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氟乙酸特异性脱卤酶和谷胱甘肽转移酶在氟乙酰胺和2,4-二硝基氟苯代谢中的作用。

The role of fluoroacetate-specific dehalogenase and glutathione transferase in the metabolism of fluoroacetamide and 2,4-dinitrofluorobenzene.

作者信息

Kostyniak P J, Soiefer A I

出版信息

Toxicol Lett. 1984 Aug;22(2):217-22. doi: 10.1016/0378-4274(84)90069-9.

DOI:10.1016/0378-4274(84)90069-9
PMID:6147909
Abstract

2,4-Dinitrofluorobenzene (DNFB) reacts with glutathione to form a stable product similar to that formed with the model glutathione-S-transferase (GST) substrate, 1-chloro-2,4-dinitrobenzene (CDNB). DNFB is approx. 40 times als reactive as CDNB in this chemical reaction. The enzymatic defluorination of DNFB also proceeds at a more rapid rate than that of CDNB in the GST assay. Fluoroacetamide (FAM), like fluoroacetate (FAC), undergoes no discernable chemical defluorination. Its enzymatic defluorination is approx. 10% of that observed for FAC and only 0.2% of the rate for DNFB. An antibody raised to the fluoroacetate specific dehalogenase (FSD) precipitated both FAC and FAM defluorinating activity but had no effect on either CDNB or DNFB activity. The data are consistent with the hypothesis that DNFB is metabolized by the GST while FAM is metabolized by the FSD.

摘要

2,4-二硝基氟苯(DNFB)与谷胱甘肽反应形成一种稳定产物,类似于与模型谷胱甘肽-S-转移酶(GST)底物1-氯-2,4-二硝基苯(CDNB)反应形成的产物。在该化学反应中,DNFB的反应活性约为CDNB的40倍。在GST测定中,DNFB的酶促脱氟反应速率也比CDNB更快。氟乙酰胺(FAM)与氟乙酸(FAC)一样,未发生可察觉的化学脱氟反应。其酶促脱氟反应约为FAC的10%,仅为DNFB反应速率的0.2%。针对氟乙酸特异性脱卤酶(FSD)产生的抗体沉淀了FAC和FAM的脱氟活性,但对CDNB或DNFB活性均无影响。这些数据与以下假设一致,即DNFB由GST代谢,而FAM由FSD代谢。

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