- Irinotecan is one of the camptothecin analog which has been shown to have a broad spectrum of antitumor activities against various malignancies. The aim of this study was to evaluate the effect of vitamin A, C, E and melatonin on proapoptotic activity of irinotecan in human cancer cells in vitro. We observed that irinotecan induced apoptosis in all types of analyzed cell lines when used as a single agent. Combination of selected antioxidants with various doses of irinotecan (7.5-60?M) resulted in significant increase in apoptotic cell death in A549 and HT29 cancer cell lines. The highest killing efficiency was observed after co-incubation of the cells with irinotecan and vitamin A (10?M), or vitamin E (25?M), respectively. The addition of vitamin C and melatonin to irinotecan treatment did not promote increase in killing of cancer cells. Our results indicate that some antioxidants can enhance the proapoptoic activity (properties) of irinotecan in human cancer cells in vitro. These findings may be supportive for the optimization of therapeutic efficacy of irinotecan treatment.Copyright © 2013 Elsevier Ltd. All rights reserved.