Pub Date : 2025-12-23DOI: 10.1016/j.fitote.2025.107043
Bin Liu , Yang Xu , Lingxiao Ren , Xiaofen Liu , Lixia Chen , Hua Li
The seeds of Dimocarpus longan Lour. are rich in bioactive compounds, notably polyphenols, flavonoids, and sesquiterpenoids, which have demonstrated antioxidant, antitumor, and antifungal activities. Phytochemical investigation of the seeds led to the isolation of thirteen compounds (1−13), comprising six previously undescribed structures (1–6) and seven known analogues (7–13). The structures of the new compounds were elucidated through comprehensive spectroscopic analysis, including 1D/2D NMR, HR-ESI-MS, UV, ECD, and optical rotation. All isolated compounds were evaluated for their protective effects against hydrogen peroxide-induced oxidative stress in BV-2 microglial cells. Among them, compounds 2, 3, 7, 11, and 12 exhibited significant antioxidant activity. These findings underscore the potential of Dimocarpus longan seeds as a valuable source of bioactive agents for medicinal and functional food applications.
{"title":"Antioxidant active ingredients from the seeds of Dimocarpus longan Lour","authors":"Bin Liu , Yang Xu , Lingxiao Ren , Xiaofen Liu , Lixia Chen , Hua Li","doi":"10.1016/j.fitote.2025.107043","DOIUrl":"10.1016/j.fitote.2025.107043","url":null,"abstract":"<div><div>The seeds of <em>Dimocarpus longan</em> Lour. are rich in bioactive compounds, notably polyphenols, flavonoids, and sesquiterpenoids, which have demonstrated antioxidant, antitumor, and antifungal activities. Phytochemical investigation of the seeds led to the isolation of thirteen compounds (<strong>1−13</strong>), comprising six previously undescribed structures (<strong>1–6</strong>) and seven known analogues (<strong>7–13</strong>). The structures of the new compounds were elucidated through comprehensive spectroscopic analysis, including 1D/2D NMR, HR-ESI-MS, UV, ECD, and optical rotation. All isolated compounds were evaluated for their protective effects against hydrogen peroxide-induced oxidative stress in BV-2 microglial cells. Among them, compounds <strong>2</strong>, <strong>3</strong>, <strong>7</strong>, <strong>11</strong>, and <strong>12</strong> exhibited significant antioxidant activity. These findings underscore the potential of <em>Dimocarpus longan</em> seeds as a valuable source of bioactive agents for medicinal and functional food applications.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"189 ","pages":"Article 107043"},"PeriodicalIF":2.6,"publicationDate":"2025-12-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145833369","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}
Pub Date : 2025-12-23DOI: 10.1016/j.fitote.2025.107046
Yu-Ying Liu , Chan-Ting Lai , Salman Khan , Qian-Jing Zheng , Rong Zhang , Wei-Yi Wang , Bin Wu , Shan He , Li Yang , Ting-Ting Wang
One undescribed quinoline derivative, xylaminoquin A (1), one new p-aminobenzoic acid derivative, xylamidate B (2), and methyl 4-(butanoylamino)-3-hydroxybenzoate, reported for the first time as a natural product and named xylamidate C (3), together with known alkaloids and diketopiperazines, methyl 4-acetylamino-3-hydroxybenzoate (4), methyl 4-[(1-oxobutyl)amino]benzoate (5), pseurotin A (6), azaspirofuran A (7), cyclo(l-Tyr-l-Leu) (8), and cyclo-(l-Tyr-l-Val) (9) were isolated from Xylaria sp. NBUF245, a fungus associated with a Demosponge sp. collected from the marine mesophotic zone. Structurally, compound 1 is the first example of 3,7-dissubstitented quinoline derivative isolated from fungi. The structures of all compounds were elucidated by combined analysis of spectroscopic data and X-ray crystallography. Bioassay results showed that compound 5 effectively prevented prednisolone-induced bone loss in zebrafish at a concentration of 30 μM, suggesting potential osteoprotective activity.
{"title":"Quinoline and para-aminobenzoic acid derivatives with anti-osteoclastic activity from a marine mesophotic zone Demosponge sponge-associated fungus Xylaria sp. NBUF245","authors":"Yu-Ying Liu , Chan-Ting Lai , Salman Khan , Qian-Jing Zheng , Rong Zhang , Wei-Yi Wang , Bin Wu , Shan He , Li Yang , Ting-Ting Wang","doi":"10.1016/j.fitote.2025.107046","DOIUrl":"10.1016/j.fitote.2025.107046","url":null,"abstract":"<div><div>One undescribed quinoline derivative, xylaminoquin A (<strong>1</strong>), one new <em>p</em>-aminobenzoic acid derivative, xylamidate B (<strong>2</strong>), and methyl 4-(butanoylamino)-3-hydroxybenzoate, reported for the first time as a natural product and named xylamidate C (<strong>3</strong>), together with known alkaloids and diketopiperazines, methyl 4-acetylamino-3-hydroxybenzoate (<strong>4</strong>), methyl 4-[(1-oxobutyl)amino]benzoate (<strong>5</strong>), pseurotin A (<strong>6</strong>), azaspirofuran A (<strong>7</strong>), cyclo(<span>l</span>-Tyr-<span>l</span>-Leu) (<strong>8</strong>), and cyclo-(<span>l</span>-Tyr-<span>l</span>-Val) (<strong>9</strong>) were isolated from <em>Xylaria</em> sp. NBUF245, a fungus associated with a <em>Demosponge</em> sp. collected from the marine mesophotic zone. Structurally, compound <strong>1</strong> is the first example of 3,7-dissubstitented quinoline derivative isolated from fungi. The structures of all compounds were elucidated by combined analysis of spectroscopic data and X-ray crystallography. Bioassay results showed that compound <strong>5</strong> effectively prevented prednisolone-induced bone loss in zebrafish at a concentration of 30 μM, suggesting potential osteoprotective activity.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"189 ","pages":"Article 107046"},"PeriodicalIF":2.6,"publicationDate":"2025-12-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145833376","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}
Pub Date : 2025-12-22DOI: 10.1016/j.fitote.2025.107051
Ke Xu , Xiao-Bin Li , Yu-Liang Xu , Fei Xie , Hong-Xiang Lou
Inclusion of the histone deacetylase (HDAC) inhibitor suberoylanilide hydroxamic acid (SAHA) into the culture medium of the endolichenic fungus Phialocephala fortinii resulted in the separation of three new perylenequinones phialocephalarins E-G (1–3) and enhanced the production of the known compounds phialocephalarins A-B (4–5). A comprehensive spectral analysis combined with electron circular dichroism (ECD) data has elucidated their structures. Phialocephalarin E (1) displayed anti-inflammatory activity with the maximum inhibition rate of 57.3 % ± 7.3 % (50 μM). Further molecular docking experiment revealed the affinity degree of compound 1 to the prostaglandin E2 receptor 4 (EP4R) and the molecular dynamics (MD) simulation results showed compound 1-EP4R complex had relatively good binding stability.
{"title":"Anti-inflammatory perylenequinones from the endolichenic fungus Phialocephala fortinii triggered by a histone deacetylase inhibitor","authors":"Ke Xu , Xiao-Bin Li , Yu-Liang Xu , Fei Xie , Hong-Xiang Lou","doi":"10.1016/j.fitote.2025.107051","DOIUrl":"10.1016/j.fitote.2025.107051","url":null,"abstract":"<div><div>Inclusion of the histone deacetylase (HDAC) inhibitor suberoylanilide hydroxamic acid (SAHA) into the culture medium of the endolichenic fungus <em>Phialocephala fortinii</em> resulted in the separation of three new perylenequinones phialocephalarins <em>E</em>-G (<strong>1</strong>–<strong>3</strong>) and enhanced the production of the known compounds phialocephalarins A-B (<strong>4</strong>–<strong>5)</strong>. A comprehensive spectral analysis combined with electron circular dichroism (ECD) data has elucidated their structures. Phialocephalarin E (<strong>1</strong>) displayed anti-inflammatory activity with the maximum inhibition rate of 57.3 % ± 7.3 % (50 μM). Further molecular docking experiment revealed the affinity degree of compound <strong>1</strong> to the prostaglandin E2 receptor 4 (EP4R) and the molecular dynamics (MD) simulation results showed compound <strong>1</strong>-EP4R complex had relatively good binding stability.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"189 ","pages":"Article 107051"},"PeriodicalIF":2.6,"publicationDate":"2025-12-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145827027","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}
Pub Date : 2025-12-22DOI: 10.1016/j.fitote.2025.107049
Zhiguo Mao , Xingyi Yang , Ying Liu , Yu Huan , Yixue Gao , Jinying Zhang , Xiangke Lin , Shuo Tian , Yagang Song , Mingsan Miao
Background
Prunella vulgaris L. is a traditional Chinese medicine known for its ability to disperse nodules and reduce swelling. However, research on the effect of the volatile oil from Prunella vulgaris L. on pulmonary nodulosis remains limited.
Aim of the study
To investigate whether essential oil from Prunella vulgaris L. (PVEO) improves pulmonary function in PS mice by inhibiting the inflammation mediated by the TLR4/MyD88/NF-κB pathway.
Methods
Network pharmacology was used to explore how PVEO might treat PS. GC–MS identified PVEO's chemical components. A PS mouse model was created using Propionibacterium acnes. ELISA measured inflammatory factors in the BALF and blood of these mice. Flow cytometry analyzed CD4+ T cell differentiation into TH1 and TH17 cells. Immunofluorescence assessed macrophage differentiation into M1 and M2 phenotypes and the expression of TLR4, MyD88, and NF-κB. PCR and WB were conducted to detect the expression of mRNAs and proteins related to the TLR4/MyD88/NF-κB pathway.
Results
Network pharmacology predictions indicated that the improvement of pulmonary function by PVEO in PS mice was associated with the TLR4/MyD88/NF-κB signaling pathway. PCR and western blot (WB) analyses demonstrated that PVEO inhibited the expression of relevant mRNAs and proteins within the TLR4/MyD88/NF-κB pathway. Immunofluorescence and flow cytometry assays suggested that PVEO suppressed the differentiation of M1 macrophages, TH1, and TH17 cells in lung tissues of PS mice.
Conclusion
PVEO exerts anti-PS effects by inhibiting the inflammation mediated by the TLR4/MyD88/NF-κB pathway in macrophages.
背景：夏枯草（Prunella vulgaris L.）是一种以散瘤消肿著称的中药。然而，关于夏枯草挥发油对肺结节病的作用的研究还很有限。研究目的：探讨枯草精油（PVEO）是否通过抑制TLR4/MyD88/NF-κB通路介导的炎症，改善PS小鼠肺功能。方法：采用网络药理学方法探讨PVEO对PS的治疗作用，GC-MS鉴定PVEO的化学成分。采用痤疮丙酸杆菌建立小鼠PS模型。ELISA法测定这些小鼠的BALF和血液中的炎症因子。流式细胞术分析CD4+ T细胞向TH1和TH17细胞分化的情况。免疫荧光检测巨噬细胞向M1和M2表型分化及TLR4、MyD88和NF-κB的表达。采用PCR和WB检测TLR4/MyD88/NF-κB通路相关mrna和蛋白的表达情况。结果：网络药理学预测提示PVEO对PS小鼠肺功能的改善与TLR4/MyD88/NF-κB信号通路有关。PCR和western blot （WB）分析表明，PVEO抑制TLR4/MyD88/NF-κB通路相关mrna和蛋白的表达。免疫荧光和流式细胞术检测显示，PVEO可抑制PS小鼠肺组织中M1巨噬细胞、TH1和TH17细胞的分化。结论：PVEO通过抑制巨噬细胞TLR4/MyD88/NF-κB通路介导的炎症，发挥抗ps作用。
{"title":"Modulation of immune cell differentiation by Prunella vulgaris L. essential oil in pulmonary sarcoidosis treatment","authors":"Zhiguo Mao , Xingyi Yang , Ying Liu , Yu Huan , Yixue Gao , Jinying Zhang , Xiangke Lin , Shuo Tian , Yagang Song , Mingsan Miao","doi":"10.1016/j.fitote.2025.107049","DOIUrl":"10.1016/j.fitote.2025.107049","url":null,"abstract":"<div><h3>Background</h3><div><em>Prunella vulgaris</em> L. is a traditional Chinese medicine known for its ability to disperse nodules and reduce swelling. However, research on the effect of the volatile oil from <em>Prunella vulgaris</em> L. on pulmonary nodulosis remains limited.</div></div><div><h3>Aim of the study</h3><div>To investigate whether essential oil from <em>Prunella vulgaris</em> L. (PVEO) improves pulmonary function in PS mice by inhibiting the inflammation mediated by the TLR4/MyD88/NF-κB pathway.</div></div><div><h3>Methods</h3><div>Network pharmacology was used to explore how PVEO might treat PS. GC–MS identified PVEO's chemical components. A PS mouse model was created using <em>Propionibacterium acnes</em>. ELISA measured inflammatory factors in the BALF and blood of these mice. Flow cytometry analyzed CD4<sup>+</sup> T cell differentiation into TH1 and TH17 cells. Immunofluorescence assessed macrophage differentiation into M1 and M2 phenotypes and the expression of TLR4, MyD88, and NF-κB. PCR and WB were conducted to detect the expression of mRNAs and proteins related to the TLR4/MyD88/NF-κB pathway.</div></div><div><h3>Results</h3><div>Network pharmacology predictions indicated that the improvement of pulmonary function by PVEO in PS mice was associated with the TLR4/MyD88/NF-κB signaling pathway. PCR and western blot (WB) analyses demonstrated that PVEO inhibited the expression of relevant mRNAs and proteins within the TLR4/MyD88/NF-κB pathway. Immunofluorescence and flow cytometry assays suggested that PVEO suppressed the differentiation of M1 macrophages, TH1, and TH17 cells in lung tissues of PS mice.</div></div><div><h3>Conclusion</h3><div>PVEO exerts anti-PS effects by inhibiting the inflammation mediated by the TLR4/MyD88/NF-κB pathway in macrophages.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"189 ","pages":"Article 107049"},"PeriodicalIF":2.6,"publicationDate":"2025-12-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145827020","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}
Pub Date : 2025-12-22DOI: 10.1016/j.fitote.2025.107050
Zijin Xu , Shaoxian Wang , Hao Chen , Tao Lv , Zhiwen Zhang , Faxiang Pu , Zhangfu Xie , Longfei Feng , Ping Wang
Ethnopharmacological relevance
Tetrastigma hemsleyanum Diels et Gilg (TDG), a traditional Chinese medicinal (TCM) plant, is historically used for liver injury treatment. Despite its ethnopharmacological significance, systematic studies on how processing affects its composition and efficacy remain lacking.
Aim of the study
This study aimed to compare the chemical profiles and hepatoprotective effects of extracts from TDG processed with three different Paozhi (TCM processing) methods (fresh, freeze-dried, and hot-air drying) and explore their mechanisms against drug-induced liver injury (DILI).
Materials and methods
Chemical constituents were analyzed via UPLC-Q-TOF-MS/MS. Hepatoprotection was evaluated using an acetaminophen (APAP)-induced human normal hepatocytes (LO2) cell model. Network pharmacology and molecular docking identified targets and pathways.
Results
Thirty-two compounds were identified across TDG extracts, with 13 shared and 19 unique to specific formulations. All extracts alleviated liver injury, but freeze-dried TDG (TDG-b) showed the strongest effect. Quercetin, procyanidin B1, catechins, kaempferol, and isorhamnetin emerged as key active constituents in TDG-b, targeting DILI through cancer, lipid and atherosclerosis, Hypoxia-Inducible Factor 1 (HIF-1), and Tumor Necrosis Factor (TNF) signaling pathways. Molecular docking confirmed robust binding between these compounds and core therapeutic targets.
Conclusions
TDG-b, a freeze-dried extract, optimally preserves bioactive constituents and demonstrates superior anti-DILI activity, validating traditional processing wisdom. This study bridges ethnopharmacological knowledge and mechanistic evidence, guiding TDG-based therapeutic optimization.
民族药理学相关性：四柱草（Tetrastigma hemsleyanum Diels et Gilg， TDG）是一种传统的中药植物，历史上被用于肝损伤治疗。尽管其具有民族药理学意义，但加工过程如何影响其成分和功效的系统研究仍然缺乏。目的：本研究旨在比较三种中药泡治方法（新鲜、冷冻干燥和热风干燥）炮制的龙胆提取物的化学成分和肝保护作用，并探讨其抗药物性肝损伤（DILI）的机制。材料与方法：化学成分分析采用UPLC-Q-TOF-MS/MS法。采用对乙酰氨基酚（APAP）诱导的人正常肝细胞（LO2）细胞模型评估肝保护作用。网络药理学和分子对接确定靶点和途径。结果：在TDG提取物中鉴定出32种化合物，其中13种是共有的，19种是独特的。所有提取物均能减轻肝损伤，但冻干TDG （TDG-b）的作用最强。槲皮素、原花青素B1、儿茶素、山奈酚和异鼠李素是TDG-b中的关键活性成分，通过癌症、脂质和动脉粥样硬化、缺氧诱导因子1 （HIF-1）和肿瘤坏死因子（TNF）信号通路靶向DILI。分子对接证实了这些化合物与核心治疗靶点之间的强大结合。结论：冻干提取物TDG-b具有较好的保存生物活性成分和抗dili活性，验证了传统的加工智慧。本研究将民族药理学知识与机制证据相结合，指导基于tdg的治疗优化。
{"title":"A comparative study of the hepatoprotective effects of the three processed products of Tetrastigma hemsleyanum Diels et Gilg: in vitro pharmacological investigation and integrating Network pharmacology","authors":"Zijin Xu , Shaoxian Wang , Hao Chen , Tao Lv , Zhiwen Zhang , Faxiang Pu , Zhangfu Xie , Longfei Feng , Ping Wang","doi":"10.1016/j.fitote.2025.107050","DOIUrl":"10.1016/j.fitote.2025.107050","url":null,"abstract":"<div><h3>Ethnopharmacological relevance</h3><div><em>Tetrastigma hemsleyanum</em> Diels et Gilg (TDG), a traditional Chinese medicinal (TCM) plant, is historically used for liver injury treatment. Despite its ethnopharmacological significance, systematic studies on how processing affects its composition and efficacy remain lacking.</div></div><div><h3>Aim of the study</h3><div>This study aimed to compare the chemical profiles and hepatoprotective effects of extracts from TDG processed with three different Paozhi (TCM processing) methods (fresh, freeze-dried, and hot-air drying) and explore their mechanisms against drug-induced liver injury (DILI).</div></div><div><h3>Materials and methods</h3><div>Chemical constituents were analyzed <em>via</em> UPLC-Q-TOF-MS/MS. Hepatoprotection was evaluated using an acetaminophen (APAP)-induced human normal hepatocytes (LO2) cell model. Network pharmacology and molecular docking identified targets and pathways.</div></div><div><h3>Results</h3><div>Thirty-two compounds were identified across TDG extracts, with 13 shared and 19 unique to specific formulations. All extracts alleviated liver injury, but freeze-dried TDG (TDG-b) showed the strongest effect. Quercetin, procyanidin B1, catechins, kaempferol, and isorhamnetin emerged as key active constituents in TDG-b, targeting DILI through cancer, lipid and atherosclerosis, Hypoxia-Inducible Factor 1 (HIF-1), and Tumor Necrosis Factor (TNF) signaling pathways. Molecular docking confirmed robust binding between these compounds and core therapeutic targets.</div></div><div><h3>Conclusions</h3><div>TDG-b, a freeze-dried extract, optimally preserves bioactive constituents and demonstrates superior anti-DILI activity, validating traditional processing wisdom. This study bridges ethnopharmacological knowledge and mechanistic evidence, guiding TDG-based therapeutic optimization.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"189 ","pages":"Article 107050"},"PeriodicalIF":2.6,"publicationDate":"2025-12-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145827046","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}
Pub Date : 2025-12-22DOI: 10.1016/j.fitote.2025.107052
Fui-Ling Voon , Yu Zhao Lee , Xiao Ying Ooi , Charlotte Zi Ern Tay , Ji Wei Tan , Chau Ling Tham , Yu-Cheng Ho , Ming Tatt Lee
Purpurin, a naturally occurring anthraquinone pigment, has gained attention for its promising anticancer properties. This systematic-narrative hybrid review summarises current preclinical evidence on its mechanisms of action, pharmacology, and translational potential. Literature searches were conducted using PubMed, Web of Science, Scopus, and Google Scholar up to June 2025. Purpurin demonstrates selective cytotoxicity across multiple cancer models through redox imbalance, mitochondrial dysfunction, inhibition of PI3K/AKT signalling, and upregulation of the tumour suppressor LHPP. It also interferes with amino acid and glutamine metabolism and suppresses oncogenic protein aggregation. As a photosensitiser, purpurin enhances photodynamic therapy through light-activated ROS generation. Despite these promising mechanistic insights, its clinical applicability remains limited by poor aqueous solubility, rapid metabolism, and insufficient pharmacokinetic and toxicological data. Early in vivo studies indicate favourable safety, and emerging nanoparticle-based delivery systems show potential to improve bioavailability and tumour targeting. Collectively, current findings highlight purpurin as a compelling candidate for further development in oncology, particularly as part of combination or photo-enhanced therapeutic approaches. Continued research is required to address existing pharmacological gaps and to evaluate purpurin in clinically relevant models.
紫癜素是一种天然存在的蒽醌色素，因其具有良好的抗癌特性而受到关注。这篇系统叙述的混合综述总结了目前关于其作用机制、药理学和转化潜力的临床前证据。截至2025年6月，使用PubMed、Web of Science、Scopus和谷歌Scholar进行文献检索。Purpurin通过氧化还原失衡、线粒体功能障碍、抑制PI3K/AKT信号和上调肿瘤抑制因子LHPP，在多种癌症模型中显示出选择性细胞毒性。它还干扰氨基酸和谷氨酰胺代谢，抑制致癌蛋白聚集。作为一种光敏剂，紫癜素通过光激活ROS的产生来增强光动力治疗。尽管这些有希望的机制见解，但其临床适用性仍然受到水溶性差，代谢快，药代动力学和毒理学数据不足的限制。早期体内研究表明良好的安全性，新兴的基于纳米颗粒的递送系统显示出提高生物利用度和肿瘤靶向性的潜力。总的来说，目前的研究结果突出了紫癜蛋白作为肿瘤学进一步发展的引人注目的候选者，特别是作为联合或光增强治疗方法的一部分。需要继续研究以解决现有的药理学空白，并在临床相关模型中评估紫癜蛋白。
{"title":"Purpurin as a promising anticancer agent: A review of preclinical evidence","authors":"Fui-Ling Voon , Yu Zhao Lee , Xiao Ying Ooi , Charlotte Zi Ern Tay , Ji Wei Tan , Chau Ling Tham , Yu-Cheng Ho , Ming Tatt Lee","doi":"10.1016/j.fitote.2025.107052","DOIUrl":"10.1016/j.fitote.2025.107052","url":null,"abstract":"<div><div>Purpurin, a naturally occurring anthraquinone pigment, has gained attention for its promising anticancer properties. This systematic-narrative hybrid review summarises current preclinical evidence on its mechanisms of action, pharmacology, and translational potential. Literature searches were conducted using PubMed, Web of Science, Scopus, and Google Scholar up to June 2025. Purpurin demonstrates selective cytotoxicity across multiple cancer models through redox imbalance, mitochondrial dysfunction, inhibition of PI3K/AKT signalling, and upregulation of the tumour suppressor LHPP. It also interferes with amino acid and glutamine metabolism and suppresses oncogenic protein aggregation. As a photosensitiser, purpurin enhances photodynamic therapy through light-activated ROS generation. Despite these promising mechanistic insights, its clinical applicability remains limited by poor aqueous solubility, rapid metabolism, and insufficient pharmacokinetic and toxicological data. Early <em>in vivo</em> studies indicate favourable safety, and emerging nanoparticle-based delivery systems show potential to improve bioavailability and tumour targeting. Collectively, current findings highlight purpurin as a compelling candidate for further development in oncology, particularly as part of combination or photo-enhanced therapeutic approaches. Continued research is required to address existing pharmacological gaps and to evaluate purpurin in clinically relevant models.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"189 ","pages":"Article 107052"},"PeriodicalIF":2.6,"publicationDate":"2025-12-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145801955","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}
Pub Date : 2025-12-22DOI: 10.1016/j.fitote.2025.107053
Yasser Fakri Mustafa
Background
Coumarins, naturally occurring benzopyrone derivatives, have long been valued in traditional medicine, fragrance industries, and therapeutics. Recent interest has surged around their anti-aging properties, particularly in skincare, due to their antioxidant, anti-inflammatory, and photoprotective effects.
Objective
This review explores the role of coumarins as promising agents in combating skin aging, offering a natural alternative to synthetic cosmetics and contributing to the development of safe, effective anti-aging products.
Methods
An integrative analysis of historical, biochemical, pharmacological, and cosmetic perspectives was conducted, supported by traditional medicine records, modern preclinical studies, bioinformatics predictions, and formulation case studies. Emphasis was placed on coumarins' mechanisms of action, extraction methods, safety profiles, and their application in skincare formulations.
Results
Coumarins act through both direct and indirect antioxidant mechanisms, targeting pathways involved in oxidative stress, inflammation, collagen degradation, and skin barrier dysfunction. Studies show that certain derivatives can inhibit MMPs and modulate sirtuin and AMPK pathways, mechanisms vital in anti-aging interventions. Traditional medicine has long leveraged coumarin-rich herbs to treat dermatological, circulatory, and neurodegenerative conditions. Case studies confirmed favorable cosmetic properties in formulations containing coumarins and hyaluronic acid. Comparative analysis with existing anti-aging ingredients revealed that coumarins provide multi-targeted, dermo-compatible action with fewer adverse effects. Despite regulatory constraints, coumarins remain widely used in skincare and perfumes, with growing interest in sustainable sourcing and green synthesis.
Conclusion
Coumarins represent a scientifically grounded, culturally enriched, and biologically potent class of compounds that align with modern demands for natural and effective anti-aging solutions. Their multifunctionality, favorable safety profile, and dermo-pharmacological compatibility support their potential as key agents in next-generation beauty products. Further interdisciplinary research and regulatory harmonization are essential for optimizing their use in cosmetic and therapeutic contexts.
{"title":"Coumarins and the science of timeless beauty: A natural anti-skin aging solution","authors":"Yasser Fakri Mustafa","doi":"10.1016/j.fitote.2025.107053","DOIUrl":"10.1016/j.fitote.2025.107053","url":null,"abstract":"<div><h3>Background</h3><div>Coumarins, naturally occurring benzopyrone derivatives, have long been valued in traditional medicine, fragrance industries, and therapeutics. Recent interest has surged around their anti-aging properties, particularly in skincare, due to their antioxidant, anti-inflammatory, and photoprotective effects.</div></div><div><h3>Objective</h3><div>This review explores the role of coumarins as promising agents in combating skin aging, offering a natural alternative to synthetic cosmetics and contributing to the development of safe, effective anti-aging products.</div></div><div><h3>Methods</h3><div>An integrative analysis of historical, biochemical, pharmacological, and cosmetic perspectives was conducted, supported by traditional medicine records, modern preclinical studies, bioinformatics predictions, and formulation case studies. Emphasis was placed on coumarins' mechanisms of action, extraction methods, safety profiles, and their application in skincare formulations.</div></div><div><h3>Results</h3><div>Coumarins act through both direct and indirect antioxidant mechanisms, targeting pathways involved in oxidative stress, inflammation, collagen degradation, and skin barrier dysfunction. Studies show that certain derivatives can inhibit MMPs and modulate sirtuin and AMPK pathways, mechanisms vital in anti-aging interventions. Traditional medicine has long leveraged coumarin-rich herbs to treat dermatological, circulatory, and neurodegenerative conditions. Case studies confirmed favorable cosmetic properties in formulations containing coumarins and hyaluronic acid. Comparative analysis with existing anti-aging ingredients revealed that coumarins provide multi-targeted, dermo-compatible action with fewer adverse effects. Despite regulatory constraints, coumarins remain widely used in skincare and perfumes, with growing interest in sustainable sourcing and green synthesis.</div></div><div><h3>Conclusion</h3><div>Coumarins represent a scientifically grounded, culturally enriched, and biologically potent class of compounds that align with modern demands for natural and effective anti-aging solutions. Their multifunctionality, favorable safety profile, and dermo-pharmacological compatibility support their potential as key agents in next-generation beauty products. Further interdisciplinary research and regulatory harmonization are essential for optimizing their use in cosmetic and therapeutic contexts.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"189 ","pages":"Article 107053"},"PeriodicalIF":2.6,"publicationDate":"2025-12-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145826979","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}
Pub Date : 2025-12-22DOI: 10.1016/j.fitote.2025.107055
Márcio B. Weiss , Jaewon Yoon , João P.B. Domingues , Fernanda R. Jacinavicius , Vitor F. Freire , Helori V. Domingos , Manoel O. de Moraes Junior , Camila M.C. Gonçalves , Sandra R. Castro , José A.L. Lindoso , Silvya S. Maria-Engler , Leticia V. Costa-Lotufo , Ricardo M. Borges , Roberto G.S. Berlinck , Camila M. Crnkovic
Natural products are a valuable source of molecules with therapeutic and biotechnological applications. However, the complexity of biological matrices and the increasing rates of rediscovery pose significant challenges in the search for new bioactive compounds. Exploring novel specimens from biodiversity and utilizing modern cheminformatics tools are essential to advancing natural product discovery. In this study, we employed metabolomics and bioassays to investigate the potential of filamentous cyanobacteria collected in Brazil as a source of new bioactive secondary metabolites. Extracts and fractions from eight freshwater cyanobacterial strains were tested for their general toxicity against Artemia salina, as well as antiparasitic and cytotoxic activities and analyzed by UHPLC-HRMS-MS/MS. Molecular networks were constructed from MS/MS data using the GNPS platform, and dereplication was guided by DAFdiscovery results for feature prioritization. Annotation and dereplication were conducted using SIRIUS combined with manual analysis of HRMS and MS/MS spectra. Our study identified three cyanobacterial strains as producers of potentially novel and bioactive metabolites for in-depth investigations.
{"title":"Uncovering chemical novelty from freshwater filamentous Cyanobacteria","authors":"Márcio B. Weiss , Jaewon Yoon , João P.B. Domingues , Fernanda R. Jacinavicius , Vitor F. Freire , Helori V. Domingos , Manoel O. de Moraes Junior , Camila M.C. Gonçalves , Sandra R. Castro , José A.L. Lindoso , Silvya S. Maria-Engler , Leticia V. Costa-Lotufo , Ricardo M. Borges , Roberto G.S. Berlinck , Camila M. Crnkovic","doi":"10.1016/j.fitote.2025.107055","DOIUrl":"10.1016/j.fitote.2025.107055","url":null,"abstract":"<div><div>Natural products are a valuable source of molecules with therapeutic and biotechnological applications. However, the complexity of biological matrices and the increasing rates of rediscovery pose significant challenges in the search for new bioactive compounds. Exploring novel specimens from biodiversity and utilizing modern cheminformatics tools are essential to advancing natural product discovery. In this study, we employed metabolomics and bioassays to investigate the potential of filamentous cyanobacteria collected in Brazil as a source of new bioactive secondary metabolites. Extracts and fractions from eight freshwater cyanobacterial strains were tested for their general toxicity against <em>Artemia salina</em>, as well as antiparasitic and cytotoxic activities and analyzed by UHPLC-HRMS-MS/MS. Molecular networks were constructed from MS/MS data using the GNPS platform, and dereplication was guided by DAFdiscovery results for feature prioritization. Annotation and dereplication were conducted using SIRIUS combined with manual analysis of HRMS and MS/MS spectra. Our study identified three cyanobacterial strains as producers of potentially novel and bioactive metabolites for in-depth investigations.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"189 ","pages":"Article 107055"},"PeriodicalIF":2.6,"publicationDate":"2025-12-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145827032","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}
Pub Date : 2025-12-21DOI: 10.1016/j.fitote.2025.107048
Pei-Pei Zhang , Ming-Yang Cui , Shui-Yuan Yang , Bo Han , Wei Yu , Tian-Tian Wei , Ke-Wu Zeng , Peng-Fei Tu
Recent studies have demonstrated the therapeutic potential of Astragalus membranaceus in diabetic kidney disease (DKD); however, the underlying mechanisms remain incompletely elucidated. In this study, we established a streptozotocin-induced DKD mouse model to evaluate the effects of A. membranaceus extract (AME) on glycemic control, renal function, gut microbiota composition, and metabolic profiles. Biochemical analyzes revealed that A. membranaceus significantly attenuated hyperglycemia and improved renal function, as indicated by reduced serum creatinine and blood urea nitrogen levels. Metagenomic sequencing demonstrated that A. membranaceus reversed microbial dysbiosis by suppressing pathogenic bacteria (e.g., Aerococcus urinaeequi) and enriching beneficial probiotics (e.g., Thomasclavelia cocleata). Furthermore, LC/MS-based metabolomics identified key metabolic pathways, including glycerophospholipid metabolism and bile acid synthesis, as potential mediators of the therapeutic effects. These findings underscore the crucial role of the gut-renal axis in DKD pathogenesis and provide a mechanistic basis for the clinical application of A. membranaceus.
{"title":"Astragalus membranaceus improves blood glucose and renal function in diabetic kidney disease mice via gut microbial metabolite axis","authors":"Pei-Pei Zhang , Ming-Yang Cui , Shui-Yuan Yang , Bo Han , Wei Yu , Tian-Tian Wei , Ke-Wu Zeng , Peng-Fei Tu","doi":"10.1016/j.fitote.2025.107048","DOIUrl":"10.1016/j.fitote.2025.107048","url":null,"abstract":"<div><div>Recent studies have demonstrated the therapeutic potential of <em>Astragalus membranaceus</em> in diabetic kidney disease (DKD); however, the underlying mechanisms remain incompletely elucidated. In this study, we established a streptozotocin-induced DKD mouse model to evaluate the effects of <em>A. membranaceus</em> extract (AME) on glycemic control, renal function, gut microbiota composition, and metabolic profiles. Biochemical analyzes revealed that <em>A. membranaceus</em> significantly attenuated hyperglycemia and improved renal function, as indicated by reduced serum creatinine and blood urea nitrogen levels. Metagenomic sequencing demonstrated that <em>A. membranaceus</em> reversed microbial dysbiosis by suppressing pathogenic bacteria (e.g., <em>Aerococcus urinaeequi</em>) and enriching beneficial probiotics (e.g., <em>Thomasclavelia cocleata</em>). Furthermore, LC/MS-based metabolomics identified key metabolic pathways, including glycerophospholipid metabolism and bile acid synthesis, as potential mediators of the therapeutic effects. These findings underscore the crucial role of the gut-renal axis in DKD pathogenesis and provide a mechanistic basis for the clinical application of <em>A. membranaceus</em>.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"189 ","pages":"Article 107048"},"PeriodicalIF":2.6,"publicationDate":"2025-12-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145818606","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}
Six new polyketides, including three naphthalene-types (1–3) and three γ-lactones-types (4–6), along with 14 known polyketides (7–20), were isolated from a pathogen endophytic fungus Phomopsis sp. XP-8 of Eucommia ulmoides Oliver. Their structures were elucidated by spectrometric analysis using MS and NMR data. The absolute configurations were established using statistical comparative analysis of the experimental ECD data, in conjunction with quantum mechanical calculations. All the compounds and crude extracts were evaluated for their antibacterial activity. Compounds 2, 3, 6, 7, 8, and 10 exhibited moderate inhibition on three gram-positive bacteria, Staphylococcus aureus, Bacillus subtilis, and Bacillus thuringiensis. Synergistic antibacterial interaction experiments showed that compounds 1, 2, 3, 6, 7, 8, and 19 with antibiotics can greatly enhance the inhibition rate against bacteria. The target screening and molecular docking of these compounds were also carried out, with further verification of molecular dynamics, revealing that the compounds exert antibacterial activity by targeting both the Fur-regulated basic protein (FbpB) and drug resistance protein D (EmrD), exhibiting synergy with antibiotics by inhibiting the DNA polymerase III β-subunit resulting in enhanced efficacy.
{"title":"Synergistic effects of new lactone polyketides from an endophytic fungus Phomopsis sp. XP-8 with antibiotics","authors":"Hao Ren , Yamei Miao , Desire Girimpuhwe, Jianjin Guo, Shuxian Ge, Wei Zhang, Ge-Ge Yang, Shang Liu, Quan-Xiang Wu","doi":"10.1016/j.fitote.2025.107045","DOIUrl":"10.1016/j.fitote.2025.107045","url":null,"abstract":"<div><div>Six new polyketides, including three naphthalene-types (<strong>1</strong>–<strong>3</strong>) and three <em>γ</em><strong>-</strong>lactones<strong>-</strong>types (<strong>4</strong>–<strong>6</strong>), along with 14 known polyketides (<strong>7</strong>–<strong>20</strong>), were isolated from a pathogen endophytic fungus <em>Phomopsis</em> sp. XP-8 of <em>Eucommia ulmoides Oliver</em>. Their structures were elucidated by spectrometric analysis using MS and NMR data. The absolute configurations were established using statistical comparative analysis of the experimental ECD data, in conjunction with quantum mechanical calculations. All the compounds and crude extracts were evaluated for their antibacterial activity. Compounds <strong>2</strong>, <strong>3</strong>, <strong>6, 7</strong>, <strong>8</strong>, and <strong>10</strong> exhibited moderate inhibition on three gram-positive bacteria, <em>Staphylococcus aureus</em>, <em>Bacillus subtilis,</em> and <em>Bacillus thuringiensis</em>. Synergistic antibacterial interaction experiments showed that compounds <strong>1</strong>, <strong>2</strong>, <strong>3</strong>, <strong>6</strong>, <strong>7</strong>, <strong>8</strong>, and <strong>19</strong> with antibiotics can greatly enhance the inhibition rate against bacteria. The target screening and molecular docking of these compounds were also carried out, with further verification of molecular dynamics, revealing that the compounds exert antibacterial activity by targeting both the Fur-regulated basic protein (FbpB) and drug resistance protein D (EmrD), exhibiting synergy with antibiotics by inhibiting the DNA polymerase III <em>β</em>-subunit resulting in enhanced efficacy.</div></div>","PeriodicalId":12147,"journal":{"name":"Fitoterapia","volume":"188 ","pages":"Article 107045"},"PeriodicalIF":2.6,"publicationDate":"2025-12-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145803695","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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