A facile assay for 2-hydroxylation of estradiol by liver microsomes.
A facile assay for 2-hydroxylation of estradiol by liver microsomes.
复制标题
肝微粒体对雌二醇 2-羟基化的简便测定。
DOI：
10.1016/0003-2697(81)90317-1
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发表时间：
1981
影响因子：
2.9
通讯作者：
Bulger,WH
中科院分区：
文献类型：
--
作者：
Kupfer,D;Miranda,GK;Bulger,WH
各种研究表明，C-2位羟基化是人类和大鼠雌激素代谢的主要途径（1 -4，38-40）。在大鼠检查的组织中，发现肝脏含有最高的2-羟基化活性，其次是大脑，其他组织的活性较低（5）。2-在良性和恶性人类乳腺肿瘤中也观察到羟化酶活性（3 1）。发现肝和脑（6、7、30）以及肾（27）中2-羟化酶活性的主要部分存在于微粒体组分中。相比之下，肺中的2-羟化酶在线粒体组分中最高（27）。此外，虽然肝和脑2-羟化酶似乎是细胞色素P-450介导的（17，29，30），但它对某些典型的单加氧酶诱导剂（如3-甲基胆蒽和苯巴比妥）没有显著反应（5，7）。最近的研究结果还表明，在成年大鼠脑和人胎脑、脑垂体和肝脏中存在2-羟基雌激素（5，8，9）。关于儿茶酚雌激素生物活性的某些研究结果（IO-17）表明，2-羟基化可能不完全是一种分解代谢途径，儿茶酚雌激素可能具有生物活性。直到最近，动物组织中2-羟基化的评估还涉及相对费力的程序，其中包括薄层层析（18）、放射免疫测定
Various studies have demonstrated that hydroxylation at C-2 is a major pathway of metabolism of estrogens in man and rat (l-4, 38-40). Among the tissues examined in the rat, the liver was found to contain the highest 2-hydroxylating activity, followed by the brain, with other tissues having lower activity (5). 2-Hydroxylase activity was also observed in benign and malignant human breast tumors (3 1). The major portion of the 2-hydroxylase activity in the liver and brain (6, 7, 30) and kidney (27) was found to be present in the microsomal fraction. By contrast, 2-hydroxylase in the lung was highest in the mitochondrial fraction (27). Additionally, though the liver and brain 2-hydroxylase appears to be cytochrome P-450 mediated (17, 29, 30), it does not respond significantly to certain typical inducers of monooxygenase such as 3-methylcholanthrene and phenobarbital (5, 7). Recent findings also showed the presence of 2-hydroxyestrogens in adult rat brain and in human fetus brain, pituitary, and liver (5, 8, 9). Certain findings (IO-17) on the biological activity of catechol estrogens have suggested that 2-hydroxylation is probably not entirely a catabolic pathway and that catechol estrogens may be biologically active. IJntil recently, the assessment of 2-hydroxylation in animal tissues has involved relatively laborious procedures, among these, thin-layer chromatography (18), radioimmunoassays