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大鼠和无毛小鼠皮肤微粒体中的UDP-葡萄糖醛酸基转移酶活性

UDP-glucuronosyltransferase activity in rat-and hairless mouse skin-microsomes.

作者信息

Moloney S J, Bridges J W, Fromson J M

出版信息

Xenobiotica. 1982 Aug;12(8):481-7. doi: 10.3109/00498258209038925.

DOI:10.3109/00498258209038925
PMID:6815905
Abstract
  1. Cutaneous UDP-glucuronosyltransferase activity (E.C.2.4.1.17) was demonstrated in rat- and hairless mouse-skin microsomes using 1-naphthol as substrate. 2. Addition of the detergent Brij 35 increased the activity by approximately twofold in both species. 3. Inhibitor studies demonstrated that under the assay conditions used any UDP-glucuronic acid pyrophosphatase or beta-glucuronidase present did not interfere with the conjugation reaction. 4. Substrate inhibition was observed in hairless mouse-skin preparations and biphasic response to increasing naphthol concentration was seen in rat-skin microsomes. 5. The apparent Km values were considerably lower than those reported for liver. The sp. activity (per mg microsomal protein) in unactivated rat-skin microsomes was about 50% of that reported in unactivated rat-liver microsomes. 6. Pretreatment with 3-methylcholanthrene resulted in a small increase in cutaneous UDP-glucuronosyltransferase activities in both species.
摘要
  1. 以1-萘酚为底物,在大鼠和无毛小鼠皮肤微粒体中证实了皮肤UDP-葡萄糖醛酸基转移酶活性(E.C.2.4.1.17)。2. 添加去污剂Brij 35后,两个物种的活性均增加了约两倍。3. 抑制剂研究表明,在所使用的测定条件下,任何存在的UDP-葡萄糖醛酸焦磷酸酶或β-葡萄糖醛酸酶均不干扰结合反应。4. 在无毛小鼠皮肤制剂中观察到底物抑制,在大鼠皮肤微粒体中观察到对萘酚浓度增加的双相反应。5. 表观Km值明显低于肝脏报道的值。未活化大鼠皮肤微粒体中的比活性(每毫克微粒体蛋白)约为未活化大鼠肝脏微粒体报道值的50%。6. 用3-甲基胆蒽预处理导致两个物种的皮肤UDP-葡萄糖醛酸基转移酶活性略有增加。

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