Abstract
Aim: To systematically investigate the effects of a class of curcumin-based compounds on cancer cell viability, proliferation, and apoptosis. Materials and Methods: Cytotoxicity and anti-proliferative potency were estimated by the trypan blue exclusion assay and WST-1 cell proliferation assay, respectively. Cell death pathways were discriminated according to plasma membrane integrity and lipid asymmetry cell profiles using a F2N12S and CYTOX AADvanced double staining flow cytometry-based assay. Results: Nine compounds (2-10) exhibit 13- to 58-fold better cytotoxic and anti-proliferative potencies than curcumin towards HeLa cells. In this cervical cancer cell model, dienone and 1-methylpiperidone serve as the favorable central linkers; 5-methylisoxazol-3-yl and 3-methylisoxazol-5-yl act as the optimal terminal aromatic moiety. Finally, the effects of compounds 6 and 10 on HeLa cells' plasma membrane integrity and lipid asymmetry suggest that the early cytotoxic effect of these compounds is due to a stimulation of apoptosis.
- Received June 11, 2015.
- Revision received July 10, 2015.
- Accepted July 13, 2015.
- Copyright© 2015 International Institute of Anticancer Research (Dr. John G. Delinassios), All rights reserved