Morris I D, Higgins C, Matlin S A
J Reprod Fertil. 1986 Jul;77(2):607-12. doi: 10.1530/jrf.0.0770607.
The inhibitory effect of (+)-, (-)-, (+/-)-gossypol and (+/-)-gossypol acetic acid upon testicular cytosolic LDH-X was measured in vitro. Gossypol acetic acid (0-100 mumol/l) inhibited LDH-X prepared from the testes of the mouse greater than rabbit greater than human greater than rat greater than hamster. There was no relationship between inhibition and in-vivo antifertility activity. LDH activity measured in vitro in serum of men and hamsters was unaffected by gossypol. Gossypol and its isomers were non-competitive inhibitors of human and hamster LDH-X with respect to the coenzyme NADH, competitive inhibitors of human LDH-X and noncompetitive-competitive inhibitors of hamster LDH-X with respect to the substrate alpha-ketobutyrate. Co-incubation with human serum albumin or poly-L-lysine but not lysine protected human and hamster LDH-X from gossypol.
在体外测定了（+）-、（-）-、（±）-棉酚和（±）-醋酸棉酚对睾丸胞质乳酸脱氢酶-X（LDH-X）的抑制作用。醋酸棉酚（0-100μmol/L）对从小鼠睾丸制备的LDH-X的抑制作用大于兔大于人大于大鼠大于仓鼠。抑制作用与体内抗生育活性之间没有关系。在体外测定的人和仓鼠血清中的LDH活性不受棉酚影响。棉酚及其异构体对辅酶NADH而言是人和仓鼠LDH-X的非竞争性抑制剂，对底物α-酮丁酸而言是人类LDH-X的竞争性抑制剂和仓鼠LDH-X的非竞争性-竞争性抑制剂。与人血清白蛋白或聚-L-赖氨酸共同孵育可保护人和仓鼠的LDH-X免受棉酚影响，但赖氨酸则不能。
