sorbinil and glucogallin

sorbinil has been researched along with glucogallin* in 2 studies

Other Studies

2 other study(ies) available for sorbinil and glucogallin

Article	Year
Aldose reductase inhibition alleviates hyperglycemic effects on human retinal pigment epithelial cells. Chemico-biological interactions, 2015, Jun-05, Volume: 234 Chronic hyperglycemia is an important risk factor involved in the onset and progression of diabetic retinopathy (DR). Among other effectors, aldose reductase (AR) has been linked to the pathogenesis of this degenerative disease. The purpose of this study was to investigate whether the novel AR inhibitor, beta-glucogallin (BGG), can offer protection against various hyperglycemia-induced abnormalities in human adult retinal pigment epithelial (ARPE-19) cells. AR is an enzyme that contributes to cellular stress by production of reactive oxygen species (ROS) under high glucose conditions. A marked decrease in cell viability (from 100% to 78%) following long-term exposure (4 days) of RPE cells to high glucose (HG) was largely prevented by siRNA-mediated knockdown of AR gene expression (from 79% to 97%) or inhibition using sorbinil (from 66% to 86%). In HG, BGG decreased sorbitol accumulation (44%), ROS production (27%) as well as ER stress (22%). Additionally, we demonstrated that BGG prevented loss of mitochondrial membrane potential (MMP) under HG exposure. We also showed that AR inhibitor pretreatment reduced retinal microglia-induced apoptosis in APRE-19 cells. These results suggest that BGG may be useful as a therapeutic agent against retinal degeneration in the diabetic eye by preventing RPE cell death. Topics: Aldehyde Reductase; Apoptosis; Cell Survival; Cells, Cultured; Diabetic Retinopathy; Enzyme Inhibitors; Epithelial Cells; Glucose; Humans; Hydrolyzable Tannins; Hyperglycemia; Imidazolidines; Membrane Potential, Mitochondrial; Microglia; Reactive Oxygen Species; Retinal Pigments	2015
Design of an amide N-glycoside derivative of β-glucogallin: a stable, potent, and specific inhibitor of aldose reductase. Journal of medicinal chemistry, 2014, Jan-09, Volume: 57, Issue:1 β-Glucogallin (BGG), a major component of the Emblica officinalis medicinal plant, is a potent and selective inhibitor of aldose reductase (AKR1B1). New linkages (ether/triazole/amide) were introduced via high yielding, efficient syntheses to replace the labile ester, and an original two-step (90%) preparation of BGG was developed. Inhibition of AKR1B1was assessed in vitro and using transgenic lens organ cultures, which identified the amide linked glucoside (BGA) as a stable, potent, and selective therapeutic lead toward the treatment of diabetic eye disease. Topics: Aldehyde Reductase; Amides; Drug Design; Drug Stability; Enzyme Inhibitors; Glycosides; Humans; Hydrolyzable Tannins	2014

Article

Year

Aldose reductase inhibition alleviates hyperglycemic effects on human retinal pigment epithelial cells.

Chemico-biological interactions, 2015, Jun-05, Volume: 234

Chronic hyperglycemia is an important risk factor involved in the onset and progression of diabetic retinopathy (DR). Among other effectors, aldose reductase (AR) has been linked to the pathogenesis of this degenerative disease. The purpose of this study was to investigate whether the novel AR inhibitor, beta-glucogallin (BGG), can offer protection against various hyperglycemia-induced abnormalities in human adult retinal pigment epithelial (ARPE-19) cells. AR is an enzyme that contributes to cellular stress by production of reactive oxygen species (ROS) under high glucose conditions. A marked decrease in cell viability (from 100% to 78%) following long-term exposure (4 days) of RPE cells to high glucose (HG) was largely prevented by siRNA-mediated knockdown of AR gene expression (from 79% to 97%) or inhibition using sorbinil (from 66% to 86%). In HG, BGG decreased sorbitol accumulation (44%), ROS production (27%) as well as ER stress (22%). Additionally, we demonstrated that BGG prevented loss of mitochondrial membrane potential (MMP) under HG exposure. We also showed that AR inhibitor pretreatment reduced retinal microglia-induced apoptosis in APRE-19 cells. These results suggest that BGG may be useful as a therapeutic agent against retinal degeneration in the diabetic eye by preventing RPE cell death.

Topics: Aldehyde Reductase; Apoptosis; Cell Survival; Cells, Cultured; Diabetic Retinopathy; Enzyme Inhibitors; Epithelial Cells; Glucose; Humans; Hydrolyzable Tannins; Hyperglycemia; Imidazolidines; Membrane Potential, Mitochondrial; Microglia; Reactive Oxygen Species; Retinal Pigments

2015

Design of an amide N-glycoside derivative of β-glucogallin: a stable, potent, and specific inhibitor of aldose reductase.

Journal of medicinal chemistry, 2014, Jan-09, Volume: 57, Issue:1

β-Glucogallin (BGG), a major component of the Emblica officinalis medicinal plant, is a potent and selective inhibitor of aldose reductase (AKR1B1). New linkages (ether/triazole/amide) were introduced via high yielding, efficient syntheses to replace the labile ester, and an original two-step (90%) preparation of BGG was developed. Inhibition of AKR1B1was assessed in vitro and using transgenic lens organ cultures, which identified the amide linked glucoside (BGA) as a stable, potent, and selective therapeutic lead toward the treatment of diabetic eye disease.

Topics: Aldehyde Reductase; Amides; Drug Design; Drug Stability; Enzyme Inhibitors; Glycosides; Humans; Hydrolyzable Tannins

2014