Korea Research Institute of Chemical Technology, Daejeon 305-600, Korea.
J Agric Food Chem. 2010 Sep 22;58(18):9988-93. doi: 10.1021/jf101926j.
In the course of searching for new classes of α-glucosidase inhibitors originated from natural resources, 11 kinds of isoflavones, i.e., medicarpin (1), formononetin (2), mucronulatol (3), (3R)-calussequinone (5), (3R)-5'-methoxyvestitol (6), tectorigenin (7), biochanin A (8), tuberosin (9), calycosin (10), daidzein (11), and genistein (12), as well as a flavone, liquritigenin (4), were isolated as active principles responsible for the yeast α-glucosidase inhibitory activity from two leguminous plant extracts, i.e., the heartwood extract of Dalbergia odorifera and the roots extract of Pueraria thunbergiana. Each components (1-12) demonstrated a significantly potent inhibition on yeast α-glucosidase in a dose dependent manner when the p-nitrophenyl-α-D-glucopyranoside was used as a substrate in vitro. The concentration required for 50% enzyme inhibition (IC50) were calculated as 2.93 mM (1), 0.51 mM (2), 3.52 mM (7) 0.35 mM (8), 3.52 mM (9), 0.85 mM (11), and 0.15 mM (12) when that of reference drug acarbose was evaluated as 9.11 mM, in vitro. However, isoflavone glycosides, i.e., puerarin (13), daidzin (14), formononetin-7-O-β-glucopyranoside (15), and genistin (16), exhibited a relatively poor inhibitory activity on yeast α-glucosidase as compared with the corresponding isoflavone (2, 11, 12), respectively.
在从天然资源中寻找新的 α-葡萄糖苷酶抑制剂的过程中，从两种豆科植物提取物（即降香的心材提取物和野葛的根提取物）中分离出 11 种异黄酮，即芒柄花素（1）、芒柄花苷（2）、毛蕊异黄酮（3）、（3R）-卡鲁塞醌（5）、（3R）-5'-甲氧基维斯托醇（6）、染料木黄酮（7）、大豆黄素（8）、金雀异黄素（9）、大豆苷元（10）、染料木苷元（11）和染料木黄酮（12），以及一种黄酮，甘草素（4），作为负责酵母 α-葡萄糖苷酶抑制活性的活性成分。当使用对硝基苯-α-D-吡喃葡萄糖苷作为体外底物时，每个成分（1-12）均表现出对酵母 α-葡萄糖苷酶的显著抑制作用，呈剂量依赖性。计算出的 50%酶抑制所需浓度（IC50）分别为 2.93 mM（1）、0.51 mM（2）、3.52 mM（7）、0.35 mM（8）、3.52 mM（9）、0.85 mM（11）和 0.15 mM（12），而参考药物阿卡波糖的 IC50 为 9.11 mM。然而，与相应的异黄酮（2、11、12）相比，异黄酮糖苷，即葛根素（13）、大豆苷元（14）、芒柄花苷-7-O-β-吡喃葡萄糖苷（15）和染料木苷元（16）对酵母 α-葡萄糖苷酶的抑制活性相对较差。
