Syntheses and anti-cancer activities of glycosylated derivatives of diosgenin
Syntheses and anti-cancer activities of glycosylated derivatives of diosgenin
复制标题
薯蓣皂苷元糖基化衍生物的合成及其抗癌活性
DOI：
10.1007/s40242-016-6296-y
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发表时间：
2017-02
期刊：
影响因子：
--
通讯作者：
PAN Weidong
中科院分区：
文献类型：
--
作者：
TAN Yonghua;XIAO Xiao;YAO Jianing;HAN Fei;LOU Huayong;LUO Heng;LIANG Guangyi;BEN-DAVID Yaacov;PAN Weidong
为了获得更好的抗癌化合物，以薯蓣皂苷元为原料，设计合成了9个糖基化衍生物。它们的结构经1H NMR、13 C NMR和MS确证。采用MTT法研究了中间体化合物5a ~ 5i和目标化合物6a ~ 6 i对人白血病细胞系HEL、K562、HL 60和黑色素瘤细胞系WM 9的抗肿瘤活性。生物活性测试结果表明，这些衍生物对四种癌细胞株均具有较好的抑制活性。此外，这些衍生物对K562的抑制活性优于对其他细胞系的抑制活性，并且大多数衍生物的抑制活性优于亲本材料。此外，当对抗这些细胞时，化合物6a-6 i比它们的中间体5a-5i更有活性。上述结果表明薯蓣皂苷元3-OH的糖基化和糖基的乙酰化对其抗肿瘤活性的影响。
In order to obtain better anti-cancer compounds, nine glycosylated derivatives were designed and synthe-sized using diosgenin as starting material. Their structures were confirmed by1H NMR,13C NMR and MS spectra. The anti-cancer activities of intermediate compounds5a—5i and the target compounds6a—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, compounds6a—6i are more active than their inter-mediates5a—5i when against these cells. The above results demonstrate the effects of glycosylation on 3-OH of di-osgenin and acetylation of the sugar moiety on their antitumor activities.
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