3′-O-(3-Chloropivaloyl)quercetin, α-glucosidase inhibitor with multi-targeted therapeutic potential in relation to diabetic complications
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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© 2016 Institute of Chemistry, Slovak Academy of Sciences
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- Original Paper
- Fluorescence-enhanced optical sensor for detection of Al3+ in water based on functionalised nanoporous silica type SBA-15
- Original Paper
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- Original Paper
- Production of high-content galacto-oligosaccharides mixture using β-galactosidase and Kluyveromyces marxianus entrapped in polyvinylalcohol gel
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- Efficient utilization of inulin and glycerol as fermentation substrates in erythritol and citric acid production using Yarrowia lipolytica expressing inulinase
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- Production and characterization of surfactant-stable fungal keratinase from Gibberella intermedia CA3-1 with application potential in detergent industry
- Original Paper
- Vapour-phase condensation of methyl propionate with trioxane over alumina-supported potassium catalyst
- Original Paper
- Slow pyrolysis of pre-dried sewage sludge
- Original Paper
- Synthesis, antioxidant, antibacterial, and DFT study on a coumarin based salen-type Schiff base and its copper complex
- Original Paper
- Identification of selective oxidation of TiC/SiC composite with X-ray diffraction and Raman spectroscopy
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- Toxicity of zinc oxide nanoparticles to the annelid Enchytraeus crypticus in agar-based exposure media
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- Synthesis and antibacterial evaluation of novel Schiff base derivatives containing 4(3H)-quinazolinone moiety
- Short Communication
- The aza-Pudovik reaction accelerated in external constant magnetic field