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