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首页> 外文期刊>Tropical Animal Health and Production >Zearalenone is bioactivated in the river Buffalo (Bubalus bubalis): hepatic biotransformation
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Zearalenone is bioactivated in the river Buffalo (Bubalus bubalis): hepatic biotransformation

机译：玉米赤霉烯酮在布法罗河（Bubalus bubalis）中被生物激活：肝脏的生物转化

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摘要

Zearalenone (ZEA) as a mycoestrogen is found frequently in human foods and animal feeds. Its estrogenic effects depend on its biotransformation fate including both first- and second-phase reactions, which are predominantly governed by hydroxylation and glucuronidation, respectively. In this study, we investigate the hepatic biotransformation of ZEA in river buffalo. To evaluate the hepatic biotransformation of ZEA, both subcellular fractions of the liver were prepared. ZEA was incubated with intracellular subfractions in the presence of nicotinamide dinucleotide phosphate, and the products were determined by means of high-performance liquid chromatography. Moreover, in the same frame of experiment and in the presence of uridine diphosphate glucuronic acid, the rate of glucuronidation for substrate and products were estimated as well. We found that l-zearalenol (l-ZOL) is the major hydroxylated hepatic metabolite of ZEA produced by both studied subcellular fractions. The enzymatic kinetics analyses indicated that the l-ZOL and o-ZOL production by microsomal fraction were two- and three-fold higher than those by postmitochondrial fraction, respectively. The calculated data showed that l-ZOL is conjugated with glucuronic acid more than ZEA and o-ZOL, especially at the lower concentrations, which seems to be more applicable. Our data suggest that unlike other domestic ruminants including cattle and sheep, the hepatic biotransformation of ZEA in river buffalo results in bioactivation and formation of potent estrogenic metabolite. Moreover, at the relevant concentrations, the produced potent estrogenic metabolite is entirely conjugated with glucuronic acid and, consequently, may cause the prolongation of presence of the compound in the body due to enterohepatic cycle.
机译：玉米赤霉烯酮（ZEA）作为霉菌雌激素经常在人类食品和动物饲料中发现。它的雌激素作用取决于其生物转化的命运，包括第一阶段和第二阶段反应，分别主要由羟基化和葡萄糖醛酸化作用决定。在这项研究中，我们调查了水牛河中ZEA的肝脏生物转化。为了评估ZEA的肝生物转化，准备了肝的两个亚细胞部分。在烟酰胺二核苷酸磷酸酯存在下，将ZEA与细胞内亚组分孵育，并通过高效液相色谱法测定产物。此外，在相同的实验框架中，在尿苷二磷酸葡糖醛酸的存在下，还估算了底物和产物的葡糖醛酸化率。我们发现1-玉米赤霉烯醇（1-ZOL）是两个研究亚细胞级分产生的ZEA的主要羟基化肝代谢产物。酶动力学分析表明，微粒体级分的l-ZOL和o-ZOL产量分别比线粒体后级分的高两倍和三倍。计算数据表明，l-ZOL与葡萄糖醛酸的共轭作用大于ZEA和o-ZOL，尤其是在较低浓度下，这似乎更适用。我们的数据表明，与包括牛和羊在内的其他反刍动物不同，布法罗河中ZEA的肝生物转化可导致生物激活并形成有效的雌激素代谢物。而且，在相关浓度下，产生的有效雌激素代谢物与葡萄糖醛酸完全结合，因此，由于肠肝循环，可能导致化合物在体内的存在时间延长。

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