Münch G, Taneli Y, Schraven E, Schindler U, Schinzel R, Palm D, Riederer P
Department of Psychiatry, University of Würzburg, Federal Republic of Germany.
J Neural Transm Park Dis Dement Sect. 1994;8(3):193-208. doi: 10.1007/BF02260940.
Non-enzymatic glycosylation of proteins, also called Maillard reaction, which occurs at an accelerated rate in diabetes, can lead to the formation of advanced glycosylation endproducts (AGEs). Tenilsetam (CAS 997: (+/-)-3-(2-thienyl)-2-piperazinone), a cognition-enhancing drug successfully used for treatment of patients suffering from Alzheimer's disease, when included in the Maillard reaction apparently inhibits protein crosslinking by AGEs in vitro. According to the mechanism proposed, Tenilsetam acts via covalent attachment to glycated proteins, thus blocking the reactive sites for further polymerisation reactions. A beneficial effect of Tenilsetam in Alzheimer's disease could come from the interference with AGE-derived crosslinking of amyloid plaques and a decreased inflammatory response by diminished activation of phagocytosing microglia.
蛋白质的非酶糖基化，也称为美拉德反应，在糖尿病患者中会加速发生，可导致晚期糖基化终产物（AGEs）的形成。替奈西坦（化学物质登记号997：(+/-)-3-(2-噻吩基)-2-哌嗪酮）是一种成功用于治疗阿尔茨海默病患者的认知增强药物，当它参与美拉德反应时，在体外显然可抑制AGEs引起的蛋白质交联。根据提出的机制，替奈西坦通过与糖化蛋白共价结合起作用，从而阻断进一步聚合反应的活性位点。替奈西坦在阿尔茨海默病中的有益作用可能源于对淀粉样斑块AGE衍生交联的干扰以及通过减少吞噬性小胶质细胞的激活而降低炎症反应。
