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在培养的人胎儿肝细胞中,暴露于氯化汞时高亲和力形式的尿苷二磷酸葡萄糖醛酸基转移酶的表达。

Expression of a high-affinity form of UDP-glucuronosyltransferase in human foetal liver cells in culture on exposure to mercuric chloride.

作者信息

Tan T M, Wong K P, Sit K H

机构信息

Department of Biochemistry, Faculty of Medicine, National University of Singapore.

出版信息

Biochem J. 1991 Aug 15;278 ( Pt 1)(Pt 1):99-103. doi: 10.1042/bj2780099.

Abstract

The activity of UDP-glucuronosyltransferase (UDPGT, EC 2.4.1.17) in human foetal liver cells in culture was measured with two acceptor substrates, namely harmol and 1-naphthol. There was a dose-dependent increase of about 10-400% in UDPGT activity when the cells were exposed to 1-30 microM-HgCl2. Above a critical concentration of 30 microM-HgCl2, the heavy metal ion was toxic to the cells. Kinetic studies of the glucuronidation reaction with harmol and 1-naphthol showed that Hg2+ ions seemed to induce the expression of a high-affinity form of UDPGT, which was absent from the normal controls. The dramatic increase in specific activity in UDPGT was accompanied by a parallel increase in Vmax. measured with harmol and UDP-glucuronic acid. The significance of a possible induction of UDPGT in human foetal liver cells by HgCl2 is discussed.

摘要

利用两种受体底物——去甲骆驼蓬碱和1-萘酚,测定了培养的人胎儿肝细胞中尿苷二磷酸葡萄糖醛酸基转移酶(UDPGT,EC 2.4.1.17)的活性。当细胞暴露于1-30微摩尔/升的氯化汞时,UDPGT活性呈剂量依赖性增加,增幅约为10%-400%。当氯化汞浓度超过临界值30微摩尔/升时,这种重金属离子对细胞有毒性。对去甲骆驼蓬碱和1-萘酚的葡萄糖醛酸化反应进行的动力学研究表明,汞离子似乎诱导了一种高亲和力形式的UDPGT的表达,而正常对照组中不存在这种形式。UDPGT比活性的显著增加伴随着用去甲骆驼蓬碱和尿苷二磷酸葡萄糖醛酸测得的Vmax的平行增加。文中讨论了氯化汞可能诱导人胎儿肝细胞中UDPGT的意义。

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The pharmacology of mercury compounds.汞化合物的药理学。
Annu Rev Pharmacol. 1972;12:375-406. doi: 10.1146/annurev.pa.12.040172.002111.

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