槟榔子中抗血小板聚集及抑制乙酰胆碱酯酶活性的有效成分(英文)

Identification of antiplatelet and acetylcholinesterase inhibitory constituents in betel nut

目的:研究槟榔子(Areca catechu)粗提取物中所含的抗血小板聚集及抑制乙酰胆碱酯酶活性的有效成分及其作用机制。方法:使用70%甲醇水溶液对槟榔子进行粗提取。使用生物发光血小板凝集仪在富血小板血浆中测定槟榔子粗提取物的抗血小板聚集作用,使用分光光度计在试管内测定槟榔子粗提取物对乙酰胆碱酯酶活性的抑制作用。检测槟榔子中的多种化合物以测定槟榔子中抗血小板聚集及抑制乙酰胆碱酯酶活性的有效成分。结果:槟榔子粗提取物能够抑制花生四烯酸、二磷酸腺苷、血小板活化因子、肾上腺素及钙离子载体引起的血小板聚集,尤其对二磷酸腺苷及钙离子载体引起的血小板聚集的抑制最为明显;槟榔子粗提取物能够显著抑制乙酰胆碱酯酶的活性。在所检测的槟榔子所含化合物中,只有儿茶素对肾上腺素引起的血小板聚集有显著的抑制作用,而这种抑制作用显著弱于槟榔子粗提取物,提示槟榔子中的其他成分参与了这种抑制作用;鞣酸、没食子酸、薯蓣皂苷元和异去甲槟榔次碱能够抑制乙酰胆碱酯酶的活性,其中鞣酸的抑制作用强于槟榔子粗提取物。结论:槟榔子中含有抗血小板聚集及抑制乙酰胆碱酯酶活性的有效成分,而发挥这些功效的确切成分有待进一步的研究证实。

Objective：To investigate the possible mechanism and the compound（s）responsible for the antiplatelet and acetylcholinesterase（AChE）inhibitory effects of Areca catechu crude extract（Ac.Cr）.Methods：Aqueous-methanol（70%）was used for extraction of plant material（betel nut）.Antiplatelet activity was measured in human platelet-rich plasma by using a Lumi-aggregometer while anti-AChE activity was measured spectrophotometrically in vitro.In an attempt to find the responsible compound（s）in betel nut for antiplatelet and anti-AChE activities,different commercially available betel nut compounds were tested.Results：Ac.Cr inhibited platelet aggregation induced by arachidonic acid（AA）,adenosine diphosphate（ADP）,platelet-activating factor（PAF）,epinephrine and Ca2＋-ionophore.Ac.Cr was the most potent in inhibiting ADP-and Ca2＋-ionophore-induced aggregation.In the AChE assay,Ac.Cr showed significant AChE inhibitory activity with almost complete inhibition of the enzyme.Out of the tested compounds,none of the compounds in betel nut showed any antiplatelet effect except for catechin that was the most potent against epinephrine-induced aggregation.Catechin was significantly less potent than Ac.Cr,indicating a presence of additional compound（s）with antiplatelet activity.For the AChE inhibitory effect,only tannic acid,gallic acid,diosgenin and isoguvacine were found to be active,whereby tannic acid was more potent than Ac.Cr.Conclusion：This study shows the possible antiplatelet and AChE inhibitory potential of betel nut while further studies are needed to confirm and identify more compounds in betel nut for these actions.