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Wogonin glucuronidation in liver and intestinal microsomes of humans, monkeys, dogs, rats, and mice.
Xenobiotica ( IF 1.3 ) Pub Date : 2020-02-12 , DOI: 10.1080/00498254.2020.1725180
Nobumitsu Hanioka 1 , Takashi Isobe 1 , Toshiko Tanaka-Kagawa 1 , Susumu Ohkawara 1
Affiliation  

  1. Wogonin, one of the flavonoids isolated from Scutellaria baicalensis, exhibits some beneficial bioactivities, including anti-inflammatory and anticancer effects, and is metabolized into glucuronide by UDP-glucuronosyltransferase (UGT) enzymes in humans. In the present study, wogonin glucuronidation was examined in the liver and intestinal microsomes of humans, monkeys, dogs, rats, and mice using a kinetic analysis.

  2. The kinetics of wogonin glucuronidation by liver microsomes followed the biphasic model in all species examined. CLint values (x-intercept) based on v versus V/[S] plots were rats > humans ≈ monkeys > mice > dogs. The kinetics of intestinal microsomes fit the Michaelis–Menten model for humans, monkeys, rats, and mice and the substrate inhibition model for dogs. CLint values were rats > monkeys > mice > dogs > humans. The tissue dependence of CLint values was liver microsomes > intestinal microsomes for humans, dogs, and rats, and liver microsomes ≈ intestinal microsomes for monkeys and mice.

  3. These results demonstrated that the metabolic abilities of UGT enzymes toward wogonin in the liver and intestines markedly differ among humans, monkeys, dogs, rats, and mice, and suggest that species differences are closely associated with the biological effects of wogonin.



中文翻译:

人,猴,狗,大鼠和小鼠的肝和肠微粒体中的Wogonin葡萄糖醛酸苷化作用。

  1. Wogonin是从cut中分离出的一种黄酮类化合物,具有一些有益的生物活性,包括抗炎和抗癌作用,并且可以通过人体内的UDP-葡萄糖醛酸转移酶(UGT)酶代谢为葡萄糖醛酸。在本研究中,使用动力学分析检查了人,猴,狗,大鼠和小鼠的肝脏和肠微粒体中的wogonin葡萄糖醛酸苷化作用。

  2. 在所有检查的物种中,肝微粒体对wogonin葡萄糖醛酸苷化的动力学遵循双相模型。基于vV / [ S ]的图的CL int值(x截距)为大鼠>人≈猴子>小鼠>狗。肠道微粒体的动力学适合人类,猴子,大鼠和小鼠的Michaelis–Menten模型,以及适合狗的底物抑制模型。CL int值是大鼠>猴子>小鼠>狗>人类。CL int值的组织依赖性是人,狗和大鼠的肝微粒体>肠微粒体,而猴和小鼠的肝微粒体≈肠微粒体。

  3. 这些结果表明,人,猴,狗,大鼠和小鼠中,UGT酶对肝和肠中wogonin的代谢能力明显不同,并且表明物种差异与wogonin的生物学效应密切相关。

更新日期:2020-02-12
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