2,3-二羟基-甘草次酸酯类化合物的合成及其抗肿瘤活性

Synthesis and Antitumor Activity of 2,3-Dihydroxy-glycyrrhetinic Acid Esters

对甘草次酸30位和A环结构改造,经酯化、消除、环氧化、水解开环得到2,3-二羟基-甘草次酸酯类化物(6a~6e)。所合成化合物的结构经IR、MS、^(1)HNMR表征。采用SRB法,测定6a~6e对人乳腺癌细胞(MCF-7)、人肺癌细胞(A549)的体外细胞毒活性。其中6a、6c、6d对MCF-7的抑制作用显著,IC_(50)分别为4.36、8.37、6.54μmol·L^(-1)。

The 30-position and A-ring structure of glycyrrhetinic acid were modified,and 2,3-dihydroxy-glycyrrhetinic acid esters(6a~6e)were obtained by esterification,elimination,epoxidation and hydrolysis.The structures of the synthesized compounds were characterized by IR,MS and ^(1)HNMR.Human land breast cancer cell(MCF-7)and lung cancer cells(A549)were selected to test the cytotoxicity of 6a~6e in vitro by SRB method.6a,6c and 6d had obvious inhibitory effects on MCF-7 with IC_(50)of 4.36μmol·L^(-1),8.37μmol·L^(-1)and 6.54μmol·L^(-1),respectively.