【摘要】 自印度马兜铃（Aristolochia indica L.）中提得的马兜铃次酸（Aris-tolic acid）（Ⅰ）及其甲酯,经动物实验证明具有较好的抗着床和引产作用。为了寻找结构简化、活性更强的抗生育药,我们合成了马兜铃次酸开环衍生物(Ⅱ_1-8)。鉴于对-羟基苯丙烯酸类化合物亦有抗生育作用,因此将五个苯丙烯酸型中间体作为Ⅲ_1-5化合物。初步药理试验表明:Ⅱ类化合物无抗着床和抗旱孕作用。化合物Ⅲ₁和Ⅲ₂分别具有显著的抗早孕和抗着床作用（P<0.01,P<0.05）,Ⅲ₄兼有上述二种作用（P<0.01）。这说明菲环破裂后,抗生育活性消失,而具有苯丙烯酸型结构的中间体仍能保持抗生育作用。更多还原

【Abstract】 It was reported that aristolic acid, an active principle isolated from the rootof Aristolochia indica L., showed anti-implantation effect in mice and abortioneffect in female albino rabbits, and its methyl ester also exerted abortifacientactivity in mice. In order to search for new antifertility agents with simplerstructure and stronger activity, eight ring opening derivatives of aristolic acid（Ⅱ 1-8）were synthesized. All the compounds and fheiv iatermediates（Ⅲ 1-5） havecis-stilbene configuration and have not been reported in literature. Considering that p-coumaric acid also exhibited antifertility activity, five inter-mediates with such chemical feature and the eight ring opening derivatives weresubjected to Pharmacological test, none of the compounds （Ⅱ1-8）showed antifer-tility activity in mice. It seemed that aristolic acid lost its activity by openingthe phenanthrene ring. The intermediates Ⅲ₁ and Ⅲ₂ exerted significant action oftermination of early pregnancy and anti-implantation respectively, Ⅲ₄ showedthe both effects in mice.更多还原