期刊
FITOTERAPIA
卷 125, 期 -, 页码 33-40出版社
ELSEVIER
DOI: 10.1016/j.fitote.2017.12.014
关键词
Tigogenin; Neoglycosylation; Steroidal saponins; Glycosylalkoxylamines
资金
- National Nature Science Foundation of China (NSFC) [21302052]
- Program for New Century Excellent Talents in University
- '111 Project' from the Ministry of Education of China [B16046]
- Natural Science Foundation of Jiangsu Province [BK20141243]
- Postgraduate Research & Practice Innovation Program of Jiangsu Province [KYCX17_0696]
To discover new potent cytotoxic steroidal saponins, a series of tigogenin neoglycosides were synthesized via oxyamine neoglycosylation for the first time. The preliminary bioassays for their in vitro antitumor activities against five human cancer cell lines (A375, A-549, HCT-116, HepG2 and MCF-7) were conducted. The results revealed a sugar-dependent activity profile of their cytotoxicity, the glycoconjugation converted the non-active tigogenin to the most potential product Tg29 ((3R)-N-methoxyamino-tigogenin-beta-2-deoxy-D-galactoside) with IC50 value of 2.7 mu M and 4.6 mu M against HepG2 and MCF-7 cells respectively. And the 3R-tigogenin neoglycosides exhibited enhanced antitumor activity while the 3S-tigogenin almost showed no activity. Among the five cell lines, HepG2 and MCF-7 cells showed more sensitive cytotoxic responses to the products. Therefore, the neoglycosylation could be a promising strategy for the synthesis of antitumor steroidal saponins and it also proved the essential role of carbohydrate moiety of steroidal saponins in the biological activity.
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