浙江香茶菜属植物抗肿瘤活性成分的比较研究及药效物质的快速发现  

Comparative Study on Antineoplastic Active Components and Rapid Detection of Pharmacodynamic Substances of Lamiaceae Isodon from Zhejiang Province

作　　者：滕飞 杨波[1] 林能明 TENG Fei;YANG Bo;LIN Nengming(College of Pharmaceutical Sciences,Zhejiang Chinese Medical University,Hangzhou(310053),China;Key Laboratory of Clinical Cancer Pharmacology and Toxicology Research of Zhejiang Province,Affiliated Hangzhou First People's Hospital,Zhejiang University School of Medicine;Translational Medicine Research Center,Affilialed Hangzhou First People's Hospital,Zhejiang University School of Medicine)

机构地区：[1]浙江中医药大学药学院,杭州310053 [2]浙江大学医学院附属杭州市第一人民医院浙江省临床肿瘤药理与毒理学研究重点实验室 [3]浙江大学医学院附属杭州市第一人民医院转化医学研究中心

出　　处：《浙江中医药大学学报》2020年第3期297-302,共6页Journal of Zhejiang Chinese Medical University

基　　金：杭州市科技发展计划项目(20172016A01);浙江省省级重点实验室培育项目(2020E10021)。

摘　　要：[目的]比较香茶菜属植物体外抗肿瘤成分及作用的差异,初步阐明其抗肿瘤药效物质。[方法]制备香茶菜属植物地上和地下部分乙酸乙酯提取物,以薄层色谱(thin layer chromatography,TLC)分析研究香茶菜属植物及其不同入药部位的成分差异;MTT法研究不同样品对人源乳腺癌细胞MCF-7的抑制作用,筛选出具有体外抗肿瘤活性的香茶菜属植物种类及入药部位;以有效乙酸乙酯提取物与还原型谷胱甘肽(glutathione,GSH)共同孵育,超高效液相色谱(ultra performance liquid chromatography,UPLC)分析孵育前后成分的变化,推测其可能的抗肿瘤药效物质的化学结构类别。[结果]TLC分析显示,浙江香茶菜属不同种植物地上与地下部分之间化学成分存在差异,其中香茶菜[Isodon amethystoides(Bentham)H.Hara]、大萼香茶菜[Isodon macrocalyx(Miquel)Kud觝]与本属其他植物对比成分明显不同;对MCF-7细胞抑制作用最好的是大萼香茶菜的地上部分,半数抑制浓度(50%inhibiting concentration,IC50)为8.29μg·m L-1;UPLC分析显示,该样品中存在能够与GSH结合的成分,可能为迈克尔受体分子型二萜类成分。[结论]浙江产大萼香茶菜的地上部分具有较强抗肿瘤作用,初步确定其抗肿瘤药效物质为迈克尔受体分子型二萜类成分。[Objective]To compare the in vitro antitumor activity and components of Lamiaceae Isodon,and to elucidate the antitumor pharmacodynamic substances of Lamiaceae Isodon.[Methods]The ethyl acetate extracts of aboveground and underground parts of Lamiaceae Isodon were prepared,and thin layer chromatography(TLC)was used to study the composition differences of their different medicinal parts.MTT method was used to study the inhibitory effect of different samples on human breast cancer cell MCF-7,and to screen out the species and drug sites with anti-tumor activity in vitro.Effective ethyl acetate extract was incubated with reduced glutathione(GSH),and the changes of components before and after incubation were analyzed by ultra performance liquid chromatography(UPLC),so as to determine the possible chemical structure categories of anti-tumor efficacy substances.[Results]The chemical compositions of aboveground and underground parts of Lamiaceae Isodon are different,especially,Isodon amethystoides(Bentham)H.Hara and Isodon macrocalyx(Miquel)Kudo are significantly different from other plants of the genus.The best inhibitory effect on MCF-7 cells was found in the aboveground part of Isodon macrocalyx,50%inhibiting concentration(IC50)was 8.29μg·m L-1.UPLC analysis showed that GSH binding components were present in the sample,which might be Michael acceptor molecular diterpenoids.[Conclusion]In this study,it was found by screening that the aboveground part of Lamiaceae Isodon from Zhejiang Province had strong antitumor effect,and its antitumor active substance was Michael acceptor molecular diterpenoids.

关 键 词：香茶菜属 迈克尔受体分子 抗肿瘤活性 超高效液相色谱 成分差异 

分 类 号：R282[医药卫生—中药学]