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.

中文翻译：

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维格列汀和西格列汀的体外细胞遗传学评估和比较。


维格列汀和西他列汀是常用的抗糖尿病药物。采用染色体畸变（CA）、姐妹染色单体交换（SCE）和胞质分裂阻断微核（CBMN）测定来评估和比较这些药物的细胞毒性和基因毒性作用。将外周淋巴细胞暴露于 125 μg/ml、250 μg/ml 和 500 μg/ml 维格列汀以及 250 μg/ml、500 μg/ml 和 1000 μg/ml 西他列汀 24 小时和 48 小时，有或没有外源代谢激活。研究结束时确定这些药物及其代谢物对CA、SCE和CBMN没有基因毒性作用。另一方面，与剂量增加平行，维格列汀对有丝分裂指数显示出弱的细胞毒性，并且取决于其剂量的增加；西格列汀对有丝分裂指数、核分裂指数和增殖指数具有潜在的细胞毒性和细胞抑制作用。由于其细胞毒性和细胞抑制潜力，这些药物可抑制细胞增殖。