羟基丹参酮ⅡA的合成及体外抗肿瘤作用  

Synthesis and in vitro Anti-Tumor Effects of Hydroxytanshinone ⅡA

作　　者：张丽娟[1] 徐文清[1] 江城峰 杨福军[1] 沈秀[1] 

机构地区：[1]中国医学科学院放射医学研究所天津市放射医学与分子核医学重点实验室,天津300192

出　　处：《天然产物研究与开发》2015年第12期2027-2030,2089,共5页Natural Product Research and Development

基　　金：国家自然科学基金(81273005);天津市应用基础与前沿技术研究重点项目(14JCZDJC36400);中国医学科学院放射医学研究所发展基金(SF1528)

摘　　要：对丹参酮ⅡA进行结构修饰,合成了羟基丹参酮ⅡA。采用MTT法考察了羟基丹参酮ⅡA对人宫颈癌细胞株Hela细胞,人肝癌细胞株HepG-2细胞、人胃癌细胞株SGC-7901细胞的增殖抑制作用。结果表明:羟基丹参酮ⅡA对三种肿瘤细胞增殖都有很好的抑制作用,抑制作用呈剂量依赖性。羟基丹参酮ⅡA对SGC-7901细胞抑制作用最强,其IC_(50)为4.18μM;对HeLa细胞的抑制作用次之,其IC_(50)为6.08μM;对HepG-2细胞抑制作用较弱,其IC_(50)为10.20μM。而丹参酮ⅡA对SGC-7901细胞、HeLa细胞和HepG-2细胞的IC_(50)分别是17.15μM、27.28μM和46.34μM。羟基丹参酮ⅡA抑制肿瘤细胞增殖作用明显强于丹参酮ⅡA(P<0.05)。Hydroxytanshinone IIA was synthesized with tanshinone IIA as lead compound. MTr assay was adopted to evaluate its inhibition effect against Hela, HepG-2 and SGC-7901 cells. Results indicated that hydroxytanshinone IIA inhibited cell proliferation in a dose-dependent manner. The half inhibitory concentrations （IC50） of hydroxytanshinone IIA against SGC-7901, HeLa and HepG-2 cells were 4.18 μM,6.08 μM and 10.20 μM, respectively. But the IC50 of tanshinone IIA against SGC-7901, HeLa and HepG-2 cells were 17.15 μM,27.28 μM and 46.34μM, respectively. The inhibition effect of hydroxytanshinone ILk to SGC-7901 cells was powerful. Compared with tanshinone IIA,hydroxytanshi- none IIA signhqcanfly increased inhibition effect （ P 〈 0.05 ）.

关 键 词：丹参酮IIA 羟基丹参酮IIA HELA细胞 HEPG-2细胞 SGC-7901细胞 

分 类 号：R962[医药卫生—药理学]