Chemical constituents isolated from the aerial parts of Swertia pseudochinensis and their potential neuroprotective effects  

从瘤毛獐牙菜中分离的化学成分及其潜在的神经保护作用

作　　者：Ke Xiang Qi He Yanmei Chen Dongxin Yang Yanwei Duan Hua Li Lixia Chen 项珂;何琪;陈彦梅;杨栋鑫;段衍伟;李华;陈丽霞(沈阳药科大学无涯创新学院基于靶点的药物设计与研究教育部重点实验室,沈阳110016;华中科技大学同济医学院药学院,湖北省天然药物化学与资源评价重点实验室,武汉430030)

机构地区：[1]Wuya College of Innovation,Key Laboratory of Structure-Based Drug Design&Discovery,Ministry of Education,Shenyang Pharmaceutical University,Shenyang,China [2]Hubei Key Laboratory of Natural Medicinal Chemistry and Resource Evaluation,School of Pharmacy,Tongji Medical College,Huazhong University of Science and Technology,Wuhan,China

出　　处：《Acupuncture and Herbal Medicine》2021年第1期59-64,共6页针灸和草药（英文）

基　　金：financially supported by the Liaoning Revitalization Talents Program(No.XLYC1807182);the Liaoning Province Natural Science Foundation(No.2019-MS-299).

摘　　要：Objective:Swertia pseudochinensis,an annual herb of the genus Swertia in the family Gentianaceae.Some constituents and extracts from the Swertia genus have been recently reported to possess neuroprotective effects,suggesting their potential utility in the prevention and treatment of Parkinson disease(PD).The aim of this work is to identify the chemical constituents and evaluate the potential biological activists of Swertia pseudochinensis.Methods:The phytochemicals from the aerial parts of S.pseudochinensis were isolated and purified by silica gel,Sephadex LH-20 gel,semi-preparative high-performance liquid chromatography,and identified by the spectroscopic methods.All compounds were evaluated for their potential neuroprotective effects against 1-methyl-4-phenylpyridinium-induced apoptosis in the SH-SY5Y human neuroblastoma cell line using the 3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide assay.Then,we performed an enrichment analysis using the Database for Annotation,Visualization,and Integrated Discovery and investigated the mechanisms by which bellidifolin regulates neurodegenerative disease.Results:Two new anthraquinone,1,5,6-trimethoxy-2-hydroxy-3-methy-anthraquinone(1)and 1,5,6,8-tetramethoxy-2-hydroxy-3-methyanthraquinone(2),together with nine known including 7-O-b-d-glucopyranosyl-1,8-dihydroxy-3-methoxyxanthone(3),gentisin(4),swertianolin(5),bellidifolin(6),gentiacaulein(7),norswertianolin(8),5-O-b-d-glucopyranosyl-1,3,8-trihydroxyapatone(9),1-hydroxy-3,5,8-trimethoxyxanthone(10),and aurantio-obtusin(11),were isolated and compounds 6–8 and 10 exhibited neuroprotective effects at a concentration of 50mmol/L.Among them,bellidifolin showed significant protective activity,and might have potential as a neuroprotective agent for the treatment of PD,possibly by acting on oxidative damage and reactive oxygen species.Conclusions:These findings indicate that further research on the genus Swertia and its bioactive constituents toward neurodegenerative disorders could be extremely rewarding.目的:瘤毛獐牙菜,是龙胆科獐芽菜属的一年生草本植物。最近有报道称,獐牙菜属的一些成分和提取物具有神经保护作用,这表明它们在预防和治疗帕金森病(PD)中具有潜在的应用价值。本研究的目的是鉴定瘤毛獐牙菜的化学成分和评价潜在的生物活性分子。方法:该研究通过用硅胶、葡聚糖凝胶、半制备HPLC分离纯化化学物质,并用光谱法进行结构鉴定。采用MTT法评估所有化合物对1-甲基-4-苯基吡啶诱导的SH-SY5Y人神经母细胞瘤细胞凋亡的潜在神经保护作用。使用注释、可视化和整合发现数据库(David)进行了富集分析,并研究了化合物6调节神经退行性疾病的机制。鉴定瘤毛獐牙菜的化学成分和评价潜在的生物活性分子。结果:分离出两种新的蒽醌类(1,2)和9种已知化合物(3-11),化合物6-8和10在50μmol/L浓度下表现出神经保护作用。其中化合物6表现出显著的保护活性,可能通过作用于氧化损伤和活性氧而成为潜在的治疗PD的神经保护剂。结论:这些结果表明,进一步研究獐牙菜属及其活性成分对神经退行性疾病的治疗具有重要意义。

关 键 词：ANTHRAQUINONE Neuroprotective effect Parkinson disease Swertia pseudochinensis XANTHONE 

分 类 号：R284[医药卫生—中药学] R285[医药卫生—中医学]