1. Cytoprotective and antioxidant properties of organic selenides for the myelin-forming cells, oligodendrocytes.
- Author
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Shaaban, Saad, Vervandier-Fasseur, Dominique, Andreoletti, Pierre, Zarrouk, Amira, Richard, Philippe, Negm, Amr, Manolikakes, Georg, Jacob, Claus, and Cherkaoui-Malki, Mustapha
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SELENIDES , *OLIGODENDROGLIA , *GLUTATHIONE peroxidase , *PHARMACOKINETICS , *BLOOD-brain barrier - Abstract
Here a new series of twenty-one organoselenides, of potential protective activity, were synthesized and tested for their intrinsic cytotoxicity, anti-apoptotic and antioxidant capacities in oligodendrocytes. Most of the organoselenides were able to decrease the ROS levels, revealing antioxidant properties. Compounds 5b and 7b showed a high glutathione peroxidase (GPx)-like activities, which were 1.5 folds more active than ebselen. Remarkably, compound 5a diminished the formation of the oligodendrocytes SubG1 peak in a concentration-dependent manner, indicating its anti-apoptotic properties. Furthermore, based on the SwissADME web interface, we performed an in-silico structure-activity relationship to explore the drug-likeness of these organoselenides, predicting the pharmacokinetic parameters for compounds of interest that could cross the blood-brain barrier. Collectively, we present new organoselenide compounds with cytoprotective and antioxidant properties that can be considered as promising drug candidates for myelin diseases. [ABSTRACT FROM AUTHOR]
- Published
- 2018
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