scholarly journals Carboxymethylated tetrahydropyridoindoles as aldose reductase inhibitors: in vitro selectivity study in intact rat erythrocytes in relation to glycolytic pathway

2009 ◽  
Vol 28 (4) ◽  
pp. 325-330 ◽  
Author(s):  
M. Juskova ◽  
V. Snirc ◽  
A. Gajdosikova ◽  
A. Gajdosik ◽  
L. Krizanova ◽  
...  
Keyword(s):  
Aldose Reductase ◽  
Glycolytic Pathway ◽  
Rat Erythrocytes ◽  
Aldose Reductase Inhibitors ◽  
Reductase Inhibitors

scholarly journals Development of Novel Indole-Based Bifunctional Aldose Reductase Inhibitors/Antioxidants as Promising Drugs for the Treatment of Diabetic Complications

Molecules ◽  
2021 ◽  
Vol 26 (10) ◽  
pp. 2867
Author(s):  
Lucia Kovacikova ◽  
Marta Soltesova Prnova ◽  
Magdalena Majekova ◽  
Andrej Bohac ◽  
Cimen Karasu ◽  
...  
Keyword(s):  
Aldose Reductase ◽  
Diabetic Complications ◽  
Therapeutic Potential ◽  
Ex Vivo ◽  
Biological Activities ◽  
In Vivo Models ◽  
Aldose Reductase Inhibitors ◽  
Reductase Inhibitors ◽  
Promising Therapeutic Approach

Aldose reductase (AR, ALR2), the first enzyme of the polyol pathway, is implicated in the pathophysiology of diabetic complications. Aldose reductase inhibitors (ARIs) thus present a promising therapeutic approach to treat a wide array of diabetic complications. Moreover, a therapeutic potential of ARIs in the treatment of chronic inflammation-related pathologies and several genetic metabolic disorders has been recently indicated. Substituted indoles are an interesting group of compounds with a plethora of biological activities. This article reviews a series of indole-based bifunctional aldose reductase inhibitors/antioxidants (ARIs/AOs) developed during recent years. Experimental results obtained in in vitro, ex vivo, and in vivo models of diabetic complications are presented. Structure–activity relationships with respect to carboxymethyl pharmacophore regioisomerization and core scaffold modification are discussed along with the criteria of ‘drug-likeness”. Novel promising structures of putative multifunctional ARIs/AOs are designed.

Spirohydantoin derivatives of thiopyrano[2,3-b]pyridin-4(4H)-one as potent in vitro and in vivo aldose reductase inhibitors

2005 ◽  
Vol 13 (2) ◽  
pp. 491-499 ◽  
Author(s):  
Federico Da Settimo ◽  
Giampaolo Primofiore ◽  
Concettina La Motta ◽  
Silvia Salerno ◽  
Ettore Novellino ◽  
...  
Keyword(s):  
Aldose Reductase ◽  
Aldose Reductase Inhibitors ◽  
Reductase Inhibitors ◽  
Derivatives Of

In-vitro Studies on α-Amylase, α-Glucosidase and Aldose Reductase Inhibitors found in Endophytic Fungi Isolated from Ocimum sanctum

2015 ◽  
Vol 10 (2) ◽  
pp. 129-136
Author(s):  
Pavithra N. ◽  
Sathish L. ◽  
Suneel Kumar A. ◽  
Venkatarathanamma V. ◽  
Pushpalatha H. ◽  
...  
Keyword(s):  
Aldose Reductase ◽  
Endophytic Fungi ◽  
In Vitro Studies ◽  
Ocimum Sanctum ◽  
Aldose Reductase Inhibitors ◽  
Reductase Inhibitors

Permeability characteristics of novel aldose reductase inhibitors using rat jejunum in vitro

2006 ◽  
Vol 28 (1-2) ◽  
pp. 128-133 ◽  
Author(s):  
Katja Šturm ◽  
Lea Levstik ◽  
Vassilis J. Demopoulos ◽  
Albin Kristl
Keyword(s):  
Aldose Reductase ◽  
Rat Jejunum ◽  
Permeability Characteristics ◽  
Aldose Reductase Inhibitors ◽  
Reductase Inhibitors

scholarly journals In Vitro and Insilico screening platform for the identification of aldose reductase inhibitors for antidiabetic lead compounds from Abutilon indicum (L.)

2020 ◽  
Author(s):  
L Lavanya ◽  
V. Veeraraghavan ◽  
CN Prashantha ◽  
Renuka Srihari
Keyword(s):  
Aldose Reductase ◽  
Developed Countries ◽  
Docking Studies ◽  
Binding Interaction ◽  
Reference Drug ◽  
Rat Lens Aldose Reductase ◽  
Aldose Reductase Inhibitors ◽  
Reductase Inhibitors ◽  
Abutilon Indicum

AbstractIntroductionType 2 Diabetes Mellitus (T2DM) is a long-term metabolic disorder that primarily characterized by impaired insulin resistance to become hyperglycemia. People suffering from T2DM have a higher risk of developing various diseases but, on top of that, some diabetic drugs are also suspected of increasing the risk in some cases. Aldose reductase is a key target enzyme to catalyze the reduction of glucose to sorbitol and does not readily diffuse across cell membranes and cause retinopathy and neuropathy. The aldolase reductase inhibitors prevent the conversion of glucose to sorbitol and may have the capacity of preventing and / or treating several diabetic complications. It will be expected to be twofold in the subsequent decade due to intensification in the senile population with the number of people affected, thus adding to the liability on medical providers in poor developed countries using herbal medicine to control the diabetes. In recent investigation, the antidiabetic property of phytochemicals extracted from leafs of Abutilon indicum (L.) is elucidated using animal models.Materials and MethodsIn the current study using aldose reductase enzyme assay inhibitor of Rat lens Aldose reductase were treated with A. indicum methanolic leaf extract at different concentrations (6.25, 12.5, 25, 50, 100, and 200μg/mL). Copper sulphate was used as reference drug and docking studies to predict the screen the best aldose reductase inhibitor.Results and DiscussionThe crude extract exhibited cytotoxicity against rat lens aldose reductase (IC50 = 135.8 μg/L vs ref 13.60 μg/L) using In Vitro. The docking is performed with 11 compounds shows Ertugliflozin, 9H-Cycloisolongifolene, 8-oxo and 7-hydroxy cadalene showed a good binding interaction with aldose reductase.ConclusionWe are concluding that the invitro and in silico analysis helps researchers to utilize these compound for aldose reductase inhibitors and further can be used for clinical applications.

In vitro evaluation of 5-arylidene-2-thioxo-4-thiazolidinones active as aldose reductase inhibitors

2011 ◽  
Vol 21 (1) ◽  
pp. 200-203 ◽  
Author(s):  
Rosanna Maccari ◽  
Antonella Del Corso ◽  
Marco Giglio ◽  
Roberta Moschini ◽  
Umberto Mura ◽  
...  
Keyword(s):  
Aldose Reductase ◽  
In Vitro Evaluation ◽  
Aldose Reductase Inhibitors ◽  
Reductase Inhibitors

ChemInform Abstract: Synthesis of Pyrrolo(3,4-c)pyridine Derivatives Possessing an Acid Group and Their in vitro and in vivo Evaluation as Aldose Reductase Inhibitors.

ChemInform ◽  
2010 ◽  
Vol 27 (23) ◽  
pp. no-no
Author(s):  
A. DA SETTIMO ◽  
G. PRIMOFIORE ◽  
F. DA SETTIMO ◽  
F. SIMORINI ◽  
C. LA MOTTA ◽  
...  
Keyword(s):  
Aldose Reductase ◽  
Acid Group ◽  
Pyridine Derivatives ◽  
In Vivo Evaluation ◽  
Aldose Reductase Inhibitors ◽  
Reductase Inhibitors
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