α－双炔失碳酯及其代谢产物双炔失碳醇的体外抗肿瘤作用比较

COMPARISON OF ANTITUMOR EFFECT OF α-ANORDRIN AND ITS METABOLITE AF-45

双块失碳酯是国内常用的探亲避孕药，它的α异构体在体内外有明显的抗癌活性。本文比较了α－双炔失碳酯及其体内代谢产物双炔失碳醇的体外抗癌作用。结果表明，α－双块失碳酯对体外培养的六种肿瘤细胞株的生长抑制作用均比双炔失碳醇强一倍左右，其对ＨｅｐＡ细胞ＤＮＡ和ＲＮＡ合成的抑制作用亦强于双炔失碳醇，因此，至少从体外实验来看，双炔失碳醇并非α小双炔失碳酯的抗癌活性产物。

α-Anordrin, a contraceptive, was previously found to possess antitumor activity.In this report,we compared the in vitro antitumor activity of α-anordrin and its metabolite AF-45. α-Anordrin and AF-45 showed an inhibitory action against a number of tumor cell lines and the inhibitory effect of α-anordrin was twice stronger than that of AF-45. They both showed obvious inhibition on RNA and DNA synthesis of Hep A cells, however α-anordrin was also stronger than AF-45. It indicates that AF-45 is not an active antitumor metabolite of α-anordrin.*AF-45=2a, 17α-diethynyl-A-nor-androstane-2β,17β-diol