EFFECTS OF 1-(3-BROMOBENZOFURAN-2-YLSULFONYL)HYDANTOIN ON HUMAN ALDOSE REDUCTASE EXAMINED BY A NEW APPLICATION OF HPLC SYSTEM FOR MEASURINGTISSUE POLYOL

Citation
N. Murakami et al., EFFECTS OF 1-(3-BROMOBENZOFURAN-2-YLSULFONYL)HYDANTOIN ON HUMAN ALDOSE REDUCTASE EXAMINED BY A NEW APPLICATION OF HPLC SYSTEM FOR MEASURINGTISSUE POLYOL, Arzneimittel-Forschung, 47(11), 1997, pp. 1222-1225
Citations number
13
Journal title
ISSN journal
00044172
Volume
47
Issue
11
Year of publication
1997
Pages
1222 - 1225
Database
ISI
SICI code
0004-4172(1997)47:11<1222:EO1OHA>2.0.ZU;2-B
Abstract
M16209 (1-(3-bromobenzofuran-2-ylsulfonyl)hydantoin CAS 128851-36-5) d isplayed potent inhibitory effects upon recombinant human aldose reduc tase (rhAR, IC50 = 0.051 mu mol/l). The inhibition of rhAR by M16209 w as uncompetitive with respect to both glyceraldehyde and NADPH. The ef fects of M16209 on human AR were investigated using a new application of HPLC system developed for analysis of tissue polyol. M16209 and epa lrestat suppressed galactitol accumulation in human erythrocytes cultu red in 25 mmol/l galactose with IC50 values of 1.2 and 2.6 mu mol/l, r espectively. The new application of HPLC system equipped with an elect rochemical detector did not require any derivatization procedure for p olyols and enabled simultaneous determination of glucose, galactose, f ructose, myo-inositol, galactitol and sorbitol.