Gasiorowski K, Brokos B, Szyba K, Leszek J
Department of Basic Medical Sciences, Wrocłlaw Medical University, 14 Kochanowskiego Str., 51-601 Wrocłlaw, Poland.
Mutagenesis. 2001 Jan;16(1):31-8. doi: 10.1093/mutage/16.1.31.
Fluphenazine, an antipsychotic drug that belongs to the phenothiazine family, reduced the genotoxicity of direct- and indirect-acting mutagens in the Ames test, both in the presence and in the absence of promutagen-activating S9 fraction. In short-term tests on human lymphocytes, the inhibitory effect of fluphenazine on the genotoxicity of standard mutagens was strongest in the cytokinesis-blocked micronucleus assay and in the thioguanine resistance test, and weakest in the sister chromatid exchange test. Fluphenazine also considerably reduced the level of free radicals estimated in in vitro samples of human granulocytes. The results suggest that, in the range of the tested concentrations, fluphenazine could be considered for use to prevent the genotoxicity of daunorubicin, methyl methanesulfonate, benzo[a]pyrene, and mitomycin C. Reduction in the level of free radicals appears to be an important mechanism of the antimutagenic action of fluphenazine.
氟奋乃静是一种属于吩噻嗪类的抗精神病药物,在艾姆斯试验中,无论有无前诱变剂激活的S9组分,它都能降低直接和间接作用诱变剂的遗传毒性。在对人类淋巴细胞的短期试验中,氟奋乃静对标准诱变剂遗传毒性的抑制作用在胞质分裂阻滞微核试验和硫鸟嘌呤抗性试验中最强,而在姐妹染色单体交换试验中最弱。氟奋乃静还显著降低了人类粒细胞体外样本中估计的自由基水平。结果表明,在所测试的浓度范围内,氟奋乃静可被考虑用于预防柔红霉素、甲基磺酸甲酯、苯并[a]芘和丝裂霉素C的遗传毒性。自由基水平的降低似乎是氟奋乃静抗诱变作用的重要机制。