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Pharmaceutical Chemistry Journal

, Volume 53, Issue 6, pp 539–543 | Cite as

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

  • Dong-Jun Fu
  • Jia-Huan Li
  • Ping Li
  • Zhen-Wei Cui
  • Sai-Yang Zhang
  • Jiang-Feng LiEmail author
Article
  • 16 Downloads

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.

Keywords

chalcone MGC-803 apoptosis Bax NAC ROS generation 

Notes

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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Copyright information

© Springer Science+Business Media, LLC, part of Springer Nature 2019

Authors and Affiliations

  • Dong-Jun Fu
    • 1
  • Jia-Huan Li
    • 1
  • Ping Li
    • 1
  • Zhen-Wei Cui
    • 2
    • 3
  • Sai-Yang Zhang
    • 4
  • Jiang-Feng Li
    • 4
    Email author
  1. 1.School of Pharmaceutical Sciences & Collaborative Innovation Center of New Drug Research and Safety EvaluationZhengzhou UniversityZhengzhouChina
  2. 2.School of life Sciences, Institute of Biodiversity and EcologyZhengzhou UniversityZhengzhouChina
  3. 3.Charles Perkins Centre, Sydney Medical SchoolUniversity of SydneySydneyAustralia
  4. 4.School of Basic MedicineZhengzhou UniversityZhengzhouChina

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