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Antiproliferative Evaluation In Vitro of a New Chalcone Inducing Apoptosis by ROS Generation Against MGC-803 Cells


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Abstract

We have evaluated the antiproliferative activity of (E)-3-(3,5-difluorophenyl)-1-(2,4,6-trimethoxyphenyl)- prop-2-en-1-one (chalcone 5) against MGC-803 cells. This chalcone analog displayed a potent antiproliferative activity with an IC50 value of 0.23 μM against MGC-803 cells. It could induce apoptosis and regulate the apoptosis-related markers (Bax, Bcl-2, Bcl-xl, and Bid) in a concentration dependent manner. Treatment with NAC almost completely attenuated chalcone-induced cell inhibition and cell apoptosis in MGC-803 cells, indicating that the apoptotic mechanisms were related to ROS generation. Therefore, this chalcone derivative is a new apoptosis inducer for prevention and treatment of gastric cancer.

About the authors

Dong-Jun Fu

School of Pharmaceutical Sciences & Collaborative Innovation Center of New Drug Research and Safety Evaluation, Zhengzhou University

Email: fade3532@163.com
China, Zhengzhou, 450001

Jia-Huan Li

School of Pharmaceutical Sciences & Collaborative Innovation Center of New Drug Research and Safety Evaluation, Zhengzhou University

Email: fade3532@163.com
China, Zhengzhou, 450001

Ping Li

School of Pharmaceutical Sciences & Collaborative Innovation Center of New Drug Research and Safety Evaluation, Zhengzhou University

Email: fade3532@163.com
China, Zhengzhou, 450001

Zhen-Wei Cui

School of life Sciences, Institute of Biodiversity and Ecology, Zhengzhou University; Charles Perkins Centre, Sydney Medical School, University of Sydney

Email: fade3532@163.com
China, Zhengzhou, 450001; Camperdown, Sydney, New South Wales, 2006

Sai-Yang Zhang

School of Basic Medicine, Zhengzhou University

Email: fade3532@163.com
China, Zhengzhou, 450001

Jiang-Feng Li

School of Basic Medicine, Zhengzhou University

Author for correspondence.
Email: fade3532@163.com
China, Zhengzhou, 450001

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