%A Fang,Yuanying
%A Hu,Daoyong
%A Li,Huilan
%A Hu,Jianguo
%A Liu,Yanhua
%A Li,Zhifeng
%A Xu,Guoliang
%A Chen,Lanying
%A Jin,Yi
%A Yang,Shilin
%A Yang,Zunhua
%D 2019
%J Frontiers in Pharmacology
%C
%F
%G English
%K Pulsatilla saponin D,Synthesis,Antiproliferative activity,acute toxicity,Apoptosis
%Q
%R 10.3389/fphar.2019.01208
%W
%L
%M
%P
%7
%8 2019-October-15
%9 Original Research
%+ Guoliang Xu,Research Center for Differentiation and Development of Basic Theory of Traditional Chinese Medicine, Jiangxi University of Traditional Chinese Medicine,China,xuguoliang6606@126.com
%+ Zunhua Yang,College of Pharmacy, Jiangxi University of Traditional Chinese Medicine,China,xuguoliang6606@126.com
%#
%! Pulsatilla Saponin D derivatives as promising anticancer agents
%*
%<
%T Synthesis, Biological Evaluation, and Mode of Action of Pulsatilla Saponin D Derivatives as Promising Anticancer Agents
%U https://www.frontiersin.org/articles/10.3389/fphar.2019.01208
%V 10
%0 JOURNAL ARTICLE
%@ 1663-9812
%X A series of ester and amide derivatives of triterpenoid saponin Pulsatilla saponin D (PSD) were designed, synthesized, and evaluated for their antiproliferative activity. Compounds 1 and 6 displayed 1.7–8.3 times more potent cytotoxicity (IC50 = 1.2–4.7 and 1.7–4.5 μM, respectively) against five human tumor cell lines (SMMC-7721, MCF-7, NCI-H460, A549, and HCT-116) in vitro and lower acute toxicity to mice in vivo than did PSD. Furthermore, compound 6 was observed to show potent tumor growth inhibition against mice H22 hepatocellular cells (49.8% at 20 mg/kg) and induce cell cycle at G1 phase and apoptosis in HCT-116 cells.