In vitro aldose reductase inhibitory activity of 5-benzyl-2,4-thiazolidinediones

2006 ◽  
Vol 14 (2) ◽  
pp. 567-574 ◽  
Author(s):  
Dietmar Rakowitz ◽  
Rosanna Maccari ◽  
Rosaria Ottanà ◽  
Maria Gabriella Vigorita
Author(s):  
Kushagra Dubey ◽  
Raghvendra Dubey ◽  
Revathi Gupta ◽  
Arun Gupta

Background: Diosmin is a flavonoid obtained from the citrus fruits of the plants. Diosmin has blood lipid lowering activities, antioxidant activity, enhances venous tone and microcirculation, protects capillaries, mainly by reducing systemic oxidative stress. Objective: The present study demonstrates the potential of Diosmin against the enzymes aldose reductase, α-glucosidase, and α-amylase involved in diabetes and its complications by in vitro evaluation and reverse molecular docking studies. Method: The assay of aldose reductase was performed by using NADPH as starting material and DL-Glyceraldehyde as a substrate. DNS method was used for alpha amylase inhibition and in alpha glucosidase inhibitory activity p-nitrophenyl glucopyranoside (pNPG) was used as substrate. The reverse molecular docking studies was performed by using Molegro software (MVD) with grid resolution of 30 Å. Result: Diosmin shows potent inhibitory effect against aldose reductase (IC50:333.88±0.04 µg/mL), α-glucosidase (IC50:410.3±0.01 µg/mL) and α-amylase (IC50: 404.22±0.02 µg/mL) respectively. The standard drugs shows moderate inhibitory activity for enzymes. The MolDock Score of Diosmin was -224.127 against aldose reductase, -168.17 against α-glucosidase and -176.013 against α-amylase respectively, which was much higher than standard drugs. Conclusion: From the result it was concluded that diosmin was a potentially inhibitor of aldose reductase, alpha amylase and alpha glucosidase enzymes then the standard drugs and it will be helpful in the management of diabetes and its complications. This will also be benevolent to decrease the socio economical burden on the middle class family of the society.


Author(s):  
Anasuri Santhosh ◽  
C. Veeresham ◽  
A. Rama Rao

Objective: The objectives were to study the in-vitro and in-vivo aldose reductase and in-vitro advanced glycation end products formation inhibitory activities of the standardized extracts of Picrorhiza kurroa roots and Hibiscus rosa-sinensis flowers.Methods: In-vitro Aldose reductase inhibitory activity was studied by using isolated rat lens and kidney Aldose reductase by UV-Visible spectro photo metric method by using Quercetin as reference compound. In-vivo Aldose reductase inhibitory activity was evaluated by using experimental rat models of galactosemia and the final lens galactitol was evaluated by High performance liquid chromatography and Gas chromatography methods by using Quercetin as reference compound. In-vitro advanced glycation end products formation inhibitory activity was estimated by using laboratory test reaction with protein and sugars by spectro fluorimetric method by sung aminoguanidine as reference compound. Statistical analysis of the results was done by using Analysis of the variance method.Results: The plant extracts were found to possess significant aldose reductase and advanced glycation end products formation inhibitory activity.Conclusions: More study is required for isolation and characterization of the chief chemical constituents responsible for the biological activity of the plant extracts.


Planta Medica ◽  
2008 ◽  
Vol 74 (09) ◽  
Author(s):  
D Lazari ◽  
C Tsioumela ◽  
K Pegklidou ◽  
A Karioti ◽  
V Demopoulos ◽  
...  

1989 ◽  
Vol 32 (5) ◽  
pp. 1033-1038 ◽  
Author(s):  
Jack DeRuiter ◽  
Blake E. Swearingen ◽  
Vinay Wandrekar ◽  
Charles A. Mayfield

Phytomedicine ◽  
2015 ◽  
Vol 22 (1) ◽  
pp. 49-51 ◽  
Author(s):  
Sri Fatmawati ◽  
Taslim Ersam ◽  
Kuniyoshi Shimizu

Author(s):  
Singaravelu Anand ◽  
Munichetty Arasakumari ◽  
Panneervelu Prabu ◽  
Arul Joseph Amalraj

<p><strong>Objective: </strong>The objective of the present study was to determine the cellular level effect on glucose uptake and aldose reductase inhibitory activity of different extracts of traditional medicinal plant <em>Psidium guajava</em>.</p><p><strong>Methods: </strong><em>Psidium guajava</em> was selected and subjected for successive extraction from non-polar to polar solvents and subjected to glucose uptake and aldose reductase inhibition assay.</p><p><strong>Results: </strong>Based on the results <em>Psidium guajava</em><em> </em>methanolic extract (PGME) showed an enhancement in the glucose uptake and also up-regulates the gene and protein level expression of IRβ, IRS-1, PI3K and GLUT4. Wortmannin, a specific PI3K inhibitor confirms that the active PGME recruits glucose uptake through a PI3K dependent pathway. In the assay of aldose reductase inhibitory activity, the results suggested that PGME possesses a significant inhibitory effect.</p><p><strong>Conclusion: </strong>The result obtained in the present study focuses on the anti-diabetic effect of PGME by studying cellular level glucose uptake in L6 myotubes and aldose reductase inhibitory activity.<strong></strong></p>


2008 ◽  
Vol 16 (11) ◽  
pp. 5840-5852 ◽  
Author(s):  
Rosanna Maccari ◽  
Rosaria Ottanà ◽  
Rosella Ciurleo ◽  
Dietmar Rakowitz ◽  
Barbara Matuszczak ◽  
...  

2008 ◽  
Vol 23 (3) ◽  
pp. 297-301 ◽  
Author(s):  
Net Daş-Evcimen ◽  
Oya Bozdağ-Dündar ◽  
Mutlu Sarikaya ◽  
Rahmiye Ertan

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