三七二醇型皂苷氧化降解产物衍生物的合成及其抗肿瘤活性研究  

Synthesis and Anti-tumor Activity of Derivatives of Oxidation Degradation Products from Panaxadiol Sapogenin

作　　者：蒲洪[1,2] 董成梅[1] 邹澄[1] 赵庆[3] 段文越[1] 陈丹[1] 郭巍怡 胡建林[1] 

机构地区：[1]昆明医科大学药学院暨云南省天然药物药理重点实验室,昆明650500 [2]湖南医药学院药学院,怀化418000 [3]云南中医学院中药学院,昆明650500

出　　处：《天然产物研究与开发》2016年第5期749-753,共5页Natural Product Research and Development

基　　金：国家自然科学基金(81160388);云南省应用基础研究计划(2011FZ097);云南省科技厅与昆明医科大学联合专项(2011FB245)

摘　　要：本研究以三七二醇型皂苷原料,通过琼斯氧化得到化合物1,将化合物1的3位羰基经还原胺化反应转化为氨基得到化合物4,再用化合物4与酰化试剂反应得到化合物5~8,此外还通过其它两种反应得到化合物2和3,总共8个化合物,其中6个化合物未见文献报道,结构均经过核磁共振、质谱确证。所得化合物用MTS法对人白血病细胞株HL-60、肝癌细胞株SMMC-7721、肺癌细胞株A-549、乳腺癌细胞株MCF-7、结肠癌细胞株SW480等肿瘤细胞株进行抗肿瘤活性评价。药理活性评价结果显示,化合物3有一定的抗肿瘤活性,值得进一步研究。In this study,Jones oxidation of the did-type saponins of Panax notoginseng afforded compound 1. Its 3-car- bony] group was converted into amino group by reductive amination to give compound 4, and then compound 4 was reacted with acyl reagent to give compounds 5-8. In addition,compounds 2 and 3 were obtained by the other two reactions. The syntheses of the 6 derivatives had not been reported. Their structures were identified by 1H NMR, 13 C NMR and MS. Their in vitro anti-tumor activities against HL-60, SMMC-7721, A-549, MCF-7 and SW480 cancer cells were evaluated by MTS assay. The evaluation results showed that compound 3 had some anti-tumor activity and wass worthy of further study.

关 键 词：三七二醇型皂苷 皂苷元 抗肿瘤活性 

分 类 号：R284.3[医药卫生—中药学] R965.1[医药卫生—中医学]