Abstract
A series of 8-substituted alkyl xanthines were evaluated in vitro to test the cytotoxocity in cells. For this experiment, we utilized different mammalian cancer cell lines primarily representing prostrate and lung. One of the compounds synthesized, viz. 8-tertbutyl caffeine showed potent anticancer activity at low concentrations against DU145 when compared to adriamycin. Further experiments were carried out to check the cell cycle arrest in the DU145 cells treated with adriamycin, caffeine and 8-tert butyl caffeine. We observed that there was an arrest in G1 phase of cell cycle at 24 hours while at 48 hours of incubation, the cells were constantly distributed (59.71% -70.79%). We conclude that the effect of 8-tertbutyl caffeine is relatively comparable to caffeine whereas in adriamycin treated cells, we observed the cells underwent G2 arrest. We evaluate the studies on these effects by showing potent analogues which could be used as promising anticancer agents.
Highlights
Xanthines are purine bases which are known to act as anti-depressants, anti-therapeutic and anti-hyperuraemic agents
Further experiments were carried out to check the cell cycle arrest in the DU145 cells treated with adriamycin, caffeine and 8-tert butyl caffeine
The present studies revealed that a set of 8-substituted alkyl xanthines exhibited cytotoxicity on wide range of human cancer cell lines
Summary
Xanthines are purine bases which are known to act as anti-depressants, anti-therapeutic and anti-hyperuraemic agents. More recent studies on xanthines have shown that these are sensitive in irradiating tumor cells inhibiting G2 checkpoint [1], furthering cells to become more sensitive to DNA dama*. The best example of xanthine is caffeine, known to be involved in human carcinogenesis at various sites of the tumors. These studies on caffeine have shown to enhance the cytocidal and growth inhibitory effect suggesting that caffeine may be useful in enhancing the tumoricidal effect of anticancer drugs, especially DNAdamaging agents, and possibly aid in overcoming natural drug resistance. In the recent-past, studies on xanthines have resulted in several cancer studies. Human adenocarcinoma cell line (A-549) was derived from a primary lung cancer expressing wild-type p53 [2]
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