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3′-O-(3-Chloropivaloyl)quercetin, α-glucosidase inhibitor with multi-targeted therapeutic potential in relation to diabetic complications

  • Marta Soltesova-Prnova , Ivana Milackova and Milan Stefek EMAIL logo
Published/Copyright: June 25, 2016
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Abstract

The novel derivative of quercetin 3′-O-(3-chloropivaloyl)quercetin (CPQ) inhibited α-glucosidase in a non-competitive manner with an efficacy exceeding that of the parent quercetin. In addition, it inhibited aldose reductase isolated from rat lenses with an IC50 in the low micromolar range and attenuated sorbitol accumulation in isolated rat eye lenses with an activity comparable with that of quercetin. Moreover, it scavenged stable free-radicals of DPPH more efficiently than did quercetin. By inhibiting α-glucosidase and affecting both the polyol pathway and oxidative stress, CPQ represents a promising agent for the multi-targeted pharmacology of diabetic complications.

Acknowledgements

This work was supported by grants VEGA 2/0041/15 and the Agency of the Ministry of Education, Science, Research and Sport of the Slovak Republic for the Structural Funds of EU, OP R&D of ERDF within the project ”Evaluation of natural substances and their selection for prevention and treatment of lifestyle diseases” (ITMS 26240220040).

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Received: 2016-1-20
Revised: 2016-3-1
Accepted: 2016-3-17
Published Online: 2016-6-25
Published in Print: 2016-11-1

© 2016 Institute of Chemistry, Slovak Academy of Sciences

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