title: Inhibitory effects of polyphenols isolated from Rhus verniciflua on Aldo-keto reductase family 1 B10.
abstract: Aldo-keto reductase family 1 B10 (AKR1B10) is a member of the NADPH-dependent aldo-keto reductase (AKR) superfamily, and has been considered to be a potential cancer therapeutic target. Total extract from the bark of Rhus verniciflua (Toxicodendron vernicifluum (Stokes)) showed AKR1B10 inhibitory activity. To identify the active compounds from R. verniciflua responsible for AKR1B10 inhibition, nine compounds were isolated via bioactivity-guided isolation and tested for their effects against recombinant human AKR1B10 (rhAKR1B10). Results showed that butein, isolated from the ethyl acetate fraction, was most able to inhibit rhAKR1B10. The inhibitory rate of butein against rhAKR1B10 was 42.86% at 1 microM with an IC(50) value of 1.47 microM, and enzyme kinetic analysis revealed its inhibition mode to be uncompetitive.
authors.affiliation: Natural Products Research Center, Korea Institute of Science and Technology Gangneung Institute, Gangneung 210-340, Korea.
authors.forename: Dae-Geun
authors.initials: DG
authors.lastname: Song
authors.forename: Joo Young
authors.initials: JY
authors.lastname: Lee
authors.forename: Eun Ha
authors.initials: EH
authors.lastname: Lee
authors.forename: Sang Hoon
authors.initials: SH
authors.lastname: Jung
authors.forename: Chu Won
authors.initials: CW
authors.lastname: Nho
authors.forename: Kwang Hyun
authors.initials: KH
authors.lastname: Cha
authors.forename: Song Yi
authors.initials: SY
authors.lastname: Koo
authors.forename: Cheol-Ho
authors.initials: CH
authors.lastname: Pan
mesh_terms: D000449:Aldehyde Reductase / Q000037:antagonists & inhibitors* / Q000235:genetics / Q000378:metabolism; D000074408:Aldo-Keto Reductases; D047188:Chalcones / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D005419:Flavonoids / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D006801:Humans; D007700:Kinetics; D010636:Phenols / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D024301:Plant Bark / Q000737:chemistry; D059808:Polyphenols; D011994:Recombinant Proteins / Q000037:antagonists & inhibitors / Q000235:genetics / Q000378:metabolism; D029045:Rhus / Q000737:chemistry*
chemical_list: D047188:Chalcones; D005419:Flavonoids; D010636:Phenols; D059808:Polyphenols; D011994:Recombinant Proteins; C040918:butein; C120471:AKR1B10 protein, human; D000074408:Aldo-Keto Reductases; D000449:Aldehyde Reductase