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Milackova, Ivana; Prnova, Marta Soltesova; Majekova, Magdalena; Sotnikova, Ruzena; Stasko, Michal; Kovacikova, Lucia; Banerjee, Sreeparna; Veverka, Miroslav; Stefek, Milan
{ "@context": "https://schema.org/", "@id": 82639, "@type": "ScholarlyArticle", "creator": [ { "@type": "Person", "affiliation": "Slovak Acad Sci, Inst Expt Pharmacol & Toxicol, Bratislava, Slovakia", "name": "Milackova, Ivana" }, { "@type": "Person", "affiliation": "Slovak Acad Sci, Inst Expt Pharmacol & Toxicol, Bratislava, Slovakia", "name": "Prnova, Marta Soltesova" }, { "@type": "Person", "affiliation": "Slovak Acad Sci, Inst Expt Pharmacol & Toxicol, Bratislava, Slovakia", "name": "Majekova, Magdalena" }, { "@type": "Person", "affiliation": "Slovak Acad Sci, Inst Expt Pharmacol & Toxicol, Bratislava, Slovakia", "name": "Sotnikova, Ruzena" }, { "@type": "Person", "affiliation": "Slovak Acad Sci, Inst Expt Pharmacol & Toxicol, Bratislava, Slovakia", "name": "Stasko, Michal" }, { "@type": "Person", "affiliation": "Slovak Acad Sci, Inst Expt Pharmacol & Toxicol, Bratislava, Slovakia", "name": "Kovacikova, Lucia" }, { "@type": "Person", "affiliation": "Middle E Tech Univ, Dept Biol Sci, TR-06531 Ankara, Turkey", "name": "Banerjee, Sreeparna" }, { "@type": "Person", "affiliation": "Eurofins Bel Novamann Ltd, Nove Zamky, Slovakia", "name": "Veverka, Miroslav" }, { "@type": "Person", "affiliation": "Slovak Acad Sci, Inst Expt Pharmacol & Toxicol, Bratislava, Slovakia", "name": "Stefek, Milan" } ], "datePublished": "2015-01-01", "description": "The ability of flavonoids to affect multiple key pathways of glucose toxicity, as well as to attenuate inflammation has been well documented. In this study, the inhibition of rat lens aldose reductase by 3,7-di-hydroxy-2-[4-(2-chloro-1,4-naphthoquinone-3-yloxy)-3-hydroxyphenyl]-5-hydroxy-chromen-4-one (compound 1), was studied in greater detail in comparison with the parent quercetin (compound 2). The inhibition activity of 1, characterized by IC50 in low micromolar range, surpassed that of 2. Selectivity in relation to the closely related rat kidney aldehyde reductase was evaluated. At organ level in isolated rat lenses incubated in the presence of high glucose, compound 1 significantly inhibited accumulation of sorbitol in a concentration-dependent manner, which indicated that 1 was readily taken up by the eye lens cells and interfered with cytosolic aldose reductase. In addition, compound 1 provided macroscopic protection of colonic mucosa in experimental colitis in rats. At pharmacologically active concentrations, compound 1 and one of its potential metabolite 2-chloro-3-hydroxy[1,4]-naphthoquinone (compound 3) did not affect osmotic fragility of red blood cells.", "headline": "2-Chloro-1,4-naphthoquinone derivative of quercetin as an inhibitor of aldose reductase and anti-inflammatory agent", "identifier": 82639, "image": "https://aperta.ulakbim.gov.tr/static/img/logo/aperta_logo_with_icon.svg", "license": "http://www.opendefinition.org/licenses/cc-by", "name": "2-Chloro-1,4-naphthoquinone derivative of quercetin as an inhibitor of aldose reductase and anti-inflammatory agent", "url": "https://aperta.ulakbim.gov.tr/record/82639" }
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