Schatz F, Hochberg R B
Endocrinology. 1981 Sep;109(3):697-703. doi: 10.1210/endo-109-3-697.
The incubation of estradiol with human breast tumors as well as several estrogen-responsive tissues of the rat, including dimethylbenzanthracene-induced mammary tumors, leads to the formation of a nonpolar metabolite. This compound has been called a lipoidal derivative of estradiol because of its nonpolar characteristics and because it is converted back into estradiol with alkali. The properties of this metabolite are similar to those of the endogenous lipoidal derivatives of the delta 5-3 beta-hydroxysteroids, pregnenolone, 17-hydroxypregnenolone, and dehydroisoandrosterone, that were found in the adrenal. When estrone was incubated in a similar manner, a nonpolar metabolite was formed, but it was the lipoidal derivative of estradiol, not estrone. The lipoidal derivative of estradiol was not oxidized by treatment with CrO3, which showed that the lipoidal moiety is linked to the C-17 of the steroid nucleus. Unlike other estrogen metabolites, the lipoidal derivative of estradiol is found only within the tissue and cannot be detected in the incubation medium.
雌二醇与人乳腺肿瘤以及大鼠的几种雌激素反应性组织(包括二甲基苯并蒽诱导的乳腺肿瘤)一起孵育,会导致形成一种非极性代谢物。由于其非极性特征以及它能在碱性条件下转化回雌二醇,这种化合物被称为雌二醇的类脂衍生物。这种代谢物的性质与在肾上腺中发现的δ5 - 3β - 羟基类固醇、孕烯醇酮、17 - 羟基孕烯醇酮和脱氢异雄酮的内源性类脂衍生物相似。当以类似方式孵育雌酮时,会形成一种非极性代谢物,但它是雌二醇的类脂衍生物,而非雌酮的。雌二醇的类脂衍生物经CrO3处理后不会被氧化,这表明类脂部分与甾体核的C - 17相连。与其他雌激素代谢物不同,雌二醇的类脂衍生物仅在组织内被发现,在孵育培养基中无法检测到。