Genotoxic effects of metronidazole

Guillermo Elizondo , María E. Gonsebatt , Ana María Salazar , Ismael Lares , Pilar Santiago , Jorge Herrera , Enrique Hong , Patricia Ostrosky-Wegman
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引用次数: 50

Abstract

Metronidazole (MTZ) is an effective agent used in the treatment of parasitic infections. Its genotoxic effects have been shown in a variety of prokaryotic systems; however, negative results have been reported in human in vivo studies. Due to its wide spread use, a study was performed to evaluate the chromosomal aberration frequencies in peripheral blood lymphocyte cultures from 10 individuals, before and after metronidazole treatment. A significant increase in the percentage of cells with chromatid and isochromatid breaks was observed after metronidazole treatment (1500 mg per day for 10 days). The percentages of cells with aberrations did not correlate with the levels of MTZ found in plasma. Individual variability was observed with respect to both the induction of aberrations and the concentration of MTZ in plasma. They could represent differences at the metabolic level, since metronidazole is known to be biotransformed by a polymorphic P450 cytochrome, and its metabolites have shown mutagenic activity.

甲硝唑的基因毒性作用
甲硝唑(MTZ)是一种治疗寄生虫感染的有效药物。其基因毒性作用已在多种原核生物系统中得到证实;然而,在人体体内研究中,已经报道了阴性结果。由于甲硝唑的广泛使用,我们进行了一项研究,评估了10个人在甲硝唑治疗前后外周血淋巴细胞培养中染色体畸变的频率。在甲硝唑处理(每天1500 mg,持续10天)后,染色单体和等染色单体断裂的细胞百分比显著增加。畸变细胞的百分比与血浆中发现的MTZ水平无关。在诱导畸变和血浆中MTZ浓度方面观察到个体差异。它们可能代表了代谢水平上的差异,因为已知甲硝唑是由多态P450细胞色素进行生物转化的,其代谢物已显示出致突变活性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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