呋咱氮氧化薯蓣皂苷元拼合物的合成及其抗肿瘤活性研究

摘要

目的:合成强生物活性的薯蓣皂苷元衍生物并探讨其体外抗肿瘤活性.方法:实验通过环加成、缩合、氧化等反应,设计薯蓣皂苷元与呋咱氮氧化物类一氧化氮供体拼合得到目标化合物.并采用噻唑蓝(MTT)法考察目标化合物对HT-29、HepG-2、MCF-7等3种肿瘤细胞株的体外细胞毒性.结果:实验合成了6个新的呋咱氮氧化薯蓣皂苷元拼合物,其结构均经IR、tH NMR和、13C NMR等确证.同时MTT实验结果表明,所合成目标化合物对HT-29、Hepg-2、MCF-7 3种肿瘤细胞均无明显细胞毒性.结论:实验设计的呋咱氮氧化薯蓣皂苷元拼合物合成路径可行,但化合物的无明显抗肿瘤活性,推测化合物NO释放呈低浓度释放,而低浓度NO释放表现为抑制细胞凋亡.%To synthesize a novel diosgenin derivative of nitric oxide and to investigate its antitumor activity in vitro.Methods:Diosgenin was designed to combine with nitric oxide donor of nitric oxide through the cycloaddition,condensation and oxidation reactions,to obtain the target compound.The cytotoxicity on cells of HT-29,HepG-2 and MCF-7,was evaluated by MTT.Results:The 6 new combinations of diosgenin were synthesized,and their structures were confirmed by IR,1H NMR and 13C NMR.At the same time,MTT experiments showed that the target compounds were not obviously cytotoxic to HT-29,HepG2,MCF-7 cells.Conclusion:The synthetic route of the experiment is feasible,but there is no obvious anti-tumor activity of the new compound.It is speculated that the release of NO is low concentration,while the low concentration of NO release inhibits apoptosis.