5-氢过氧化二十碳四烯酸是神经元钠钾-ATP酶活性的强效抑制剂。
5-HPETE is a potent inhibitor of neuronal Na+, K(+)-ATPase activity.
作者信息
Foley T D
机构信息
Section on Neurochemistry, LCS, DICBR, National Institute on Alcohol Abuse and Alcoholism, NIH, Rockville, Maryland 20852, USA.
出版信息
Biochem Biophys Res Commun. 1997 Jun 18;235(2):374-6. doi: 10.1006/bbrc.1997.6790.
The effects of 1 microM concentrations of arachidonic acid hydroperoxide (HPETES) products of 5-, 12- and 15-lipoxygenase on Na+, K(+)-ATPase activity were investigated in synaptosomal membrane preparations from rat cerebral cortex. 5-HPETE inhibited Na+, K(+)-ATPase activity by up to 67 %. In contrast, 12-HPETE and 15-HPETE did not inhibit Na+, K(+)-ATPase activity. In addition, neither 5-HETE or LTA4 inhibited Na+, K(+)-ATPase activity. Dose-response studies indicated that 5-HPETE was a potent (IC25 = 10(-8) M) inhibitor of Na+, K(+)-ATPase activity. These findings indicate that 5-HPETE inhibits Na+, K(+)-ATPase activity by a mechanism that is dependent on the hydroperoxide position and independent of further metabolism by 5-lipoxygenase. It is proposed that 5-HPETE production by 5-lipoxygenase and subsequent inhibition of neuronal Na+, K(+)-ATPase activity may be a mechansim for modulating synaptic transmission.
在大鼠大脑皮层突触体膜制剂中，研究了5-、12-和15-脂氧合酶产生的1微摩尔浓度花生四烯酸氢过氧化物（HPETEs）产物对Na +、K(+)-ATP酶活性的影响。5-HPETE可使Na +、K(+)-ATP酶活性抑制高达67%。相比之下，12-HPETE和15-HPETE并不抑制Na +、K(+)-ATP酶活性。此外，5-HETE或LTA4均不抑制Na +、K(+)-ATP酶活性。剂量反应研究表明，5-HPETE是Na +、K(+)-ATP酶活性的强效抑制剂（IC25 = 10(-8) M）。这些发现表明，5-HPETE通过一种依赖于氢过氧化物位置且独立于5-脂氧合酶进一步代谢的机制抑制Na +、K(+)-ATP酶活性。有人提出，5-脂氧合酶产生5-HPETE以及随后对神经元Na +、K(+)-ATP酶活性的抑制可能是调节突触传递的一种机制。
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