In vitro cytogenetic assessment and comparison of vildagliptin and sitagliptin

维格列汀与西他列汀的体外细胞遗传学评估与比较

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作者:Ceren Börçek Kasurka, Mehmet Elbistan, Ayşegül Atmaca, Zülal Atlı Şekeroğlu

Abstract

Vildagliptin and sitagliptin are commonly used antidiabetic drugs. Chromosomal aberration (CA), sister chromatid exchange (SCE) and cytokinesis-block micronucleus (CBMN) assays were employed to assess and compare cytotoxic and genotoxic effects of these drugs. Peripheral lymphocytes were exposed to 125 μg/ml, 250 μg/ml and 500 μg/ml of vildagliptin and 250 μg/ml, 500 μg/ml and 1000 μg/ml of sitagliptin for 24 h and 48 h with and without exogenous metabolic activation. At the end of the study, it was determined that these drugs and their metabolites had no genotoxic effects on CA, SCE and CBMN. On the other hand, parallel to the increase in dose, vildagliptin showed weak cytotoxicity on the mitotic index, and depending on its increase in dose; sitagliptin caused potential cytotoxicity and cytostatic effect on the mitotic index, nuclear division index and proliferation index. Due to their cytotoxic and cytostatic potential, these drugs inhibit cell proliferation.

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