Syntheses and Anti-cancer Activities of Glycosylated Derivatives of Diosgenin  

作　　者：TAN Yonghua XIAO Xiao YAO Jianing HAN Fei LOU Huayong LUO Heng LIANG Guangyi BEN-DAVID Yaacov PAN Weidong 

机构地区：[1]Key Laboratory of Chemistry for Natural Products of Guizhou Province and Chinese Academy of Sciences, Guiyang 550002, P R. China [2]Key Laboratory of Chemistry for Natural Products of Guizhou Medical University, Guiyang 550001, P. R. China

出　　处：《Chemical Research in Chinese Universities》2017年第1期80-86,共7页高等学校化学研究（英文版）

基　　金：Supported by the National Natural Science Foundation of China（Nos.81360479, 81472609） and the Project of the Science and Technology Department of Guizhou Province, China（Nos.QKHRC[2016]4037,QKHRCTD[2015]4026, QKHJZ[2014]2099）.

摘　　要：In order to obtain better anti-cancer compounds, nine glycosylated derivatives were designed and synthe- sized using diosgenin as starting material. Their structures were confn-med by 1H NMR, 13C NMR and MS spectra. The anti-cancer activities of intermediate compounds 5a-5i and the target compounds 6a-6i were investigated against human leukemia HEL, K562, HL60 and melanoma WM9 cell lines via MTT method. The bioassay results show that these derivatives possess good inhibitory activities against the four cancer cell lines. Furthermore, these derivatives show better inhibitory activities against K562 than against other cell lines, and most derivatives show better inhibitory activities than the parental material. Moreover, compounds 6a--6i are more active than their inter- mediates 5a--5i when against these ceils. The above results demonstrate the effects of glycosylation on 3-OH of di- osgenin and acetylation of the sugar moiety on their antitumor activities.In order to obtain better anti-cancer compounds, nine glycosylated derivatives were designed and synthe- sized using diosgenin as starting material. Their structures were confn-med by 1H NMR, 13C NMR and MS spectra. The anti-cancer activities of intermediate compounds 5a-5i and the target compounds 6a-6i were investigated against human leukemia HEL, K562, HL60 and melanoma WM9 cell lines via MTT method. The bioassay results show that these derivatives possess good inhibitory activities against the four cancer cell lines. Furthermore, these derivatives show better inhibitory activities against K562 than against other cell lines, and most derivatives show better inhibitory activities than the parental material. Moreover, compounds 6a--6i are more active than their inter- mediates 5a--5i when against these ceils. The above results demonstrate the effects of glycosylation on 3-OH of di- osgenin and acetylation of the sugar moiety on their antitumor activities.

关 键 词：DIOSGENIN GLYCOSYLATION Anti-cancer activity 

分 类 号：O[理学]