Abstract:
[1-(2-isopropyl-5-methylphenoxy)-3-(yridine-3-ylmethylamino)propan-2-ol] is a novel oxipropanolamine derivative. It had been synthesized in a previous study with the idea that could be a prodrug and determined to show anti-alpha-glycosidase, antiacetylcholinesterase, anticarbonic anhydrase and antibacterial activities. However, to suggest it as a drug candidate, genotoxicity data related to it should be available. Thus, in this research, we aimed to evaluate its genotoxicity. We performed the chromosomal aberration and micronucleus tests in human peripheral lymphocytes. In all tests, lymphocyte cultures were treated with four concentrations (50, 25, 12.5, 6.25 mu g/mL) of this derivative. According to our results, it significantly increased the chromosomal abnormalities at 25 and 50 mu g/mL concentrations both 24 h and 48 h periods. Also, it significantly decreased the mitotic index at all concentrations. On the other hand, it significantly increased the micronucleus frequencies at 6.25, 12.5, and 25 mu g/mL concentrations. In micronucleus test, no binucleate cells were detected at the highest concentration (50 mu g/mL) and a total number of 4000 binucleate cells couldn't be reached at the second-highest concentration (25 mu g/mL). These results evaluated together, we can suggest that the test substance is cytotoxic and aneugenic at all used concentrations in human peripheral lymphocytes. Also, it's clastogenic and genotoxic at high application concentrations.
