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[5-(Benzyloxy)-1H-indol-1-yl]acetic acid, an aldose reductase inhibitor and PPAR gamma ligand
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Date
2015-01-01
Author
Prnova, Marta Soltesova
Majekova, Magdalena
Milackova, Ivana
Diez-Dacal, Beatriz
Perez-Sala, Dolores
Ceyhan, Muserref Seyma
Banerjee, Sreeparna
Stefek, Milan
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Based on overlapping structural requirements for both efficient aldose reductase inhibitors and PPAR ligands, [5-(benzyloxy)-1H-indol-1-yl] acetic acid (compound 1) was assessed for inhibition of aldose reductase and ability to interfere with PPAR gamma. Aldose reductase inhibition by 1 was characterized by IC50 in submicromolar and low micromolar range, for rat and human enzyme, respectively. Selectivity in relation to the closely related rat kidney aldehyde reductase was characterized by approx. factor 50. At organ level in isolated rat lenses, compound 1 significantly inhibited accumulation of sorbitol in a concentration-dependent manner. To identify crucial interactions within the enzyme binding site, molecular docking simulations were performed. Based on luciferase reporter assays, compound 1 was found to act as a ligand for PPAR gamma, yet with rather low activity. On balance, compound 1 is suggested as a promising lead-like scaffold for agents with the potential to interfere with multiple targets in diabetes.
Subject Keywords
Aldose Reductase Inhibitor
,
PPAR. Ligand
,
Diabetes
,
Indole
URI
https://hdl.handle.net/11511/42379
Journal
ACTA BIOCHIMICA POLONICA
DOI
https://doi.org/10.18388/abp.2014_953
Collections
Department of Biology, Article