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 (IC(50) = 1.2–4.7 and 1.7–4.5 μM, respectively) against five h...

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Detalles Bibliográficos
Autores principales: Fang, Yuanying, Hu, Daoyong, Li, Huilan, Hu, Jianguo, Liu, Yanhua, Li, Zhifeng, Xu, Guoliang, Chen, Lanying, Jin, Yi, Yang, Shilin, Yang, Zunhua
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Frontiers Media S.A. 2019
Materias:
Pharmacology
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6804646/
https://www.ncbi.nlm.nih.gov/pubmed/31680978
http://dx.doi.org/10.3389/fphar.2019.01208
Descripción
Sumario: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(50) = 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(1) phase and apoptosis in HCT-116 cells.

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