竹叶椒对α-葡萄糖苷酶的抑制作用及机制研究

Study on the Inhibition Against α-glycosidase and Mechanism of Zanthoxylum armature DC.

DOI：10.3969/j.issn.1673-1689.2019.01.009

中文关键词: 竹叶椒 α-糖苷酶 生物碱 非竞争性抑制

英文关键词: Zanthoxylum armatumDC.,α-glucosidase,alkaloid,non-competitive inhibition

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中文摘要:

采用体外抑制模型方法评价竹叶椒生物碱对α-葡萄糖苷酶（酵母菌来源、小鼠小肠来源）抑制作用，并采用Lineweaver-Burk双倒数法分析其抑制α-葡萄糖苷酶活性的机制。结果显示，竹叶椒脂溶性生物碱和水溶性生物碱都对α-葡萄糖苷酶有一定的抑制作用。竹叶椒脂溶性生物碱和水溶性生物碱对酵母来源α-葡萄糖苷酶IC50（半数抑制浓度） 分别为（0.73±0.17） mg/mL、（2.74±0.28） mg/mL；脂溶性生物碱对小鼠小肠来源α-葡萄糖苷酶的IC50为（1.94±0.13） mg/mL。动力学研究表明，竹叶椒生物碱提取物对α-葡萄糖苷酶的抑制作用类型为典型的非竞争性抑制。竹叶椒生物碱对α-葡萄糖苷酶有较好的抑制作用，为进一步的开发利用提供强有力的理论依据。

英文摘要:

Study on the inhibition of alkaloids fromZanthoxylum armatumDC. on α-glucosidase and mechanism. The inhibitory activity of alkaloids fromZanthoxylum armatumagainst α-glucosidase（from yeast and murine small intestine） were evaluated using vitro model，and the mechanism was analyzed using Lineweaver-Burk double-reciprocal analysis. Our results revealed that fat-soluble and dissoluble alkaloids both had significant inhibition on α-glucosidase，IC50 values for α-glucosidase from yeast were （0.73±0.17） mg/mL、（2.74±0.28） mg/mL，respectively. Ones for α-glucosidase from murine small intestine were （1.94±0.13） mg/mL. Moreover，the results of kinetic studies demonstrated inhibitive mechanism of alkaloids is noncompetition inhibition. The results suggested that alkaloids can effectively inhibit the α- glucosidase，and provide strong rationale for further exploitation and utilization.

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