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牛体内14C标记雌二醇代谢产物的分离与鉴定

Isolation and identification of metabolites of 14C-labeled estradiol in cattle.

作者信息

Kaltenbach C C, Dunn T G, Koritnik D R, Tucker W F, Batson D B, Staigmiller R B, Niswender G D

出版信息

J Toxicol Environ Health. 1976 Mar;1(4):607-16. doi: 10.1080/15287397609529361.

Abstract

A total of six steers and six heifers received three daily injections containing either 200 muCi (1 mg) of [4-14C] estradiol-17beta or 312 muCi (2.16 mg) of [4-14C] estradiol 17beta 3-benzoate. Major metabolites of the administered estradiol-17beta and estradiol-17beta 3-benzoate were identified in muscle, fat, liver, and kidney samples obtained 3 hr after the final injection. Estradiol benzoate was nondetectable in the tissues analyzed, suggesting rapid hydrolysis of the benzoate ester. Consequently, the relative proportions of the various metabolites were similar for both the injected estrogens. Estradiol-17beta and estrone, which together accounted for 80-90% of the total extracted radioactivity, appear to be the major metabolites in both muscle and fats. In contrast, the major metabolites present in liver and kidney appear in the conjugate fraction. Most of the conjugated metabolites were glucuronates, which represent 85-95% of the total recovered conjugate radioactivity.

摘要

总共六头公牛和六头母牛每天接受三次注射,注射物分别含有200微居里(1毫克)的[4-¹⁴C]雌二醇-17β或312微居里(2.16毫克)的[4-¹⁴C]雌二醇17β 3-苯甲酸盐。在最后一次注射后3小时采集的肌肉、脂肪、肝脏和肾脏样本中,鉴定出了所施用的雌二醇-17β和雌二醇-17β 3-苯甲酸盐的主要代谢产物。在所分析的组织中未检测到苯甲酸雌二醇,这表明苯甲酸酯迅速水解。因此,两种注射雌激素的各种代谢产物的相对比例相似。雌二醇-17β和雌酮占总提取放射性的80-90%,似乎是肌肉和脂肪中的主要代谢产物。相比之下,肝脏和肾脏中的主要代谢产物出现在结合物部分。大多数结合代谢产物是葡萄糖醛酸酯,占回收的结合物放射性总量的85-95%。

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