pub Date : 2025-07-21 DOI: 10.1016/j.fitote.2025.106752
Shan Fan , Xiaoqun Shen , Qing Liu , Wenhui Jiang , Liuyin Wang , Yakun Hao , Jia Yan , Shengguo Ji
{"title":"Exploring the molecular mechanism of Chinese herbal extracts used to improve skin wound healing","authors":"Shan Fan ,&nbsp;Xiaoqun Shen ,&nbsp;Qing Liu ,&nbsp;Wenhui Jiang ,&nbsp;Liuyin Wang ,&nbsp;Yakun Hao ,&nbsp;Jia Yan ,&nbsp;Shengguo Ji","doi":"10.1016/j.fitote.2025.106752","DOIUrl":"10.1016/j.fitote.2025.106752","url":null,"abstract":"<div><div>This study investigates the chemical composition and therapeutic mechanisms of Compound Pyocutaneous Liniments (CPL), a traditional Chinese medicine, in treating skin ulcers. Using UPLC-Q-Orbitrap-MS, 66 bioactive components were identified, including flavonoids, phenylpropanoids, and anthraquinones. Acute oral toxicity tests demonstrated that CPL has high safety within the tested dose range. Skin irritation tests revealed that CPL does not cause skin irritation. In a rat skin ulcer model, CPL significantly accelerated wound healing, enhanced collagen deposition, and upregulated CD34, VEGF, and EGF expression. Serum and skin metabolomics revealed CPL's regulation of glycerophospholipid and sphingolipid metabolism. Network pharmacology predicted TNF, AKT1, and EGFR as core targets, with pathways such as EGFR tyrosine kinase inhibitor resistance and VEGF signaling implicated. Molecular docking validated strong interactions between CPL components (e.g., luteolin) and these targets. These findings demonstrate CPL's multi-component, multi-target, and multi-pathway mechanisms, supporting its clinical application for skin ulcers.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"185 ","pages":"Article 106752"},"PeriodicalIF":2.5,"publicationDate":"2025-07-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144697976","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 therapeutic effect of Fallopia aubertii (L.Henry) Holub against HUA combined with AGA and the separation of chemical components of ethyl acetate extract. 黄连与AGA联合治疗HUA的疗效及乙酸乙酯提取物化学成分的分离研究。
IF 2.5 3区 医学
Fitoterapia Pub Date : 2025-07-21 DOI: 10.1016/j.fitote.2025.106755
Xiao-Hua Xu, Da-Jie Zou, Di-Jun Ji, Huan Wang, Yong-Chang Lu
{"title":"Study on the therapeutic effect of Fallopia aubertii (L.Henry) Holub against HUA combined with AGA and the separation of chemical components of ethyl acetate extract.","authors":"Xiao-Hua Xu, Da-Jie Zou, Di-Jun Ji, Huan Wang, Yong-Chang Lu","doi":"10.1016/j.fitote.2025.106755","DOIUrl":"https://doi.org/10.1016/j.fitote.2025.106755","url":null,"abstract":"<p><p>Fallopia aubertii (L.Henry) Holub, also known as Polygonum aubertii, is a traditional Tibetan medicinal plant widely used for its pharmacological effects, including clearing heat, dispelling wind and dampness, and promoting diuresis.Modern pharmacological studies have shown that Fallopia aubertii has better pharmacological effects on analgesic, anti-inflammatory and anti-hyperuricemia. However, its mechanism of action has not been elucidated.Therefore, in this study, the therapeutic effects of different extracts of Fallopia aubertii on HUA + AGA model rats were verified by in vivo experiments. Meanwhile, the main active parts of Fallopia aubertii were enriched and purified by on-line MCI column combined with two-dimensional preparative liquid chromatography to prepare high-purity single compounds, which initially explored the pharmacological constituents and mechanism of action of Fallopia aubertii. The pharmacological experiments showed that the ethyl acetate extracted part of Fallopia aubertii had significant efficacy in the treatment of acute gouty arthritis combined with hyperuricemia in rats. In addition, the main compounds isolated from the Fr6 fraction of the ethyl acetate fraction of Fallopia aubertii were flavonoids. It is speculated that the mechanism of action may be that the flavonoid compounds in Fallopia aubertii ethyl acetate inhibit the activity of XOD and reduce the level of inflammatory factors, thereby slowing down the synthesis of uric acid and alleviating inflammation. The online MCI column combined with two-dimensional liquid chromatography used in this study showed great potential in the separation of high-purity compounds from Fallopia aubertii, providing broad application prospects for the efficient separation of single compounds in natural plants.</p>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":" ","pages":"106755"},"PeriodicalIF":2.5,"publicationDate":"2025-07-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144697977","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
Adding value to botanical resources: Metabolic network analysis along with high-resolution bioassays screening and UHPLC-qToF-high-resolution MS/MS profiling detail the pharmacological potential of underexplored Latin-American plants. 增加植物资源的价值:代谢网络分析以及高分辨率生物测定筛选和uhplc - qtof高分辨率MS/MS分析详细介绍了未开发的拉丁美洲植物的药理潜力。
IF 2.5 3区 医学
Fitoterapia Pub Date : 2025-07-20 DOI: 10.1016/j.fitote.2025.106748
Chao Liang, Oliver Gericke, Yong Zhao, Casper Steinmann, Parvathy Krishnan, Gerardo Flores-Iga, Karel Miettinen, Bekzod Khakimov, Aldo Almeida
{"title":"Adding value to botanical resources: Metabolic network analysis along with high-resolution bioassays screening and UHPLC-qToF-high-resolution MS/MS profiling detail the pharmacological potential of underexplored Latin-American plants.","authors":"Chao Liang, Oliver Gericke, Yong Zhao, Casper Steinmann, Parvathy Krishnan, Gerardo Flores-Iga, Karel Miettinen, Bekzod Khakimov, Aldo Almeida","doi":"10.1016/j.fitote.2025.106748","DOIUrl":"https://doi.org/10.1016/j.fitote.2025.106748","url":null,"abstract":"<p><p>Healthcare services are challenged by an increased incidence of diseases and a decline in new drugs being brought to market. Thus, there is renewed interest in drug discovery from plants. This paper focused on enhancing the value of a small but diverse botanical resource of 45 Latin-American plant species, mostly from Mexican origin, through untargeted metabolomics, metabolic network analysis and parallel-in-vitro-bioactivity screening. The plant-extract collection was tested for inhibitory activity of human neutrophil elastase (HNE), α-glucosidase and PTP-1B as well as reviewing in detail antifungal and CB<sub>2</sub>-agonist activities previously reported for this collection. Through these approaches it was found that only 30 % of plants mentioned in traditional medicine to treat diabetes, had greater than 60 % inhibitory activity against PTP-1B or α-glucosidase and this could be part of their modes of action, while six plant species previously undescribed for antidiabetic use could inhibit these enzymes, with three of these plant species being ornamentals (Cosmos bipinnatus, Cuphea ignea and Clarkia amoena). Biochromatograms from active extracts show that the bioactivity is due to specific fractions/compounds. The results, indicate that parallel-in-vitro-bioactivity screening of plants is a valuable approach that could lead to the expansion of the natural-product chemical space for new therapeutics, even if no previous evidence of their use in traditional medicine exists. Results for HNE, CB<sub>2</sub>-agonist and antifungal assays were similar. This study delivers a valuable UHPLC-qToF-HRMS/MS dataset along with bioactivity screens that can serve the natural-products community for future endeavors in exploring the valuable chemical space of Latin-American plants.</p>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":" ","pages":"106748"},"PeriodicalIF":2.5,"publicationDate":"2025-07-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144689672","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 oxygenated sesquiterpenes from Bontia daphnoides L. leaves and in vitro evaluation of its antiviral and anti-inflammatory activity 新含氧倍半萜类化合物及其抗病毒抗炎活性的体外评价。
IF 2.5 3区 医学
Fitoterapia Pub Date : 2025-07-20 DOI: 10.1016/j.fitote.2025.106743
Amany A. Thabet , Iriny M. Ayoub , Fadia S. Youssef , Eman Al Sayed , Mohamed S. Elnaggar , Saad Moghannem , Michal Korinek , Rainer Kalscheuer , Abdel Nasser B. Singab
{"title":"New oxygenated sesquiterpenes from Bontia daphnoides L. leaves and in vitro evaluation of its antiviral and anti-inflammatory activity","authors":"Amany A. Thabet ,&nbsp;Iriny M. Ayoub ,&nbsp;Fadia S. Youssef ,&nbsp;Eman Al Sayed ,&nbsp;Mohamed S. Elnaggar ,&nbsp;Saad Moghannem ,&nbsp;Michal Korinek ,&nbsp;Rainer Kalscheuer ,&nbsp;Abdel Nasser B. Singab","doi":"10.1016/j.fitote.2025.106743","DOIUrl":"10.1016/j.fitote.2025.106743","url":null,"abstract":"<div><div><em>Bontia</em> is a monotypic genus containing <em>Bontia daphnoides</em> which is known as olive bush. It was used traditionally for the treatment of herpes, cough, colds, inflammation, ulcers and wounds. Therefore, in this study the anti-inflammatory and antiviral activities of the leaves extract and fractions were measured <em>in vitro</em>. Also phytochemical investigation of the non-polar fractions was done to identify the compounds responsible for activity. The anti-inflammatory activity was assessed by measuring the inhibition of superoxide anion generation and elastase release in fMLF/CB-induced human neutrophils. The antiviral activity was measured against Herpes simplex virus type 1 (HSV-1) and Hepatitis A virus (HAV<img>H10). The dichloromethane fraction showed the most potent anti-inflammatory activity by inhibiting superoxide anion generation and elastase release with IC<sub>50</sub> 5.21and 6.72 μg/mL, respectively. It showed antiviral activity with EC<sub>50</sub> of 332 and 290 μg/mL for HSV-1 and HAV<img>H10, respectively. The total extract showed a promising antiviral activity with EC<sub>50</sub> of 214 and 190 μg/mL against HSV-1 and HAV<img>H10, respectively. Phytochemical investigation of the <em>n</em>-hexane fraction of <em>B. daphnoides</em> resulted in the isolation of three oxygenated sesquiterpenes; dehydroepingaione (<strong>1</strong>), 10,11-dehydromyoporone (<strong>2</strong>) and the newly isolated compound; 1,2,15 trihydro-1,15-dimethoxy-2, 3-dihydroxy-dehydrongaione (<strong>3</strong>). Phytochemical investigation of dichloromethane fraction resulted in the isolation of new epimeric isomers 1<em>R</em>/1<em>S</em>-1-methoxy-1-hydro-15-oxodehydrongaione (<strong>4</strong>) and (<strong>5</strong>). From the results, it was concluded that nonpolar fractions of <em>B. daphnoides</em> could exhibit anti-inflammatory and antiviral activities, probably owing to the major oxygenated sesquiterpenes.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"185 ","pages":"Article 106743"},"PeriodicalIF":2.5,"publicationDate":"2025-07-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144689675","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
Combining transcriptomics and network pharmacology to reveal the mechanisms of QuZhuoHuaYu decoction ameliorating gouty arthritis 结合转录组学和网络药理学研究祛燥化瘀汤改善痛风性关节炎的作用机制
IF 2.5 3区 医学
Fitoterapia Pub Date : 2025-07-20 DOI: 10.1016/j.fitote.2025.106744
Haibo Tan , Shan Zhang , Ziyu Wang , Zhihao Zhang , Jianyong Zhang , Ertao Jia
{"title":"Combining transcriptomics and network pharmacology to reveal the mechanisms of QuZhuoHuaYu decoction ameliorating gouty arthritis","authors":"Haibo Tan ,&nbsp;Shan Zhang ,&nbsp;Ziyu Wang ,&nbsp;Zhihao Zhang ,&nbsp;Jianyong Zhang ,&nbsp;Ertao Jia","doi":"10.1016/j.fitote.2025.106744","DOIUrl":"10.1016/j.fitote.2025.106744","url":null,"abstract":"<div><div>QuZhuoHuaYu decoction (QZHY), a traditional Chinese medicine, has demonstrated a potential effect in gouty arthritis (GA) treatment, but its underlying mechanisms have yet to be fully elucidated. In this study, a strategy of UHPLC-Q-Orbitrap-MS/MS, transcriptomics, and network pharmacology combined with experimental verification was conducted to explore the constituents and the potential mechanisms of QZHY. A total of 26 compounds were identified from QZHY. Furthermore, QZHY significantly reduced the swelling index and inflammatory cell infiltration, and restrained macrophage M1 polarization and NLRP3/IL-1β pathway in ankle joints of GA mice. According to network pharmacology and transcriptomic analysis, it found NF-κB, HIF-1, and neutrophil extracellular trap (NET) formation pathways are the potential pathways for QZHY against GA. Experimental verification revealed that QZHY treatment inhibited NF-κB, HIF-1, and NET formation pathways in GA mice. In conclusion, QZHY ameliorates inflammation in GA mice, which may be associated with the inhibition of NLRP3, NF-κB, HIF-1, and NET formation pathways. It highlights a multi-target pharmacological mechanism of QZHY and provides a scientific basis for further study of QZHY on GA treatment.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"185 ","pages":"Article 106744"},"PeriodicalIF":2.5,"publicationDate":"2025-07-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144679366","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
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