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Synthesis, Biological Evaluation, and Mode of Action of Pulsatilla Saponin D Derivatives as Promising Anticancer Agents.

Authors :
Fang, Yuanying
Hu, Daoyong
Li, Huilan
Hu, Jianguo
Liu, Yanhua
Li, Zhifeng
Xu, Guoliang
Chen, Lanying
Jin, Yi
Yang, Shilin
Yang, Zunhua
Source :
Frontiers in Pharmacology; 10/15/2019, p1-9, 9p
Publication Year :
2019

Abstract

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 (IC<subscript>50</subscript> = 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 G<subscript>1</subscript> phase and apoptosis in HCT-116 cells. [ABSTRACT FROM AUTHOR]

Details

Language :
English
ISSN :
16639812
Database :
Complementary Index
Journal :
Frontiers in Pharmacology
Publication Type :
Academic Journal
Accession number :
139144330
Full Text :
https://doi.org/10.3389/fphar.2019.01208