97490-50-1Relevant academic research and scientific papers
Design, Synthesis, and In Vitro Evaluation of a Novel Probucol Derivative: Protective Activity in Neuronal Cells Through GPx Upregulation
Quispe, Ruth Liliám,Canto, R?mulo Faria Santos,Jaramillo, Michael Lorenz,Barbosa, Flavio Augusto Rocha,Braga, Ant?nio Luiz,de Bem, Andreza Fabro,Farina, Marcelo
, p. 7619 - 7634 (2018/02/19)
Recent studies have shown that probucol (PB), a hipocholesterolemic agent with antioxidant and anti-inflammatory properties, presents neuroprotective properties. On the other hand, adverse effects have limited PB’s clinical application. Thus, the search for PB derivatives with no or less adverse effects has been a topic of research. In this study, we present a novel organoselenium PB derivative (RC513) and investigate its potential protective activity in an in vitro experimental model of oxidative toxicity induced by tert-butyl hydroperoxide (tBuOOH) in HT22 neuronal cells, as well as exploit potential protective mechanisms. tBuOOH exposure caused a significant decrease in the cell viability, which was preceded by (i) increased reactive species generation and (ii) decreased mitochondrial maximum oxygen consumption rate. RC513 pretreatment (48?h) significantly prevented the tBuOOH-induced decrease of cell viability, RS generation, and mitochondrial dysfunction. Of note, RC513 significantly increased glutathione peroxidase (GPx) activity and mRNA expression of GPx1, a key enzyme involved in peroxide detoxification. The use of mercaptosuccinic acid, an inhibitor of GPx, significantly decreased the protective activity of RC513 against tBuOOH-induced cytotoxicity in HT22 cells, highlighting the importance of GPx upregulation in the observed protection. In summary, the results showed a significant protective activity of a novel PB derivative against tBuOOH-induced oxidative stress and mitochondrial dysfunction, which was related to the upregulation of GPx. Our results point to RC513 as a promising neuroprotective molecule, even though studies concerning potential beneficial effects and safety aspects of RC513 under in vivo conditions are well warranted.
COMPOSITIONS AND METHODS FOR TREATING CARDIOVASCULAR DISORDERS
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Page/Page column 60-61, (2010/11/08)
The present invention relates to compounds and methods for the treatment of cardiovascular diseases and disorders. Compounds according to the present invention may comprise an optionally substituted phenyl ring linked to an aromatic or alkyl group by a spacer, wherein the spacer comprises two groups selected from selenium, sulfur, S(O) and S(O)2 and may further optionally comprise an alkylene, alkenylene, cycloalkylene or arylene moiety between the respective selenium, sulfur, S(O) and S(O)2 groups.
