目的 合成并表征α-常春藤皂苷一氧化氮供体衍生物，并对其抗肿瘤活性进行研究。方法 采用苯硫酚作为起始原料，以不同长度的二醇作为连接臂，将α-常春藤皂苷的28位羧基和呋咱氮氧化物连接在一起得到α-常春藤皂苷一氧化氮供体衍生物；并采用MTT法对目标化合物进行体外抗乳腺癌活性研究。结果 合成了4个α-常春藤皂苷一氧化氮供体衍生物，其结构均通过¹H-NMR和MS确证。生物活性结果测试表明其抗肿瘤活性均优于阳性对照药α-常春藤皂苷。结论 α-常春藤皂苷一氧化氮供体衍生物抗肿瘤活性明显，具有很好的开发价值。

Objective To synthesize and characterize nitric oxide-donating derivatives of α-hederin, and evaluate their anti-cancer effect in vivo. Methods Thiophenol was used as the starting materials. Glycol with different chain lengths was the linker, and the 28-carboxyl group was connected with furoxans to synthesize nitric oxide-donating derivatives of α-hederin. The anti-breast cancer activities were determined by MTT assays.Results The four nitric oxide-donating derivatives of α-hederin were synthesized and the structures had been confirmed by ¹H-NMR and MS spectra. The biological results showed that they displayed the better biological effect than α-hederin. Conclusion The nitric oxide-donating derivatives of α- hederin have good antitumor activities, which has the further development value.

江西省卫计委中医药课题资助项目（2015A245）