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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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Pharmaceutical Chemistry Journal Aims and scope

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.

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Acknowledgments

This work was supported by the National Natural Sciences Foundations of China (No. 81703541 and 81673322), and project funded by China Postdoctoral Science Foundation. This work was supported by MEDCHEMEXPRESS. Thanks to MCE Award for Scientists Promoting Biology and Medicine Research.

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Authors and Affiliations

  1. School of Pharmaceutical Sciences & Collaborative Innovation Center of New Drug Research and Safety Evaluation, Zhengzhou University, Zhengzhou, 450001, China

    Dong-Jun Fu, Jia-Huan Li & Ping Li

  2. School of life Sciences, Institute of Biodiversity and Ecology, Zhengzhou University, Zhengzhou, 450001, China

    Zhen-Wei Cui

  3. Charles Perkins Centre, Sydney Medical School, University of Sydney, Camperdown, Sydney, New South Wales, 2006, Australia

    Zhen-Wei Cui

  4. School of Basic Medicine, Zhengzhou University, Zhengzhou, 450001, China

    Sai-Yang Zhang & Jiang-Feng Li

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  1. Dong-Jun Fu
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  2. Jia-Huan Li
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  4. Zhen-Wei Cui
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  5. Sai-Yang Zhang
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Correspondence to Jiang-Feng Li.

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Fu, DJ., Li, JH., Li, P. et al. Antiproliferative Evaluation In Vitro of a New Chalcone Inducing Apoptosis by ROS Generation Against MGC-803 Cells. Pharm Chem J 53, 539–543 (2019). https://doi.org/10.1007/s11094-019-02034-8

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  • DOI: https://doi.org/10.1007/s11094-019-02034-8

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