棉酚对猪睾丸中不依赖环核苷酸的卵黄高磷蛋白激酶的抑制作用。

Inhibition by gossypol of cyclic nucleotide-independent phosvitin kinase from pig testis.

作者信息

Katoh N, Kimura K

出版信息

Nihon Juigaku Zasshi. 1989 Feb;51(1):105-9. doi: 10.1292/jvms1939.51.105.

DOI:10.1292/jvms1939.51.105

Abstract

Gossypol, a male anti-fertility agent, was found to be an inhibitor of cyclic nucleotide-independent phosvitin kinase from pig testis. The IC50 value (concentration causing 50% inhibition) was 42 microM using phosvitin as substrate. Kinetic analysis indicated that the compound inhibited the enzyme noncompetitively with respect to ATP (Ki = 17 microM) and competitively with respect to phosvitin (Ki = 11 microM). The gossypol inhibition was reversed by the addition of polyamines. The compound also inhibited phosphorylation of high mobility group (HMG) proteins HMG 14 and 17 (the endogenous substrates in the testis located in nucleosome), with an IC50 value of 48 microM.

摘要

棉酚是一种男性抗生育剂，它被发现是猪睾丸中不依赖环核苷酸的卵黄高磷蛋白激酶的抑制剂。以卵黄高磷蛋白为底物时，半数抑制浓度（IC50值，即引起50%抑制的浓度）为42微摩尔。动力学分析表明，该化合物对ATP呈非竞争性抑制（抑制常数Ki = 17微摩尔），对卵黄高磷蛋白呈竞争性抑制（Ki = 11微摩尔）。添加多胺可逆转棉酚的抑制作用。该化合物还抑制高迁移率族（HMG）蛋白HMG 14和17（睾丸中位于核小体的内源性底物）的磷酸化，IC50值为48微摩尔。