茺蔚子萜类化学成分及其抗炎活性研究  

Terpenoids from Fructus Leonuri and Their Anti-Inflammatory Activities

作　　者：范云秋 彭成[1,2] 熊亮 周勤梅[1,2,3] 彭芳 何育霖[1,2] 敖慧 戴鸥 FAN Yun-qiu;PENG Cheng;XIONG Liang;ZHOU Qin-mei;PENG Fang;HE Yu-lin;AO Hui;DAI Ou(State Key Laboratory of Southwestern Chinese Medicine Resources,College of Pharmacy,Chengdu University of Traditional Chinese Medicine,Chengdu 611137,China;Institute of Innovative Medicine Ingredients of Southwest Specialty Medicinal Materials,Chengdu University of Traditional Chinese Medicine,Chengdu 611137,China;Institute of Traditional Chinese Medicine Innovation,Chengdu University of Traditional Chinese Medicine,Chengdu 611137,China)

机构地区：[1]成都中医药大学药学院,省部共建西南特色中药资源国家重点实验室,成都611137 [2]成都中医药大学西南特色药材创新药物成分研究所,成都611137 [3]成都中医药大学中医药创新研究院,成都611137

出　　处：《中国药学杂志》2023年第7期571-575,共5页Chinese Pharmaceutical Journal

基　　金：国家自然科学基金面上项目资助(81872991);国家自然科学基金“联合基金重点支持项目”资助(U19A2010);四川省应用基础研究项目资助(2019YJ0334);成都中医药大学“杏林学者”学科人才提升计划资助(YXRC2018005)。

摘　　要：目的 研究茺蔚子中的化学成分及其抗炎活性。方法 采用大孔吸附树脂、硅胶柱色谱以及半制备HPLC等多种色谱方法对其化学成分进行分离纯化,结合化合物的理化性质及NMR和MS等波谱数据鉴定化合物结构。通过测定化合物对脂多糖(lipopolysaccharide, LPS)诱导RAW 264.7巨噬细胞释放一氧化氮(NO)的抑制能力来评价化合物的抗炎活性。结果 从茺蔚子正丁醇提取部位中共分离得到4个萜类化合物,含1个新化合物,结构分别鉴定为(-)-(5R,6S,8R)-5,6-二羟基-二氢猕猴桃内酯(1)、蜜柑苷A(2)、淫羊藿次苷C3(3)、益母草宁素K(4)。活性筛选结果表明,化合物4对LPS诱导RAW264.7细胞释放NO具有明显的抑制作用。结论 化合物1是新化合物,化合物3是首次在益母草属植物中分离得到,化合物2和4是首次从茺蔚子中分离得到。化合物4可以显著抑制LPS诱导的RAW264.7细胞的NO释放,具有潜在的抗炎作用。OBJECTIVE To investigate the chemical constituents of Fructus Leonuri and their anti-inflammatory activities.METHODS The chemical constituents were isolated and purified by column chromatography over macroporous adsorption resin and silica gel,as well as semi-preparative HPLC.Their structures were identified by physicochemical properties and NMR and MS data.The anti-inflammatory activities of the compounds were evaluated by measuring their inhibitory effects on nitric oxide(NO)release in LPS induced RAW 264.7 macrophages.RESULTS Four terpenoids were isolated from the n-butanol extract of Fructus Leonuri,including a new compound.Their structures were identified as(-)-(5R,6S,8R)-5,6-dihydroxy-dihydroactinidiolide(1),citroside A(2),icariside C3(3),and leojaponin K(4).CONCLUSION Compound 1 is a new terpenoid.Compound 3 is isolated from the genus Leonurus for the first time.Compounds 2 and 4 are isolated from Fructus Leonuri for the first time.Among them,compound 4 cound inhibit NO release significantly in LPS-induced RAW264.7 cells,suggesting that it has a potential anti-inflammatory effect.

关 键 词：茺蔚子 (-)-(5R 6S 8R)-5 6-二羟基-二氢猕猴桃内酯 萜 抗炎活性 

分 类 号：R282[医药卫生—中药学]