Aromatase activity in the mare ovary during estrous cycle. Measurement of endogenous steroids and of their in vitro inhibitory effect.

H Amri, P Silberzahn, I al-Timimi, J L Gaillard
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引用次数: 19

Abstract

This present study was undertaken to clarify estrogen synthesis in the mare ovary. First of all, an evaluation of endogenous steroid contents was carried out in the follicular fluid and in the luteal tissue at different stages of the luteal phase. Radioimmunoassays were performed after separation and purification of each hormone by chromatography. High amounts of conjugated (0.9 mg/l) and unconjugated (4 mg/l) estradiol-17 beta were found in the follicular fluid of the large follicules (50 mm). These concentrations of estrogens decreased drastically in the luteal tissue, and only low levels of circulating estrogens are found during the luteal phase. On the other hand, a high aromatization ability has been evidenced in the cyclic corpus luteum in vitro. In an attempt to clarify the regulation of estrogen synthesis, we have tested the inhibitory effect of several endogenous steroids on equine ovarian aromatase activity. 5 alpha-Dihydrotestosterone appeared to be the most potent competitive inhibitor (Ki = 181 nmol/l) of aromatase activity, while the addition of a 3-sulfate group induced a slump in the inhibitory potency of estrone (Ki = 397 nmol/l vs 2206 nmol/l) and dehydroepiandrosterone (Ki = 291 nmol/l vs 6157 nmol/l). The physiological role of these conjugated steroids has not been known until now; we suggest that they would play a role in protecting aromatase from inhibition, in vivo. The high amounts of progesterone found in the luteal tissue (1.3 g/kg of proteins) might play a role in the regulation of estrogen production either by suppressing the induction of aromatase synthesis or by inhibiting the activity of the enzyme complex.

发情周期中母马卵巢芳香酶活性的变化。内源性类固醇的测定及其体外抑制作用。
本研究旨在阐明雌性激素在母马卵巢中的合成。首先,对黄体期不同阶段卵泡液和黄体组织中的内源性类固醇含量进行了评估。各激素经层析分离纯化后进行放射免疫测定。在大卵泡(50 mm)的卵泡液中发现大量共轭雌二醇-17 β (0.9 mg/l)和非共轭雌二醇-17 β (4mg /l)。这些雌激素浓度在黄体组织中急剧下降,在黄体期只发现低水平的循环雌激素。另一方面,体外环黄体具有较高的芳构化能力。为了阐明雌激素合成的调控,我们测试了几种内源性类固醇对马卵巢芳香酶活性的抑制作用。α -二氢睾酮是芳香化酶活性最有效的竞争性抑制剂(Ki = 181 nmol/l),而3-硫酸盐基团的加入导致雌酮(Ki = 397 nmol/l vs 2206 nmol/l)和脱氢表雄酮(Ki = 291 nmol/l vs 6157 nmol/l)的抑制效力下降。这些缀合类固醇的生理作用直到现在还不为人所知;我们认为它们可能在体内发挥保护芳香酶免受抑制的作用。黄体组织中发现的大量黄体酮(1.3 g/kg蛋白质)可能通过抑制芳香化酶合成的诱导或通过抑制酶复合物的活性来调节雌激素的产生。
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