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首页> 外文期刊>Biophysical Chemistry: An International Journal Devoted to the Physical Chemistry of Biological Phenomena >Ac-LVFFARK-NH2 conjugation to beta-cyclodextrin exhibits significantly enhanced performance on inhibiting amyloid beta-protein fibrillogenesis and cytotoxicity
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Ac-LVFFARK-NH2 conjugation to beta-cyclodextrin exhibits significantly enhanced performance on inhibiting amyloid beta-protein fibrillogenesis and cytotoxicity

机译：对β-环糊精的AC-LVFFARK-NH2缀合在抑制淀粉样蛋白β-蛋白原纤维生殖和细胞毒性上显着提高了性能

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摘要

Inhibition of amyloid beta-protein (A beta) aggregation is of significance for the potential treatment of Alzheimer's disease. We have herein conjugated heptapeptide Ac-LVFFARK-NH2 (LK7) to beta-cyclodextrin (beta CyD) and studied the inhibitory effect of the LK7-beta CyD conjugate on AA aggregation. The conjugation significantly improved the peptide solubility and suppressed the self-assembly propensity. This led to 30% increase of the binding affinity of LK7 for A beta in the conjugate due to increased hydrophobic interactions. Thus, LK7-beta CyD suppressed the conformational transition of A beta and showed stronger inhibitory effect on A beta fibrillation than LK7. Thus, LK7-beta CyD exhibited protective effect on A beta(40)-induced cytotoxicity, and the cells completely survived at 10 molar excess of LK7-beta CyD (from 67% to 100%). By contrast, LK7 showed only a moderate inhibition on A beta fibrillation, and could not inhibit the amyloid cytotoxicity. The research proved that conjugation of hydrophobic peptide to beta CyD was promising to increase its inhibition potency against A beta aggregation.
机译：抑制淀粉样蛋白β-蛋白（Aβ）聚集对阿尔茨海默病的潜在治疗具有重要意义。我们对β-环糊精（Beta Cyd）的缀合的庚肽AC-LVFFARK-NH2（LK7）进行了缀合的庚肽AC-LVFFARK-NH2（LK7），并研究了LK7-BETA CYD缀合物对AA聚集的抑制作用。缀合显着改善了肽溶解度并抑制了自组装倾向。由于增加的疏水相互作用，这导致LK7在缀合物中对β的结合亲和力增加30％。因此，LK7-Beta Cyd抑制了β的构象转变，并且对β纤维化的抑制作用较强，而不是LK7。因此，LK7-βCyd对β（40）诱导的细胞毒性表现出保护作用，并且细胞完全存活在10摩尔过量的LK7-β - β - β - β - β - β - β - β - β - β - β - β - β - β - β - β - β - β - β - β - β - β - Beta Cyd（从67％到100％）。相比之下，LK7仅显示对β纤维化的适度抑制，并且不能抑制淀粉样蛋白细胞毒性。该研究证明，疏水肽与βCyd的缀合是有希望增加其对β聚集的抑制效力。

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