Cayir Akin, Cobanoglu Hayal, Coskun Munevver
Health Services Vocational College, Çanakkale Onsekiz Mart University, Canakkale, Turkey.
Expert Opin Drug Metab Toxicol. 2020 May;16(5):441-446. doi: 10.1080/17425255.2020.1748598. Epub 2020 Apr 10.
: Eletriptan is a migraine-specific drug-containing the triptan group. In terms of drug safety, the present study aimed to investigate the genotoxic potential of eletriptan.: We conducted our study by using the cytokinesis-block micronucleus cytome (CBMN) assay, a comprehensive method for measuring micronucleus formation, and a sensitive method for detecting DNA-strand breaks. In the assay, cytokinesis-block proliferation index and the frequency of micronuclei were evaluated in lymphocytes treated with three different concentrations (1, 10 and 25 µg/ml) of eletriptan for 48 hours. In comet assays, DNA damage was evaluated in leucocytes treated with three different concentrations (1, 10 and 25 µg/ml) of eletriptan for an hour.: Eletriptan did not induce cytotoxicity nor any increased micronuclei frequencies. While the comet parameters % DNA in tail, tail moment, and the olive moment was found to be significantly increased at 10 and 25 µg/ml, the cytokinesis-block proliferation index values were not.: These findings suggest that eletriptan is non-cytotoxic but potentially weakly genotoxic at higher concentrations (10 and 25 µg/ml).
依立曲坦是一种含曲坦类的偏头痛特异性药物。在药物安全性方面,本研究旨在调查依立曲坦的遗传毒性潜力。
我们通过使用胞质分裂阻滞微核细胞组(CBMN)试验进行研究,这是一种测量微核形成的综合方法,也是一种检测DNA链断裂的灵敏方法。在该试验中,对用三种不同浓度(1、10和25μg/ml)的依立曲坦处理48小时的淋巴细胞评估胞质分裂阻滞增殖指数和微核频率。在彗星试验中,对用三种不同浓度(1、10和25μg/ml)的依立曲坦处理一小时的白细胞评估DNA损伤。
依立曲坦未诱导细胞毒性,也未使微核频率增加。虽然在10和25μg/ml时发现彗星试验参数尾中DNA%、尾矩和橄榄尾矩显著增加,但胞质分裂阻滞增殖指数值未增加。
这些发现表明,依立曲坦无细胞毒性,但在较高浓度(10和25μg/ml)时可能具有弱遗传毒性。