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CN106397540A 一种抑制淀粉样β蛋白聚集的双功能短肽抑制剂及其应用 无效 - 撤回

一种抑制淀粉样β蛋白聚集的双功能短肽抑制剂及其应用
摘要：
本发明涉及一种抑制淀粉样β蛋白(Aβ)聚集的双功能短肽抑制剂及其应用。首先从Aβ的经典抑制剂LPFFD序列出发理性设计了双功能短肽抑制剂LVFFARKHH，然后通过多种实验手段证明该双功能短肽抑制剂与Aβ40摩尔浓度比在1:1时，对Aβ40聚集及其相关细胞毒性具备最佳抑制效果：能有效地抑制Aβ40纤维生成；可显著地抑制Cu2+介导的Aβ40聚集；改变Aβ40聚集路径，造成Aβ40纤维形貌的变化；可极大的降低Aβ-Cu2+络合体催化产生氧化自由基·OH的速率；最终大幅度降低Cu2+存在下Aβ40聚集产生的细胞毒性作用。该双功能短肽抑制剂提供了用于阿尔兹海默症的原料药和保健品开发方面的用途。
摘要（英）：

The invention relates to a bifunctional oligopeptide inhibitor for inhibiting amyloid beta (A beta) protein aggregation and application thereof. Firstly, from the A beta classical inhibitor LPFFD sequence, the bifunctional oligopeptide inhibitor LVFFARKHH is rationally designed; various experiment measures prove that when the molar concentration ratio of the bifunctional oligopeptide inhibitor to the A beta 40 is 1:1, the optimal inhibition effect is achieved on the A beta 40 aggregation and relevant cytotoxicity; the A beta 40 fiber generation can be effectively inhibited; A beta 40 aggregation mediated by the Cu<2+> can be obviously inhibited; the A beta 40 aggregation path is changed, the A beta 40 fiber morphology change is caused; the velocity of generating oxyradical.OH by A beta-Cu<2+> complexes through catalysis is greatly reduced; finally, the cytotoxicity effect generated by the A beta 40 aggregation under the existence of Cu<+2> is greatly reduced. The bifunctional oligopeptide inhibitor provides raw medicine for Alzheimer's diseases and application in health care product development aspect.

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