Inhibitory effect of 2-arylbenzofurans from Erythrina addisoniae on protein tyrosine phosphatase-1B.
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.
Na
Minkyun
M
Korea Research Institute of Bioscience and Biotechnology, 52 Eoun-dong, Yuseong-gu, Daejeon 305-333, Republic of Korea.
Hoang
Duc Manh
DM
Njamen
Dieudonné
D
Mbafor
Joseph Tanyi
JT
Fomum
Zacharias Tanee
ZT
Thuong
Phuong Thien
PT
Ahn
Jong Seog
JS
Oh
Won Keun
WK
D001572:Benzofurans / Q000302:isolation & purification / Q000494:pharmacology*; D004895:Erythrina / Q000201:enzymology*; D053824:Protein Tyrosine Phosphatase, Non-Receptor Type 6 / Q000037:antagonists & inhibitors*; D013057:Spectrum Analysis / Q000379:methods
D001572:Benzofurans; C509249:PTPN6 protein, human; D053824:Protein Tyrosine Phosphatase, Non-Receptor Type 6