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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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
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author Fang, Yuanying
Hu, Daoyong
Li, Huilan
Hu, Jianguo
Liu, Yanhua
Li, Zhifeng
Xu, Guoliang
Chen, Lanying
Jin, Yi
Yang, Shilin
Yang, Zunhua
author_facet Fang, Yuanying
Hu, Daoyong
Li, Huilan
Hu, Jianguo
Liu, Yanhua
Li, Zhifeng
Xu, Guoliang
Chen, Lanying
Jin, Yi
Yang, Shilin
Yang, Zunhua
author_sort Fang, Yuanying
collection PubMed
description 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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spelling pubmed-68046462019-11-03 Synthesis, Biological Evaluation, and Mode of Action of Pulsatilla Saponin D Derivatives as Promising Anticancer Agents Fang, Yuanying Hu, Daoyong Li, Huilan Hu, Jianguo Liu, Yanhua Li, Zhifeng Xu, Guoliang Chen, Lanying Jin, Yi Yang, Shilin Yang, Zunhua Front Pharmacol Pharmacology 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. Frontiers Media S.A. 2019-10-15 /pmc/articles/PMC6804646/ /pubmed/31680978 http://dx.doi.org/10.3389/fphar.2019.01208 Text en Copyright © 2019 Fang, Hu, Li, Hu, Liu, Li, Xu, Chen, Jin, Yang and Yang http://creativecommons.org/licenses/by/4.0/ This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) and the copyright owner(s) are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.
spellingShingle Pharmacology
Fang, Yuanying
Hu, Daoyong
Li, Huilan
Hu, Jianguo
Liu, Yanhua
Li, Zhifeng
Xu, Guoliang
Chen, Lanying
Jin, Yi
Yang, Shilin
Yang, Zunhua
Synthesis, Biological Evaluation, and Mode of Action of Pulsatilla Saponin D Derivatives as Promising Anticancer Agents
title Synthesis, Biological Evaluation, and Mode of Action of Pulsatilla Saponin D Derivatives as Promising Anticancer Agents
title_full Synthesis, Biological Evaluation, and Mode of Action of Pulsatilla Saponin D Derivatives as Promising Anticancer Agents
title_fullStr Synthesis, Biological Evaluation, and Mode of Action of Pulsatilla Saponin D Derivatives as Promising Anticancer Agents
title_full_unstemmed Synthesis, Biological Evaluation, and Mode of Action of Pulsatilla Saponin D Derivatives as Promising Anticancer Agents
title_short Synthesis, Biological Evaluation, and Mode of Action of Pulsatilla Saponin D Derivatives as Promising Anticancer Agents
title_sort synthesis, biological evaluation, and mode of action of pulsatilla saponin d derivatives as promising anticancer agents
topic Pharmacology
url 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
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