Clark N W, Scott R C, Blain P G, Williams F M
Department of Environmental and Occupational Medicine, University of Newcastle-upon-Tyne, UK.
Arch Toxicol. 1993;67(1):44-8. doi: 10.1007/BF02072034.
Enzyme mediated hydrolysis of fluazifop butyl has been measured with rat and human skin post-mitochondrial fractions. Rat skin had a ten times greater capacity to metabolise fluazifop butyl than human skin, but the enzyme affinities were similar. The post-mitochondrial fraction metabolism was compared to that seen during absorption in a flow through diffusion cell with viable skin. Limited hydrolysis of absorbed fluazifop butyl was seen in rat skin, but increased two fold if the stratum corneum was removed. The stratum corneum was found to retain fluazifop butyl. When the skin was pre-incubated with the esterase inhibitor bis (p-nitrophenol) phosphate (BNPP), reduced metabolism was seen. No metabolism of fluazifop butyl was seen in human skin during absorption. Retention of the compound by the stratum corneum is postulated to restrict the accessibility of the compound to the enzyme site, thus influencing the observed metabolism during the absorption process.
已用大鼠和人类皮肤线粒体后组分测定了精稳杀得(fluazifop butyl)的酶介导水解作用。大鼠皮肤代谢精稳杀得的能力比人类皮肤强十倍,但酶亲和力相似。将线粒体后组分的代谢与在具有活性皮肤的流通扩散池中吸收过程中的代谢情况进行了比较。在大鼠皮肤中,吸收的精稳杀得水解有限,但如果去除角质层,水解增加两倍。发现角质层能保留精稳杀得。当皮肤用酯酶抑制剂磷酸双(对硝基苯酚)酯(BNPP)预孵育时,代谢减少。在吸收过程中,人类皮肤中未见精稳杀得的代谢。推测角质层对该化合物的保留限制了化合物与酶位点的接触,从而影响了吸收过程中观察到的代谢。