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大鼠和无毛小鼠皮肤条对7-乙氧基香豆素和7-羟基香豆素的代谢

The metabolism of 7-ethoxycoumarin and 7-hydroxycoumarin by rat and hairless mouse skin strips.

作者信息

Moloney S J, Fromson J M, Bridges J W

出版信息

Biochem Pharmacol. 1982 Dec 15;31(24):4005-9. doi: 10.1016/0006-2952(82)90648-7.

Abstract

The metabolism of 7-ethoxycoumarin and 7-hydroxycoumarin was studied in rat and hairless mouse skin strips. These preparations supported de-ethylation, sulphation and glucuronidation reactions. The de-ethylation reaction was inducible in both species by pretreatment with either 5,6-benzoflavone or 3-methylcholanthrene. The hairless mouse strips exhibited a greater basal de-ethylase activity than rat strips, although the latter was the more responsive to inducers. Accompanying the increase in de-ethylation activity was a change in the pattern of metabolites, with a large increase in the percentage of the unconjugated metabolite. When 7-hydroxycoumarin was employed as the primary substrate the glucuronide was the major metabolite formed by strips from both species. The glucuronidation and sulphation activities were unchanged by 3-methylcholanthrene pretreatment.

摘要

在大鼠和无毛小鼠的皮肤条中研究了7-乙氧基香豆素和7-羟基香豆素的代谢。这些制剂支持脱乙基、硫酸化和葡萄糖醛酸化反应。通过用5,6-苯并黄酮或3-甲基胆蒽预处理,两种物种中的脱乙基反应均可诱导。无毛小鼠皮肤条表现出比大鼠皮肤条更高的基础脱乙基酶活性,尽管后者对诱导剂更敏感。伴随着脱乙基活性的增加,代谢物模式发生了变化,未结合代谢物的百分比大幅增加。当使用7-羟基香豆素作为主要底物时,葡萄糖醛酸苷是两种物种的皮肤条形成的主要代谢物。3-甲基胆蒽预处理后,葡萄糖醛酸化和硫酸化活性未发生变化。

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