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.