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棉酚对人体组织氧化还原酶的体外抑制作用。

In vitro inhibition by gossypol of oxidoreductases from human tissues.

作者信息

Burgos C, Gerez de Burgos N M, Rovai L E, Blanco A

出版信息

Biochem Pharmacol. 1986 Mar 1;35(5):801-4. doi: 10.1016/0006-2952(86)90248-0.

Abstract

The effect of gossypol, a polyphenolic compound with antifertility action on human males, has been investigated on the following oxidoreductases purified from human tissues: lactate dehydrogenase (EC 1.1.1.27) isozymes 1 or B4 from heart, 5 or A4 from liver and X or C4 from spermatozoa; malate dehydrogenase (EC 1.1.1.37) mitochondrial and "soluble" isozymes from heart and NADP-glutamate dehydrogenase (EC 1.4.1.4) from liver. Gossypol proved to be a powerful inhibitor of the six enzymes studied. For all of them, inhibition was of the competitive type with respect to the coenzyme and non-competitive in relation to substrate. The lowest ki values were shown for lactate dehydrogenase isozyme 1 or B4 and for the two isozymes of malate dehydrogenase. Results did not show selectivity of gossypol for the sperm-specific isozyme X or C4 of lactate dehydrogenase.

摘要

棉酚是一种对人类男性具有抗生育作用的多酚类化合物,人们已对其对从人体组织中纯化出的以下氧化还原酶的影响进行了研究:心脏中的乳酸脱氢酶(EC 1.1.1.27)同工酶1或B4、肝脏中的同工酶5或A4以及精子中的同工酶X或C4;心脏中的苹果酸脱氢酶(EC 1.1.1.37)线粒体同工酶和“可溶性”同工酶,以及肝脏中的NADP - 谷氨酸脱氢酶(EC 1.4.1.4)。结果表明棉酚是所研究的这六种酶的强效抑制剂。对于所有这些酶而言,其抑制作用对于辅酶来说属于竞争性类型,而对于底物来说则属于非竞争性类型。乳酸脱氢酶同工酶1或B4以及苹果酸脱氢酶的两种同工酶的抑制常数(ki)值最低。结果未显示棉酚对乳酸脱氢酶精子特异性同工酶X或C4具有选择性。

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