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Proanthocyanidins for the treatment of amyloid and alpha-synuclein diseases such as alzheimer's disease and parkinson's
Proanthocyanidins for the treatment of amyloid and alpha-synuclein diseases such as alzheimer's disease and parkinson's
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机译:原花青素用于治疗淀粉样蛋白和α-突触核蛋白疾病,例如阿尔茨海默氏病和帕金森氏病
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摘要
A method of treating amyloid, alpha-synuclein or NAC fibrillogenesis in an in vitro environment comprises administrating into the in vitro environment a proanthocyanidin selected from proanthocyanidin characterized by Formula I or Formula II and proanthocyanidin characterized by oligomeric combinations of Formula I and II wherein: n is 2 to 20 R1 and R2 are hydrogen or Hydroxy R3 is hydrogen, optionally substituted O-glycosyl, -C(O)-(optionally substituted aryl) or BC(O)-(optionally substituted heteroaryl); R4 is hydrogen, catechin, epicatechin, epifzelechin or galletes of catechin and epicatechin; The lines at the 2-, 3-, and 4- positions denote R and S configurations; The lines at the 4- and 8- positions in Formula I and the 4- and 6- positions in Formula II denote possible oligomer bonds between individual units. Pharmaceutical compositions can comprises the compounds described, for the treatment of an amyloid disease, or a disease characterized by alpha-synuclein or NAC fibrillogenesis. A method for isolating proanthocyanidin from a plant material comprise dissolving the plant material with ethanol or methanol, or then loading the ethanol/methanol-extracted plant material onto a LH20 column or silica gel column, and eluting the column with a series of increasing proportions of ethanol/methanol to elute the proanthocyanidins and then separating the proanthocyanidin in the extract by reverse phase HPLC and collecting and freeze drying the pure proanthocyanidin.
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机译:在体外环境中治疗淀粉样蛋白,α-突触核蛋白或NAC原纤维形成的方法包括向体外环境中施用原花青素,原花青素选自特征为式I或式II的原花青素和特征为式I和II的低聚组合的原花青素,其中: R 2是2至20,R 1和R 2是氢或羟基R 3是氢,任选取代的O-糖基,-C(O)-(任选取代的芳基)或BC(O)-(任选取代的杂芳基); R4是氢,儿茶素,表儿茶素,表儿茶素或儿茶素和表儿茶素的加仑; 2、3和4位的线表示R和S构型;式I中的4位和8位以及式II中的4位和6位的线表示各个单元之间可能的低聚物键。药物组合物可以包含用于治疗淀粉样疾病或以α-突触核蛋白或NAC原纤维形成为特征的疾病的所述化合物。从植物材料中分离原花色素的方法包括用乙醇或甲醇溶解植物材料,或将乙醇/甲醇提取的植物材料加载到LH20柱或硅胶柱上,并用一系列递增比例的洗脱剂洗脱该柱。用乙醇/甲醇洗脱原花青素,然后通过反相HPLC分离提取物中的原花青素,然后收集并冷冻干燥纯原花青素。
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