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

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 hum...

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Main Authors: Yuanying Fang (Author), Daoyong Hu (Author), Huilan Li (Author), Jianguo Hu (Author), Yanhua Liu (Author), Zhifeng Li (Author), Guoliang Xu (Author), Lanying Chen (Author), Yi Jin (Author), Shilin Yang (Author), Zunhua Yang (Author)
Format: Book
Published: Frontiers Media S.A., 2019-10-01T00:00:00Z.
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Summary: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.
Item Description:1663-9812
10.3389/fphar.2019.01208

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