Chalcone derivatives cause accumulation of colon cancer cells in the G2/M phase and induce apoptosis.

摘要: Abstract Aims Chalcones, naturally occurring open-chain polyphenols abundant in plants, have demonstrated antiproliferative activity several cancer cell lines. In the present study, potential anticancer of two synthetic analogues named Ch1 and Ch2 colon line was investigated. Main methods Antiproliferative activities both were assessed by Growth Inhibition Assay (MTT) xCELLigence analysis. Apoptosis annexin V/PI staining (early stage) or DNA fragmentation (final stage). To study death mechanism induced tested substances, we a series assays including measurements caspase 3 activity, membrane mitochondrial (MMP) changes, reactive oxygen species (ROS) production flow cytometry expression important apoptosis-related genes realtime PCR. Key findings We found concentration time-dependent cytotoxicity, inhibition proliferation Caco-2 cells after treatment parallel with G2/M phase cycle arrest increased proportion subG0/G1 population V positivity. that caspase-dependent associated ROS production, suppressed Bcl-2 Bcl-xL enhanced Bax expression. Treatment also α-, α1- β5-tubulins, on other hand only α-tubulin Significance Presented chalcones induce apoptosis intrinsic pathways, therefore may be an interesting strategy for therapy.