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一种硝基烯烃衍生物1-(5-溴呋喃-2-基)-2-溴-2-硝基乙烯在沙门氏菌/微粒体试验和小鼠骨髓微核试验中的活性。

Activity of a nitroalkene derivative, 1-(5-bromofur-2-il)-2-bromo-2-nitroethene, in the Salmonella/microsome assay and the mouse bone marrow micronucleus test.

作者信息

Ramos A, Vizoso A, Edreira A, Betancourt J, Décalo M

机构信息

Centro de Investigación y Desarrollo de Medicamentos, Ciudad de la Habana, Cuba.

出版信息

Mutat Res. 1997 May 23;390(3):233-8. doi: 10.1016/s1383-5718(97)00017-x.

DOI:10.1016/s1383-5718(97)00017-x
PMID:9186572
Abstract

Mutagenicity of a substituted nitroalkene, 1-(5-bromofur-2-il)-2-bromo-2-nitroethene (BNF) was tested in the Salmonella/microsome assay using the strains TA 98, TA 100 and TA 100NR (nitroreductase deficient). BNF was a direct mutagen in TA 98 and TA 100; the response was lowered when exogenous metabolic activation (S9) was used. A further decrease in mutagenicity was observed in strain TA 100NR, as compared to the parental TA 100, which showed the involvement of nitroreduction in the overall response elicited by BNF. The micronucleus assay was carried out in Swiss male mice which were given a single i.p. dose of 10-20 mg/kg of BNF dissolved in peanut oil, bone marrow being sampled 24 and 48 h later. The micronucleated polychromatic erythrocyte counts (MNPCE) showed a weak response in the dose range of 10-17.5 mg/kg at the second sampling (48 h) and a significant rise for 20 mg/kg at 24 and 48 h.

摘要

使用TA 98、TA 100和TA 100NR(硝基还原酶缺陷型)菌株,在沙门氏菌/微粒体试验中测试了一种取代硝基烯烃1-(5-溴呋喃-2-基)-2-溴-2-硝基乙烯(BNF)的致突变性。BNF在TA 98和TA 100中是直接诱变剂;使用外源性代谢激活剂(S9)时,反应降低。与亲本TA 100相比,在TA 100NR菌株中观察到诱变性进一步降低,这表明硝基还原参与了BNF引发的总体反应。在瑞士雄性小鼠中进行微核试验,小鼠腹腔注射单次剂量为10 - 20 mg/kg溶解于花生油中的BNF,在24小时和48小时后采集骨髓样本。微核多染性红细胞计数(MNPCE)在第二次采样(48小时)时,在10 - 17.5 mg/kg剂量范围内显示出微弱反应,而在20 mg/kg剂量下,在24小时和48小时时显著升高。

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