title: Pterocarpans with inhibitory effects on protein tyrosine phosphatase 1B from Erythrina lysistemon Hutch.
abstract: Bioassay-guided fractionation of the MeOH extract of the stem bark of Erythrina lysistemon Hutch. resulted in isolation of pterocarpans (1-3), named erylysins A-C, along with nine known pterocarpans (4-12). Their structures were determined to be 3''-hydroxy-2',2'-dimethylpyrano[6',5':3,4]-2'',2''-dimethyldihydropyrano[6'',5'':9,10]pterocarpan (1), furano[5',4':3,4]-9-hydroxy-10-prenylpterocarpan (2), and 8-formyl-3,9-dihydroxy-4,10-diprenylpterocarpan (3), based on spectroscopic analyses. All the isolates, with the exception of 3, 6, and 11, strongly inhibited protein tyrosine phosphatase 1B (PTP1B) activity in an in vitro assay, with IC(50) values ranging from 1.01+/-0.3 to 18.1+/-0.9 microg/mL. This is the first report showing the potential of prenylated pterocarpans as a class of natural PTP1B inhibitors.
authors.affiliation: College of Pharmacy, Chosun University, 375 Seosuk-dong, Gwangju 501-759, Republic of Korea.
authors.forename: Trong Tuan
authors.initials: TT
authors.lastname: Dao
authors.forename: Phi Hung
authors.initials: PH
authors.lastname: Nguyen
authors.forename: Phuong Thien
authors.initials: PT
authors.lastname: Thuong
authors.forename: Keon Wook
authors.initials: KW
authors.lastname: Kang
authors.forename: MinKyun
authors.initials: M
authors.lastname: Na
authors.forename: Derek Tantoh
authors.initials: DT
authors.lastname: Ndinteh
authors.forename: Joseph Tanyi
authors.initials: JT
authors.lastname: Mbafor
authors.forename: Won Keun
authors.initials: WK
authors.lastname: Oh
mesh_terms: D004791:Enzyme Inhibitors / Q000302:isolation & purification / Q000378:metabolism / Q000494:pharmacology*; D004895:Erythrina / Q000737:chemistry*; D024301:Plant Bark; D010936:Plant Extracts / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D018547:Plant Stems; D054876:Prenylation; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1 / Q000037:antagonists & inhibitors*; D036343:Pterocarpans / Q000302:isolation & purification / Q000378:metabolism / Q000494:pharmacology*
chemical_list: D004791:Enzyme Inhibitors; D010936:Plant Extracts; D036343:Pterocarpans; C548520:erylysin A; C548521:erylysin B; C548522:erylysin C; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1