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一种丁内酯衍生物和自噬抑制剂;在60µM时增加HUVECs中EIF4EBP1和RPS6KB1/p70S6K1的磷酸化水平;在60µM时阻止HUVECs中雷帕霉素诱导的MAP1LC3B斑点形成;在40µg/ml时抑制血清和FGF2剥夺诱导的凋亡、衰老以及整合素β4水平的增加;在AβPP/PS1转基因阿尔茨海默病小鼠模型中,以80mg/kg剂量每日给药,减少皮层和海马的淀粉样斑块负荷,抑制大脑中的自噬,并改善学习和记忆缺陷。A butyrolactone derivative and autophagy inhibitor; increases phosphorylation of EIF4EBP1 and RPS6KB1/p70S6K1 in HUVECs at 60 μM; prevents rapamycin-induced MAP1LC3B puncta formation in HUVECs at 60 μM; inhibits apoptosis, senescence, and increases in integrin β4 levels induced by serum- and FGF2-deprivation in at 40 μg/ml; reduces cortical and hippocampal amyloid plaque burden, inhibits autophagy in the brain, and rescues learning and memory deficits in the AβPP/PS1 transgenic mouse model of Alzheimer's disease at 80 mg/kg per day.
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