来自阿迪森刺桐的2-芳基苯并呋喃对蛋白酪氨酸磷酸酶-1B的抑制作用。
Inhibitory effect of 2-arylbenzofurans from Erythrina addisoniae on protein tyrosine phosphatase-1B.
作者信息
Na Minkyun, Hoang Duc Manh, Njamen Dieudonné, Mbafor Joseph Tanyi, Fomum Zacharias Tanee, Thuong Phuong Thien, Ahn Jong Seog, Oh Won Keun
机构信息
Korea Research Institute of Bioscience and Biotechnology, 52 Eoun-dong, Yuseong-gu, Daejeon 305-333, Republic of Korea.
出版信息
Bioorg Med Chem Lett. 2007 Jul 15;17(14):3868-71. doi: 10.1016/j.bmcl.2007.05.005. Epub 2007 May 6.
Bioassay-guided fractionation of an EtOAc-soluble extract of the stem bark of Erythrina addisoniae (Leguminosae), using an in vitro PTP1B inhibitory assay, resulted in the isolation of three new (1-3) and three known (4-6) 2-arylbenzofuran derivatives. The new compounds were identified as 2-[2',4'-dihydroxy-3'-(3-methylbut-2-enyl)phenyl]-6-hydroxybenzofuran (1), 2-[2'-methoxy-4'-hydroxy-5'-(3-methylbut-2-enyl)phenyl]-6-hydroxybenzofuran (2), and 2-(2'-methoxy-4'-hydroxyphenyl)-5-(3-methylbut-2-enyl)-6-hydroxybenzofuran (3). The new 2-arylbenzofurans 1-3 inhibited PTP1B activity with IC(50) values ranging from 13.6+/-1.1 to 17.5+/-1.2 microM in vitro assay. On the basis of the data obtained, 2-arylbenzofurans with prenyl group may be considered as a new class of PTP1B inhibitors.
采用体外蛋白酪氨酸磷酸酶1B（PTP1B）抑制试验，对刺桐属植物艾氏刺桐（豆科）茎皮的乙酸乙酯可溶提取物进行生物活性导向的分离，得到了三种新的（1 - 3）和三种已知的（4 - 6）2 - 芳基苯并呋喃衍生物。新化合物被鉴定为2 - [2',4' - 二羟基 - 3' - (3 - 甲基丁 - 2 - 烯基)苯基] - 6 - 羟基苯并呋喃（1）、2 - [2' - 甲氧基 - 4' - 羟基 - 5' - (3 - 甲基丁 - 2 - 烯基)苯基] - 6 - 羟基苯并呋喃（2）和2 - (2' - 甲氧基 - 4' - 羟基苯基) - 5 - (3 - 甲基丁 - 2 - 烯基) - 6 - 羟基苯并呋喃（3）。在体外试验中，新的2 - 芳基苯并呋喃1 - 3抑制PTP1B活性的IC(50)值范围为13.6±1.1至17.5±1.2微摩尔。基于所获得的数据，带有异戊烯基的2 - 芳基苯并呋喃可被视为一类新的PTP1B抑制剂。
Zotero 插件