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致癌物/动脉粥样硬化原在培养的主动脉组织和细胞中的II期生物转化。II. 3-羟基苯并(a)芘的葡萄糖醛酸化作用。

Phase II biotransformation of carcinogens/atherogens in cultured aortic tissues and cells. II. Glucuronidation of 3-hydroxy-benzo(a)pyrene.

作者信息

Yang H Y, Majesky M W, Namkung M J, Juchau M R

出版信息

Drug Metab Dispos. 1986 May-Jun;14(3):293-8.

PMID:2872027
Abstract

Avian aortic tissues contain active UDP-glucuronosyltransferase(s) (EC 2.4.1.17) which catalyze(s) the glucuronidation of 3-hydroxybenzo(a)pyrene and p-nitrophenol. Activities were compared in abdominal segments (susceptible to the atheroma-promoting effects of polynuclear aromatic hydrocarbons) vs. thoracic segments (susceptible to the atheroma-initiating effects of polynuclear aromatic hydrocarbons). Activities measured in the abdominal segments were approximately 8-9-fold higher than those measured in thoracic segments from the same cockerels. Surprisingly, pretreatment of cockerels with phenobarbital, but not 3-methylcholanthrene, resulted in small (60-120%) but consistent increases in glucuronosyltransferase activities in both aortic segments. Activities were readily detectable in microsomal fractions of both segments and in cultured smooth muscle cells derived from aortic segments, but were not detectable in cultured endothelial cells. Avian aortic microsomal glucuronosyltransferases exhibited minimal or no response to the effects of several common activators of hepatic microsomal glucuronosyltransferases.

摘要

禽类主动脉组织含有活性UDP-葡萄糖醛酸基转移酶(EC 2.4.1.17),该酶催化3-羟基苯并(a)芘和对硝基苯酚的葡萄糖醛酸化反应。对腹段(易受多环芳烃促动脉粥样硬化作用影响)和胸段(易受多环芳烃引发动脉粥样硬化作用影响)的酶活性进行了比较。在同一公鸡的腹段测得的酶活性比胸段高约8-9倍。令人惊讶的是,用苯巴比妥而非3-甲基胆蒽预处理公鸡,会使两个主动脉段的葡萄糖醛酸基转移酶活性出现小幅度(60-120%)但持续的增加。在两个段的微粒体部分以及源自主动脉段的培养平滑肌细胞中都能轻易检测到酶活性,但在培养的内皮细胞中未检测到。禽类主动脉微粒体葡萄糖醛酸基转移酶对几种常见的肝微粒体葡萄糖醛酸基转移酶激活剂的作用表现出极小的反应或无反应。

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