glutathione peroxidase; diselenide and selenide derivatives; Ebselen; electron paramagnetic resonance; lipid peroxidation
Abstract :
[en] Four analogues of Ebselen were synthesized and their glutathione peroxidase activity and antioxidant property evaluated and compared to Ebselen. Among the studied compounds, only diselenide [3] exhibited both glutathione peroxidase activity and radical-scavenging capability. Compounds [3] and [4] showed a strong inhibitory effect (53% and 43%, respectively) on the lipid peroxidation of linoleic acid compared to Ebselen and selenide derivatives ([1] and [2]) which were less active (28%, 26% and 18% inhibition, respectively). A concentration-dependent inhibitory effect was also found in the model of the formation of ABTS*+ radical cation: 65% and 89% inhibition for compound [3] at 10(-4) M and 5 x 10(-5) M, respectively, and 68% and 90% for compound [4], compared to 14% and 52% inhibition for Ebselen and the diselenides [1] and [2] (29%, 46% and 45%, 68%, respectively). By EPR spin trapping technique, the following inhibitory profile of the Ebselen analogues was observed towards the formation of thiyl radicals: Ebselen = [3]>[1]>[2]>[4]. Studies with compound [3] are in progress on oxidative stress cell models.
Disciplines :
Biochemistry, biophysics & molecular biology
Author, co-author :
Mouithys-Mickalad, Ange ; Université de Liège - ULiège > Centre de l'oxygène : Recherche et développement (C.O.R.D.)
Mareque-Faez, Juan
Chistiaens, U.
Kohnen, Stephan ; Université de Liège - ULiège > Département clinique des animaux de compagnie et des équidés > Anesthésiologie gén. et pathologie chirurg. des grds animaux
Deby, Christiane ; Centre Hospitalier Universitaire de Liège - CHU > Administration des patients - Admission des hospitalisés
Hoebeke, Maryse ; Université de Liège - ULiège > Département de physique > Spectroscopie biomédicale
Lamy, Maurice ; Université de Liège - ULiège > Département des sciences cliniques > Anesthésie et réanimation
Deby-Dupont, G.
Language :
English
Title :
In vitro evaluation of glutathione peroxidase (GPx)-like activity and antioxidant properties of some Ebselen analogues
Publication date :
2004
Journal title :
Redox Report: Communications in Free Radical Research
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