通过抑制类固醇硫酸酯酶增强血浆脱氢表雄酮硫酸盐、脑乙酰胆碱及记忆力。
Enhanced plasma DHEAS, brain acetylcholine and memory mediated by steroid sulfatase inhibition.
作者信息
Rhodes M E, Li P K, Burke A M, Johnson D A
机构信息
Division of Pharmacology-Toxicology, Graduate School of Pharmaceutical Sciences, Duquesne University, Pittsburgh, PA 15282, USA.
出版信息
Brain Res. 1997 Oct 31;773(1-2):28-32. doi: 10.1016/s0006-8993(97)00867-6.
Steroid sulfatase inhibitors can alter the metabolism of neurosteroids which modulate brain function. Administration of the non-steroidal steroid sulfatase inhibitor (p-O-sulfamoyl)-N-tetradecanoyl tyramine (DU-14) to rats for 15 days increased plasma dehydroepiandrosterone sulfate (DHEAS) concentrations by 88.2%, decreased plasma dehydroepiandrosterone (DHEA) concentrations by 84.6%, increased hippocampal acetylcholine (ACh) release determined via in vivo microdialysis by almost 3-fold, and produced a significant blockade of scopolamine-induced amnesia as measured by a passive avoidance test. These results suggest DHEAS rather than DHEA enhances brain cholinergic function and that steroid sulfatase inhibition may become an important tool for enhancing neuronal functions, such as memory, mediated by excitatory neurosteroids.
类固醇硫酸酯酶抑制剂可改变调节脑功能的神经甾体的代谢。给大鼠连续15天施用非甾体类固醇硫酸酯酶抑制剂（对-氧-氨磺酰基）-N-十四烷酰酪胺（DU-14），可使血浆硫酸脱氢表雄酮（DHEAS）浓度增加88.2%，使血浆脱氢表雄酮（DHEA）浓度降低84.6%，通过体内微透析测定，海马乙酰胆碱（ACh）释放增加近3倍，并通过被动回避试验测量，对东莨菪碱诱导的失忆产生显著阻断作用。这些结果表明，DHEAS而非DHEA可增强脑胆碱能功能，且抑制类固醇硫酸酯酶可能成为增强由兴奋性神经甾体介导的神经元功能（如记忆）的重要工具。
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