从甘草（乌拉尔甘草根）中获得的具有过氧化物酶体增殖物激活受体γ（PPAR-γ）配体结合活性的酚类物质以及甘草甜素对遗传性糖尿病KK-A(y)小鼠的改善作用。
Phenolics with PPAR-gamma ligand-binding activity obtained from licorice (Glycyrrhiza uralensis roots) and ameliorative effects of glycyrin on genetically diabetic KK-A(y) mice.
作者信息
Kuroda Minpei, Mimaki Yoshihiro, Sashida Yutaka, Mae Tatsumasa, Kishida Hideyuki, Nishiyama Tozo, Tsukagawa Misuzu, Konishi Eisaku, Takahashi Kazuma, Kawada Teruo, Nakagawa Kaku, Kitahara Mikio
机构信息
Laboratory of Medicinal Plant Science, School of Pharmacy, Tokyo University of Pharmacy and Life Science, Hachioji, Tokyo 192-0392, Japan.
出版信息
Bioorg Med Chem Lett. 2003 Dec 15;13(24):4267-72. doi: 10.1016/j.bmcl.2003.09.052.
The EtOAc extract of licorice (Glycyrrhiza uralensis roots) exhibited considerable PPAR-gamma ligand-binding activity. Bioassay-guided fractionation of the extract using a GAL-4-PPAR-gamma chimera assay method resulted in the isolation of two isoflavenes, one of which is a new compound named dehydroglyasperin D, an isoflavan, two 3-arylcoumarins, and an isoflavanone as the PPAR-gamma ligand-binding active ingredients of licorice. The isoprenyl group at C-6 and the C-2' hydroxyl group in the aromatic ring-C part in the isoflavan, isoflavene, or arylcoumarin skeleton were found to be the structural requirements for PPAR-gamma ligand-binding activity. Glycyrin, one of the main PPAR-gamma ligands of licorice, significantly decreased the blood glucose levels of genetically diabetic KK-A(y) mice.
甘草（乌拉尔甘草根）的乙酸乙酯提取物表现出相当可观的过氧化物酶体增殖物激活受体γ（PPAR-γ）配体结合活性。使用GAL-4-PPAR-γ嵌合体检测方法对该提取物进行生物测定导向的分级分离，得到了两种异黄酮，其中一种是名为脱氢甘草asperin D的新化合物，一种异黄烷，两种3-芳基香豆素，以及一种异黄酮作为甘草的PPAR-γ配体结合活性成分。发现异黄酮、异黄烷或芳基香豆素骨架中C-6位的异戊烯基和芳环-C部分的C-2'羟基是PPAR-γ配体结合活性的结构要求。甘草素是甘草的主要PPAR-γ配体之一，可显著降低遗传性糖尿病KK-A(y)小鼠的血糖水平。
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