薯蓣皂苷元衍生物的合成和抗肿瘤活性研究

Synthesis and Anticancer Activity Study of Diosgenin Derivatives

目的合成薯蓣皂苷元衍生物并研究其体外抗肿瘤活性。方法以薯蓣皂苷元为原料,选择性地合成一系列运用AutoDock4.2对接设计的薯蓣皂苷元衍生物。采用噻唑蓝(MTT)法考察了目标化合物对人恶性黑色素瘤细胞A375、人肺腺癌细胞A549、人肝癌细胞HepG-2以及人慢性髓原白血病细胞K562进行体外抗肿瘤活性试验。结果合成12个新化合物,其结构经1H-NMR和13C-NMR确定,药理实验结果表明,大部分化合物有一定的抗肿瘤活性。结论大部分化合物有良好的抗肿瘤活性而对正常细胞无毒或低毒性。

OBJECTIVE To synthesize diosgenin derivatives and investigate their anti-tumor activities in vitro. METHODS Designed and docked by AutoDock4. 2, a series of diosgenin derivatives were selectively prepared from diosgenin. Their anti-tumor activities in vitro were evaluated for human malignant melanoma A375 cells, human lung adenocarcinoma A549 ceils, human hepatoma HepG-2 cells and human myeloid leukemia K562 cells by MTY assay. RESULTS Twelve novel compounds were synthesized and the basic structures were characterized by I H-NMR and 13C-NMR. MTT assay showed that most of the diosgenin derivatives exhibited some anti-tumor activities. CONCLUSION Most of the synthesized compounds had certain antitumor activity and showed no or little toxicity against the normal ceils.