AUTHOR=Fang Yuanying , Hu Daoyong , Li Huilan , Hu Jianguo , Liu Yanhua , Li Zhifeng , Xu Guoliang , Chen Lanying , Jin Yi , Yang Shilin , Yang Zunhua 

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

JOURNAL=Frontiers in Pharmacology

VOLUME=10

YEAR=2019

URL=https://www.frontiersin.org/journals/pharmacology/articles/10.3389/fphar.2019.01208

DOI=10.3389/fphar.2019.01208

ISSN=1663-9812

ABSTRACT=<p>A series of ester and amide derivatives of triterpenoid saponin <italic>Pulsatilla</italic> 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<sub>50</sub> = 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) <italic>in vitro</italic> and lower acute toxicity to mice <italic>in vivo</italic> 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<sub>1</sub> phase and apoptosis in HCT-116 cells.</p>