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重氮苯磺酸盐可选择性地消除UDP-N-乙酰葡糖胺对葡糖醛酸化的刺激作用。

Diazobenzenesulphonate selectively abolishes stimulation of glucuronidation by UDP-N-acetylglucosamine.

作者信息

Haeger B, de Brito R, Hallinan T

出版信息

Biochem J. 1980 Dec 15;192(3):971-4. doi: 10.1042/bj1920971.

Abstract
  1. Basal rates of glucuronidation of oestrone (guinea pig) or of 4-nitrophenol (rat or guinea pig) were not significantly altered in sealed liver microsomal vesicles, treated with the membrane-impermeant protein-modifying agent diazobenzenesulphonate at 0.5-1.0 mM. 2. Contrarily, diazobenzenesulphonate abolished the normal stimulation of glucuronidation by UDP-N-acetylglucosamine. 3. Ultrasonication to increase microsomal permeability activated glucuronidation by 680-750% and permitted significant inhibition by diazobenzenesulphonate. 4. These findings are consistent with a model wherein glucuronyltransferases are embedded in the luminal leaflet of the endoplasmic reticulum and access of UDP-glucuronic acid to the transferases is facilitated by transmembrane carriers, which are stimulated by UDP-N-acetylglucosamine and are available to diazobenzenesulphonate; ultrasonication serves to permit access of diazobenzenesulphonate to glucuronyltransferases themselves, resulting in inhibition of their activity.
摘要
  1. 用0.5 - 1.0 mM的膜不通透性蛋白质修饰剂重氮苯磺酸盐处理豚鼠肝微粒体封闭囊泡后,雌酮(豚鼠)或4 - 硝基苯酚(大鼠或豚鼠)的葡萄糖醛酸化基础速率没有显著改变。2. 相反,重氮苯磺酸盐消除了UDP - N - 乙酰葡糖胺对葡萄糖醛酸化的正常刺激作用。3. 通过超声处理增加微粒体通透性可使葡萄糖醛酸化活性提高680 - 750%,并使重氮苯磺酸盐产生显著抑制作用。4. 这些发现与一种模型相符,即葡萄糖醛酸转移酶嵌入内质网的腔面膜小叶中,UDP - 葡萄糖醛酸通过跨膜载体进入转移酶,该载体受UDP - N - 乙酰葡糖胺刺激且可被重氮苯磺酸盐作用;超声处理可使重氮苯磺酸盐接触到葡萄糖醛酸转移酶本身,从而抑制其活性。

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Metabolism of naphthalene to naphthalene dihydrodiol glucuronide in isolated hepatocytes and in liver microsomes.
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