目的 合成并表征α-常春藤皂苷一氧化氮供體衍生物，并對其抗腫瘤活性進行研究。方法 采用苯硫酚作為起始原料，以不同長度的二醇作為連接臂，將α-常春藤皂苷的28位羧基和呋咱氮氧化物連接在一起得到α-常春藤皂苷一氧化氮供體衍生物；并采用MTT法對目標化合物進行體外抗乳腺癌活性研究。結果 合成了4個α-常春藤皂苷一氧化氮供體衍生物，其結構均通過¹H-NMR和MS確證。生物活性結果測試表明其抗腫瘤活性均優(yōu)于陽性對照藥α-常春藤皂苷。結論 α-常春藤皂苷一氧化氮供體衍生物抗腫瘤活性明顯，具有很好的開發(fā)價值。

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.

江西省衛(wèi)計委中醫(yī)藥課題資助項目（2015A245）