Journal
BIOORGANIC CHEMISTRY
Volume 88, Issue -, Pages -Publisher
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2019.102951
Keywords
Cytotoxicity; Oleanolic acid-cinnamic acid ester derivatives; Glycyrrhetinic acid-cinnamic acid ester derivatives; Apoptosis; ROS; Autophagy
Funding
- Fundamental Research Funds for the Innovation and Entrepreneurship Foundation from Huancui District of Wehai City
- project of Weihai Science and Technology Bureau [1070432121708]
- National Natural Science Foundation of China [21672046, 21372054]
- Fundamental Research Funds for the Central Universities [HIT.NSRIF.201701]
- Hercules Foundation of the Flemish Government [20100225-7]
- Peterson Serving Hometown Elites Scholarship
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Oleanolic acid (OA) and glycyrrhetinic acid (GA) are natural products with anticancer effects. Cinnamic acid (CA) 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-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) assay was used to assess their in vitro cytotoxicity on three cell lines (HeLa (cervical cancer), MCF-7 (breast cancer) and L-O2 (a normal hepatic cell)). Among the evaluated compounds, 3o presented the strongest selective cytotoxicity on HeLa cells (IC50 = 1.35 mu M) and showed no inhibitory activity against MCF-7 cells (IC50 > 100 mu M) and L-O2 cells (IC50 > 100 mu M), and 3e presented the strongest selective inhibition of the MCF-7 cells (IC50 = 1.79 mu M). What's more, compound 2d also showed very strong selective inhibitory activity against HeLa cells (IC50 = 1.55 mu M). 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.
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