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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

Institute of Experimental Pharmacology and Toxicology, Slovak Academy of Sciences, Dúbravská cesta 9, 84104 Bratislava, Slovakia

 

E-mail: milan.stefek@savba.sk

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.

Keywords: 3′-O-(3-chloropivaloyl)quercetin – α-glucosidase inhibitor – aldose reductase inhibitor – antioxidant – diabetic complications

Full paper is available at www.springerlink.com.

DOI: 10.1515/chempap-2016-0078

 

Chemical Papers 70 (11) 1439–1444 (2016)

Wednesday, August 17, 2022

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