滇丁香中抑制α-葡萄糖苷酶活性成分研究
投稿时间:1900-01-01  修订日期:1900-01-01  责任编辑:  点此下载全文
引用本文:康文艺1,2*,张 丽1,2,宋艳丽1,2.滇丁香中抑制α-葡萄糖苷酶活性成分研究[J].中国中药杂志,2009,34(04):406.
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康文艺1  2*  张 丽1  2  宋艳丽1  2
1. 河南大学 天然药物研究所,河南 开封 475004;2. 河南大学 药学院,河南 开封 475004
中文摘要:目的:寻找滇丁香中具有抑制α-葡萄糖苷酶活性的成分。方法:利用体外抑制α-葡萄糖苷酶活性模型进行追踪,采用各种色谱法分离,运用多种谱学技术鉴定结构,并对活性较强的几个单体化合物进行酶抑制动力学研究。结果:滇丁香的醋酸乙酯部分具有较高的活性,从中分离出5个抑制α-葡萄糖苷酶活性的化合物,分别鉴定为:莨菪内酯(1),5-甲氧基-8-羟基香豆素(2),1α,3β,24-三羟基熊果酸(3),熊果酸(4)和齐墩果酸(5),其中化合物4(IC50 3.3 mg•L-1),5(IC50 2.88 mg•L-1)的活性最好,明显高于阳性对照阿卡波糖(IC50 1 081.27 mg•L-1)。化合物3为竞争性抑制。结论:化合物1~4为首次报道对α-葡萄糖苷酶有抑制活性。
中文关键词:滇丁香,α-葡萄糖苷酶,抑制剂
 
α-Glucosidase inhibitors from Luculia pinciana
KANG Wenyi 1  2*  ZHANG Li1  2  SONG Yanli 1  2
1. Institute of Natural Products, Henan University, Kaifeng 475004, China
2. Pharmaceutical College of Henan University, Kaifeng 475004, China
Abstract:Objective:To search α-glucosidase inhibitors from Luculia pinciana. Method: The α-glucosidase inhibitor was isolated by the column chromatographic techniques and the bioassay-guided method in vitro. A combination of MS and NMR spectroscopy was used to identify the chemical structures. The inhibitory kinetic of the isolations was also investigated. Result: The ethyl acetate extract showed strongest inhibitory activity, and five active compounds were isolated and identified as scopletin (1), 5-methoxy-8-hydroxycoumarin (2), 1α,3β,24-trihydroxyursolic acid (3), ursolic acid (4) and oleanolic acid (5). The IC50 values of all compounds were lower than that of acarbose. Four of them shown noncompetitive type manner on α-glucosidase inhibition except that compound 3 is competitive type manner. Conclusion: Compounds 1-4 as the inhibitors of α-glucosidase were reported for the first time.
keywords:Luculia pinciana  α-glucosidase  inhibitors  inhibitory type
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