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内源性木脂素——一种潜在的内源性洋地黄类药物。

Endogenous lignans--a potential endogenous digitalis.

作者信息

Braquet P, Senn N, Robin J P, Esanu A, Garay R P

出版信息

J Hypertens Suppl. 1986 Dec;4(5):S161-4.

PMID:2437273
Abstract

Lignans are natural products formed by oxidative dimerization of monomeric phenols. A few were recently discovered in human and animal urine, semen and blood plasma but their role has never been assessed. We investigated the actions of mammalian lignans obtained by total synthesis or extracted from the urine of pregnant women, on the Na+K+-pump in human red cells. Some of the tested lignans (enterolactone, prestegane B and 3-O-methylenterolactone) inhibited the Na+K+-pump activity with IC50 ranging from 5 to 9 X 10(-4) mol/l. The IC50 for ouabain (7 X 10(-7) mol/l) was not modified by addition of lignans suggesting a non-competitive inhibition.

摘要

木脂素是由单体酚氧化二聚形成的天然产物。最近在人和动物的尿液、精液及血浆中发现了几种木脂素,但它们的作用从未被评估过。我们研究了通过全合成获得或从孕妇尿液中提取的哺乳动物木脂素对人红细胞中钠钾泵的作用。一些测试的木脂素(肠内酯、前孕二烯酮B和3 - O - 甲基肠内酯)抑制钠钾泵活性,半数抑制浓度(IC50)范围为5至9×10⁻⁴摩尔/升。添加木脂素后,哇巴因的IC50(7×10⁻⁷摩尔/升)未发生改变,提示为非竞争性抑制。

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