目的 研究制首乌活性单体化合物大黄素 - 8- O-β- D -吡喃葡萄糖苷 (PMEG)的促智活性以及作用机制。方法 小鼠跳台实验以及胆碱酯酶活力测定。结果 ig PMEG后 ,正常小鼠及东莨菪碱所致学习记忆障碍小鼠错误次数显著减少 ;离体实验和整体实验中 PMEG对酶活力具可逆性抑制作用 ,体内外酶活力恢复50%所需时间分别为 T1 /2 =115 m in,T1 /2 =165min。结论 PMEG能提高正常小鼠学习记忆功能 ,对东莨菪碱所致学习记忆障碍具防护作用 ;初步认为 PMEG作用机制是对胆碱酯酶可逆性的抑制。

Object To investigate the nootropic activity of emodin-8-O-β-D-glucopyranoside, the active principle of Radix Polygoni Multiflori Preparata(PMEG), and its mechanism of action. Methods Nootropic activity was evaluated with step down test of mice, and its nootropic mechanism studied by its antiacetylcholinesterase (anti-AchE) effect on mice brain in vivo and in vitro as determined by pectrophotometry.Results PMEG (ig) significantly improved the learning and memory of both normal and intelectual deficit mice induced by scopolamine. PMEG showed dose-dependent inhibition of AchE, and the antiacetylcholinesterase effect is reversible both in vivo and in vitro. In acute experiment, the half recovery time of AchE is 115 min, and 165 min in chronic experiment. Conclusion PMEG showed good nootropic activity, and it is a reversible AchE inhibitor.

国家自然科学基金!(29872057);上海市科技发展基金!(984319117)资助项目