Pearce S, Sufi S B, O'Shaughnessy P J, Donaldson A, Jeffcoate S L
J Steroid Biochem. 1986 Nov;25(5A):683-7. doi: 10.1016/0022-4731(86)90011-7.
Gossypol, a phenolic compound that has been studied as a potential male contraceptive, inhibits basal and LH-stimulated testosterone release from Leydig cells in vitro. The present study investigates the mechanism of this inhibition using preparations of purified mouse Leydig cells. Gossypol inhibited LH-stimulated progesterone, 17-hydroxyprogesterone and androstenedione production by mouse Leydig cells incubated in vitro. It also inhibited dibutyryl cyclic AMP-stimulated production of testosterone but was without effect in the presence of added pregnenolone or 25-hydroxycholesterol. These results suggest gossypol exerts its major inhibitory effect on Leydig cell function at a point between LH-dependent stimulation of cyclic AMP dependent protein kinase activity and increased availability of cholesterol for side chain cleavage.
棉酚是一种已被研究作为潜在男性避孕药的酚类化合物，它在体外可抑制睾丸间质细胞基础状态下以及促黄体生成素（LH）刺激后的睾酮释放。本研究使用纯化的小鼠睾丸间质细胞制剂来探究这种抑制作用的机制。棉酚抑制了体外培养的小鼠睾丸间质细胞在LH刺激下的孕酮、17-羟孕酮和雄烯二酮的生成。它还抑制了二丁酰环磷腺苷（dibutyryl cyclic AMP）刺激的睾酮生成，但在添加孕烯醇酮或25-羟胆固醇的情况下没有作用。这些结果表明，棉酚在LH依赖的环磷腺苷依赖性蛋白激酶活性刺激与胆固醇用于侧链裂解的可用性增加之间的某个点上，对睾丸间质细胞功能发挥其主要抑制作用。
