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核心技术专利：CN118964589B侵权必究

核心技术专利：CN118964589B侵权必究

Research Institute, Daiichi Pharmaceutical Co. Ltd, Tokyo, Japan.

Xenobiotica. 1990 Jun;20(6):619-27. doi: 10.3109/00498259009046877.

The kinetic activity of UDP-glucuronosyltransferases (UDPGT) towards a dithiol metabolite of malotilate, 2,2-di(isopropoxycarbonyl)ethylene-1,1-dithiol, was investigated using rat and rabbit hepatic microsomes. The thio-glucuronide formed was analysed by h.p.l.c. The Km values obtained using rat and rabbit UDPGT were 36.3 +/- 3.3 and 443 +/- 43 microM, respectively. The Vmax values were 7.14 +/- 0.61 and 29.2 +/- 6.4 nmol/min per mg (mean +/- SD, n = 3). 2. Phenobarbital, an inducer of the GT2 isoform of UDPGT, increased rat microsomal UDPGT activity towards the dithiol. In inhibitory studies, menthol and borneol (specific substrates for GT2a isoform) competitively inhibited glucuronidation of the dithiol. Thus it was concluded that formation of the thio-glucuronide was catalysed mainly by the GT2a isozyme of UDPGT, which is involved in glucuronidation of monoterpenoid alcohols.

使用大鼠和兔肝微粒体研究了UDP - 葡糖醛酸基转移酶（UDPGT）对马洛替酯的二硫醇代谢物2,2 - 二（异丙氧基羰基）乙烯 - 1,1 - 二硫醇的动力学活性。通过高效液相色谱法分析形成的硫代葡糖醛酸化物。使用大鼠和兔UDPGT获得的Km值分别为36.3±3.3和443±43微摩尔。Vmax值分别为7.14±0.61和29.2±6.4纳摩尔/分钟·毫克（平均值±标准差，n = 3）。2. 苯巴比妥是UDPGT的GT2同工型的诱导剂，它增加了大鼠微粒体UDPGT对二硫醇的活性。在抑制研究中，薄荷醇和冰片（GT2a同工型的特异性底物）竞争性抑制二硫醇的葡糖醛酸化。因此得出结论，硫代葡糖醛酸化物的形成主要由UDPGT的GT2a同工酶催化，该同工酶参与单萜醇的葡糖醛酸化。

Research Institute, Daiichi Pharmaceutical Co. Ltd, Tokyo, Japan.

Xenobiotica. 1990 Jun;20(6):619-27. doi: 10.3109/00498259009046877.

The kinetic activity of UDP-glucuronosyltransferases (UDPGT) towards a dithiol metabolite of malotilate, 2,2-di(isopropoxycarbonyl)ethylene-1,1-dithiol, was investigated using rat and rabbit hepatic microsomes. The thio-glucuronide formed was analysed by h.p.l.c. The Km values obtained using rat and rabbit UDPGT were 36.3 +/- 3.3 and 443 +/- 43 microM, respectively. The Vmax values were 7.14 +/- 0.61 and 29.2 +/- 6.4 nmol/min per mg (mean +/- SD, n = 3). 2. Phenobarbital, an inducer of the GT2 isoform of UDPGT, increased rat microsomal UDPGT activity towards the dithiol. In inhibitory studies, menthol and borneol (specific substrates for GT2a isoform) competitively inhibited glucuronidation of the dithiol. Thus it was concluded that formation of the thio-glucuronide was catalysed mainly by the GT2a isozyme of UDPGT, which is involved in glucuronidation of monoterpenoid alcohols.

使用大鼠和兔肝微粒体研究了UDP - 葡糖醛酸基转移酶（UDPGT）对马洛替酯的二硫醇代谢物2,2 - 二（异丙氧基羰基）乙烯 - 1,1 - 二硫醇的动力学活性。通过高效液相色谱法分析形成的硫代葡糖醛酸化物。使用大鼠和兔UDPGT获得的Km值分别为36.3±3.3和443±43微摩尔。Vmax值分别为7.14±0.61和29.2±6.4纳摩尔/分钟·毫克（平均值±标准差，n = 3）。2. 苯巴比妥是UDPGT的GT2同工型的诱导剂，它增加了大鼠微粒体UDPGT对二硫醇的活性。在抑制研究中，薄荷醇和冰片（GT2a同工型的特异性底物）竞争性抑制二硫醇的葡糖醛酸化。因此得出结论，硫代葡糖醛酸化物的形成主要由UDPGT的GT2a同工酶催化，该同工酶参与单萜醇的葡糖醛酸化。