Synthesis of Chalcones with Anticancer Activities

Molecules

Suvitha Syam¹  Siddig Ibrahim Abdelwahab¹  Mohammed Ali Al-Mamary¹ 

[1] ¹UPM-MAKNA Cancer Research Lab, Institute of Bioscience, University Putra Malaysia, 43400 Serdang, Selangor, Malaysia

关键词: chalcone;    synthetic;    cytotoxicity;    MCF-7 cells;    apoptosis;    high content screening;    caspase;    ROS;   

DOI  :  10.3390/molecules17066179

来源: mdpi

【 摘 要 】

Several chalcones were synthesized and their in vitro cytotoxicity against various human cell lines, including human breast adenocarcinoma cell line MCF-7, human lung adenocarcinoma cell line A549, human prostate cancer cell line PC3, human adenocarcinoma cell line HT-29 (colorectal cancer) and human normal liver cell line WRL-68 was evaluated. Most of the compounds being active cytotoxic agents, four of them with minimal IC₅₀ values were chosen and studied in detail with MCF-7 cells. The compounds 1, 5, 23, and 25 were capable in eliciting apoptosis in MCF-7 cells as shown by multiparameter cytotoxicity assay and caspase-3/7, -8, and -9 activities (p < 0.05). The ROS level showed 1.3-fold increase (p < 0.05) at the low concentrations used and thus it was concluded that the compounds increased the ROS level eventually leading to apoptosis in MCF-7 cells through intrinsic as well as extrinsic pathways.

【 授权许可】

CC BY   
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.