The use of dimethylsulfoxide as a solvent in enzyme inhibition studies: the case of aldose reductase

Autor:	Vito Barracco, Umberto Mura, Mario Cappiello, Livia Misuri, Francesco Balestri, Antonella Del-Corso, Roberta Moschini
Jazyk:	angličtina
Rok vydání:	2017
Předmět:	0301 basic medicine Phloretin Stereochemistry Cell 01 natural sciences aldose reductase differential inhibitors Dose-Response Relationship Structure-Activity Relationship 03 medical and health sciences chemistry.chemical_compound Rutin Aldehyde Reductase Drug Discovery medicine Humans Enzyme Inhibitors Pharmacology chemistry.chemical_classification aldose reductase Dimethyl sulfoxide Dimethyl Sulfoxide Dose-Response Relationship Drug Recombinant Proteins Solvents Drug Discovery3003 Pharmaceutical Science Aldose reductase 010405 organic chemistry Chemistry Neohesperidin dihydrochalcone lcsh:RM1-950 General Medicine 0104 chemical sciences Solvent 030104 developmental biology medicine.anatomical_structure Enzyme lcsh:Therapeutics. Pharmacology Biochemistry Drug Research Paper
Zdroj:	Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 32, Iss 1, Pp 1152-1158 (2017) Journal of Enzyme Inhibition and Medicinal Chemistry
ISSN:	1475-6374 1475-6366
Popis:	Aldose reductase (AR) is an enzyme devoted to cell detoxification and at the same time is strongly involved in the aetiology of secondary diabetic complications and the amplification of inflammatory phenomena. AR is subjected to intense inhibition studies and dimethyl sulfoxide (DMSO) is often present in the assay mixture to keep the inhibitors in solution. DMSO was revealed to act as a weak but well detectable AR differential inhibitor, acting as a competitive inhibitor of the L-idose reduction, as a mixed type of non-competitive inhibitor of HNE reduction and being inactive towards 3-glutathionyl-4-hydroxynonanal transformation. A kinetic model of DMSO action with respect to differently acting inhibitors was analysed. Three AR inhibitors, namely the flavonoids neohesperidin dihydrochalcone, rutin and phloretin, were used to evaluate the effects of DMSO on the inhibition studies on the reduction of L-idose and HNE.
Databáze:	OpenAIRE
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