反式索布瑞醇对大鼠药物代谢酶的影响。

Effects of trans-sobrerol on drug metabolizing enzymes in the rat.

Lippi A, Gervasi P G, Bellucci G, Marioni F, Luzzani F, Ventura P

Istituto di Mutagenesi e Differenziamento, C.N.R. Pisa, Italy.

Xenobiotica. 1989 Aug;19(8):823-32. doi: 10.3109/00498258909043143.

Abstract

Metabolism of 14C-trans-sobrerol (I) by Sprague-Dawley rat liver microsomes did not result in covalent binding to proteins, lipid peroxidation or cytochrome P-450 destruction. 2. Subacute and chronic treatment of Sprague-Dawley rats with (I) resulted only in an increase in liver cytosolic GSH-S-transferase. 3. Acute treatment of rats with trans-sobrerol or its metabolite, 8-hydroxycarvotanacetone (II) produced considerable GSH depletion, faster in the case of II, in both liver and lung; the original GSH levels were restored within 24 h. No significant increase in lipid peroxidation was found even when GSH was at its lowest level. 4. UDP-glucuronyltransferase and GSH-S-transferase conjugation occurred with trans-sobrerol and some of its metabolites although at low rates.

摘要

14C - 反式异松油醇（I）在斯普拉格 - 道利大鼠肝微粒体中的代谢未导致与蛋白质的共价结合、脂质过氧化或细胞色素P - 450的破坏。2. 用（I）对斯普拉格 - 道利大鼠进行亚急性和慢性治疗仅导致肝细胞溶质谷胱甘肽 - S - 转移酶增加。3. 用反式异松油醇或其代谢物8 - 羟基香芹酮（II）对大鼠进行急性治疗会导致肝脏和肺中谷胱甘肽大量消耗，II的情况消耗更快；原始谷胱甘肽水平在24小时内恢复。即使谷胱甘肽处于最低水平时，脂质过氧化也未显著增加。4. 尿苷二磷酸葡萄糖醛酸基转移酶和谷胱甘肽 - S - 转移酶与反式异松油醇及其一些代谢物发生结合反应，尽管反应速率较低。