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作者

Wang, R. Yang, W. Fan, Y. Dehaen, W. Li, Y. Li, H. Wang, W. Zheng, Q. Huai, Q.

作者单位

Zhong Yuan Academy of Biological Medicine, Liaocheng People's Hospital/Affiliated Liaocheng Hospital, Taishan Medical University, Liaocheng, China a Marine College, Shandong University, Weihai, 264209, China School of Marine Science and Technology, Harbin Institute of Technology at Weihai, Weihai, 264209, China Molecular Design and Synthesis, Department of Chemistry, KU Leuven, Celestijnenlaan 200F, Heverlee, B-3001, Belgium

刊名

Bioorganic Chemistry

年份

2019

卷号

Vol.88

ISSN

0045-2068

关键词

Apoptosis Autophagy Cytotoxicity Glycyrrhetinic acid-cinnamic acid ester derivatives Oleanolic acid-cinnamic acid ester derivatives ROS

摘要

Oleanolic acid and glycyrrhetinic acid are natural products with anticancer effects. Cinnamic acid and its derivatives also exhibited certain anticancer activity. In order to improve the anticancer activity of OA and GA, we designed and synthesized a series of novel OA-CA ester derivatives and GA-CA ester derivatives by using molecular hybridization approach. The 3--2, 5-diphenyltetrazolium bromide assay was used to assess their in vitro cytotoxicity on three cell lines , MCF-7 and L-O2 ). ...更多

Oleanolic acid and glycyrrhetinic acid are natural products with anticancer effects. Cinnamic acid and its derivatives also exhibited certain anticancer activity. In order to improve the anticancer activity of OA and GA, we designed and synthesized a series of novel OA-CA ester derivatives and GA-CA ester derivatives by using molecular hybridization approach. The 3--2, 5-diphenyltetrazolium bromide assay was used to assess their in vitro cytotoxicity on three cell lines , MCF-7 and L-O2 ). Among the evaluated compounds, 3o presented the strongest selective cytotoxicity on HeLa cells and showed no inhibitory activity against MCF-7 cells and L-O2 cells , and 3e presented the strongest selective inhibition of the MCF-7 cells . What's more, compound 2d also showed very strong selective inhibitory activity against HeLa cells . The further research using Hoechst 33342, AO/EB dual-staining, flow cytometric analysis and DCFH-DA fluorescent dye staining assay presented that 2d and 3o could induce HeLa cells apoptosis and autophagy.收起

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