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Bioassay-guided Isolation and Identification of a Acetylcholinesterase Inhibitors from Calophyllum polyanthum

机译:Calophyllum polyanthum乙酰胆碱酯酶抑制剂的生物测定引导和鉴定

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A significant acetylcholinesterase inhibitory activity was observed for the Ethanolic extract from the leaves of Calophyllum polyanthum by using TLC bioautographic method. Further bioassay-guided isolation of this extract using TLC bioautographic method resulted in obtaining a pyranochromanone, apetalic acid (1). The structure of 1 was identified by comparison of it's spectral characteristics with previous reports. The concentration required for 50% inhibition of 1 was 0.95 mM, determined by a microplate assay. The anti-acetylcholinesterase aity of compound 1 was weak, but it was the first pyranochromanone which have anti-acetyl cholinesterase activity. As a new leading compound, it can be modified and transformed to obtain more potently active compounds.
机译:通过使用TLC BioActooth方法,观察到来自Calophyllum Polyanthum叶片的乙醇提取物的显着乙酰胆碱酯酶抑制活性。使用TLC生物法析方法的进一步生物测定引导的该提取物的分离导致获得吡喃化酮,绝经酸(1)。通过将其与先前报告的光谱特性进行比较来识别1的结构。 50%抑制1的浓度为0.95mm,由微孔盐测定确定。化合物1的抗乙酰胆碱酯酶Aity弱,但它是具有抗乙酰胆碱酯酶活性的第一种吡喃混像酮。作为一种新的主​​要化合物,可以改性和转化以获得更易于活性的化合物。

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