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Literature summary for 1.1.1.21 extracted from

  • Kato, A.; Higuchi, Y.; Goto, H.; Kizu, H.; Okamoto, T.; Asano, N.; Hollinshead, J.; Nash, R.J.; Adachi, I.
    Inhibitory effects of Zingiber officinale Roscoe derived components on aldose reductase activity in vitro and in vivo (2006), J. Agric. Food Chem., 54, 6640-6644.
    View publication on PubMed
Search for more literature for 1.1.1.21

Application

Application Comment Organism
drug development the enzyme is a target for inhibitor design, enzyme inhibition has considerable potential for the treatment of diabetes, without increased risk of hypoglycemia Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(4-hydroxy-3-methoxyphenyl)acetonitrile IC50: 0.0244 mM Homo sapiens
(4-hydroxy-3-methoxyphenyl)methamine IC50: 0.0634 mM Homo sapiens
2-(3,4-dimethoxyphenyl)-ethanoic acid IC50: 0.0303 mM Homo sapiens
2-(4-hydroxy-3-methoxyphenyl)ethanoic acid derived from ginger rhizom, Zingiber officinale, IC50: 0.0185 mM, suppresses nt only sorbitol accumulation in human erythrocytes Homo sapiens
2-(4-hydroxy-3-methoxyphenyl)ethanol derived from ginger rhizom, Zingiber officinale, IC50: 0.0192 mM, suppresses sorbitol accumulation in human erythrocytes Homo sapiens
3-(4-hydroxy-3-methoxyphenyl)propanol IC50: 0.283 mM Homo sapiens
4-(4-hydroxy-3-methoxyphenyl)-2-butanone IC50: 0.197 mM Homo sapiens
4-(4-hydroxy-3-methoxyphenyl)butanol IC50: 0.642 mM Homo sapiens
4-hydroxy-3-methoxyphenol IC50: 0.273 mM Homo sapiens
4-hydroxy-3-methoxyphenyl methanol IC50: 0.0244 mM Homo sapiens
additional information aldose reductase inhibitors have considerable potential for the treatment of diabetes, without increased risk of hypoglycemia, structure-activity relationship study, the applicable side alkyl chain length and the presence of a OCH3 group at C3 in the aromatic ring are essential features for enzyme recognition and binding, no or poor inhibition by gingerol, shogaol, 2-(4-hydroxy-3-nitrophenyl)ethanoic acid, 2-(3,4-dihydroxyphenyl)ethanoic acid, and 2-(4-hydroxyphenyl)ethanoic acid Homo sapiens
quercetin IC50: 0.027 mM Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
commercial preparation recombinant enzyme Homo sapiens
-
erythrocyte
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
DL-glyceraldehyde + NADPH + H+
-
 Homo sapiens glycerol + NADP+
-
 ?

Synonyms

Synonyms Comment Organism
aldose reductase
-
 Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
 assay at Homo sapiens

Cofactor

Cofactor Comment Organism Structure
NADPH
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0185
-
 derived from ginger rhizom, Zingiber officinale, IC50: 0.0185 mM, suppresses nt only sorbitol accumulation in human erythrocytes Homo sapiens 2-(4-hydroxy-3-methoxyphenyl)ethanoic acid
0.0192
-
 derived from ginger rhizom, Zingiber officinale, IC50: 0.0192 mM, suppresses sorbitol accumulation in human erythrocytes Homo sapiens 2-(4-hydroxy-3-methoxyphenyl)ethanol
0.0244
-
 IC50: 0.0244 mM Homo sapiens 4-hydroxy-3-methoxyphenyl methanol
0.0244
-
 IC50: 0.0244 mM Homo sapiens (4-hydroxy-3-methoxyphenyl)acetonitrile
0.027
-
 IC50: 0.027 mM Homo sapiens quercetin
0.0303
-
 IC50: 0.0303 mM Homo sapiens 2-(3,4-dimethoxyphenyl)-ethanoic acid
0.0634
-
 IC50: 0.0634 mM Homo sapiens (4-hydroxy-3-methoxyphenyl)methamine
0.197
-
 IC50: 0.197 mM Homo sapiens 4-(4-hydroxy-3-methoxyphenyl)-2-butanone
0.273
-
 IC50: 0.273 mM Homo sapiens 4-hydroxy-3-methoxyphenol
0.283
-
 IC50: 0.283 mM Homo sapiens 3-(4-hydroxy-3-methoxyphenyl)propanol
0.642
-
 IC50: 0.642 mM Homo sapiens 4-(4-hydroxy-3-methoxyphenyl)butanol