Aldose reductase inhibitors from the leaves of Myrciaria dubia (H. B. & K.) McVaugh.
Ellagic acid (1) and its two derivatives, 4-O-methylellagic acid (2) and 4-(alpha-rhamnopyranosyl)ellagic acid (3) were isolated as inhibitors of aldose reductase (AR) from Myrciaria dubia (H. B. & K.) McVaugh. Compound 2 was the first isolated from the nature. Compound 3 showed the strongest inhibition against human recombinant AR (HRAR) and rat lens AR (RLAR). Inhibitory activity of compound 3 against HRAR (IC50 value = 4.1 x 10(-8) M) was 60 times more than that of quercetin (2.5 x 10(-6) M). The type of inhibition against HRAR was uncompetitive.
Ueda
H
H
Kobe Pharmaceutical University, Higashinada-ku, Kobe, 658-8558 Japan.
Kuroiwa
E
E
Tachibana
Y
Y
Kawanishi
K
K
Ayala
F
F
Moriyasu
M
M
D000449:Aldehyde Reductase / Q000037:antagonists & inhibitors*; D000818:Animals; D004610:Ellagic Acid / Q000031:analogs & derivatives* / Q000302:isolation & purification / Q000494:pharmacology; D006801:Humans; D007908:Lens, Crystalline / Q000201:enzymology; D008297:Male; D015394:Molecular Structure; D009005:Monosaccharides / Q000302:isolation & purification / Q000494:pharmacology; D027822:Myrtaceae / Q000737:chemistry*; D018515:Plant Leaves / Q000737:chemistry; D051381:Rats; D017208:Rats, Wistar; D011994:Recombinant Proteins
C496302:4-(alpha-rhamnopyranosyl)ellagic acid; C496301:4-O-methylellagic acid; D009005:Monosaccharides; D011994:Recombinant Proteins; D004610:Ellagic Acid; D000449:Aldehyde Reductase