Sitagliptin is an active ingredient of antidiabetic drug used in the treatment of type 2 diabetes mellitus (T2DM). In this study, the genotoxic effects of sitagliptin were determined in human lymphocytes by using chromosome aberrations (CAs), sister chromatid exchanges (SCEs), micronucleus (MN) and comet assays. 31.25–1000 μg/mL concentrations of sitagliptin were used. Sitagliptin significantly increased the frequency of CAs and SCEs at the highest concentration at 24 h treatment and all concentrations (except 250 μg/mL for CA, except 31.25 and 62.50 μg/mL for SCE) at 48 h treatment compared with solvent control (DMSO). This compound increased the MN at only the highest concentration compared with the solvent control. Mitotic index (MI) significantly decreased at the three highest concentrations of sitagliptin at 48 h treatment. However, replication (RI) and nuclear division (NDI) indices were not affected at all the treatments. Comet assay results indicated that sitagliptin significantly increased mean comet tail intensity and tail moment at only two concentrations (62.50 and 1000 μg/mL for intensity, 125 and 1000 μg/mL for tail moment), and tail length at all concentrations (except 125 and 500 μg/mL). It was concluded that higher concentration of sitagliptin had genotoxic effects in the human lymphocytes in vitro.

西他列汀是用于治疗2型糖尿病（T2DM）的抗糖尿病药物的活性成分。在这项研究中，西格列汀的遗传毒性作用是通过使用染色体畸变（CAs），姐妹染色单体交换（SCE），微核（MN）和彗星试验确定的，在人淋巴细胞中的遗传毒性。使用西他列汀浓度为31.25–1000μg/ mL。与溶剂对照组（DMSO）相比，西他列汀在24 h处理最高浓度和所有浓度（CA的250μg/ mL除外，SCE的31.25和62.50μg/ mL除外）在所有浓度时均显着增加CAs和SCE的频率。与溶剂对照相比，该化合物仅以最高浓度增加了MN。在治疗后48小时，西他列汀的三个最高浓度下，有丝分裂指数（MI）显着降低。然而，复制（RI）和核分裂（NDI）指数在所有处理中均未受到影响。彗星试验结果表明，西他列汀仅在两种浓度下（强度分别为62.50和1000μg/ mL，尾矩为125和1000μg/ mL）显着增加了平均彗尾强度和尾矩，并且在所有浓度下（125和125除外）尾巴长度均显着增加。 500μg/ mL）。结论是西他列汀浓度升高对人淋巴细胞具有遗传毒性作用体外。