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1.
Eur J Pharmacol ; 770: 78-84, 2016 Jan 05.
Article in English | MEDLINE | ID: mdl-26667999

ABSTRACT

Mesoionic compounds have shown antitumor and citotoxic activity against different tumor cells lines, which has been attributed to their physical and chemical characteristics. Among these compounds, the 1,3,4-thiadiazolium-2-phenylamine derivatives have been highlighted due to their important anti-melanoma activity. In this work, the effects of three derivatives that belong this class, MI-J, MI-4F and MI-2,4diF, on the oxidative stress parameters were evaluated using rat liver mitochondria. All the derivatives prevented natural and calcium induced oxidation of pyridine nucleotides at lower concentrations (6.5 and 32.5nmol/mg protein). The calcium uptake was inhibited by all the derivatives at higher concentrations (65 and 130nmol/mg protein), whereas the cation efflux was inhibited only by the MI-J (52%) and MI-4F (50%), possibly by inhibiting the formation of the permeability transition pore (PTP) by 100% and 50%, respectively, as observed in the same experimental conditions. MI-2,4diF did not inhibit the mitochondrial permeability transition or calcium efflux. The enzymatic activity of glutathione reductase, glutathione peroxidase and catalase was not affected by any derivative, but superoxide dismutase was inhibited by all the derivatives. MI-J inhibited enzyme activity significantly (85%) at the highest concentration (130nmol/mg protein); on the other hand, their activity was less affected by fluorine derivatives (MI-4F-20% and MI-2,4diF-32%). These results suggest that these derivatives exert antioxidant effects on isolated mitochondria.


Subject(s)
Antioxidants/chemistry , Antioxidants/pharmacology , Mitochondria/drug effects , Mitochondria/metabolism , Thiadiazoles/chemistry , Thiadiazoles/pharmacology , Animals , Biological Transport/drug effects , Calcium/metabolism , Male , Mitochondria/enzymology , Nucleotides/metabolism , Oxidation-Reduction/drug effects , Permeability/drug effects , Rats , Rats, Wistar
2.
Comp Biochem Physiol A Mol Integr Physiol ; 146(4): 588-600, 2007 Apr.
Article in English | MEDLINE | ID: mdl-16626983

ABSTRACT

Oxidative stress can take place in marine bivalves under a series of environmental adverse conditions. The study of different systems related to oxidative stress in these organisms can give important information about their physiological status and also about environmental health. Bivalves have been proposed as good sentinel organisms in pollution monitoring studies through the analysis of biochemical biomarkers, and most of the biomarkers analyzed are those related to oxidative stress. However, it is very important to know how other environmental factors not associated to the presence of pollutants might affect these parameters. We have studied a series of mechanisms related to oxidative stress in mussels which inhabit the Brazilian coast, especially in Perna perna species, subjected to different stress conditions, such as the exposure to different contaminants in the laboratory and in the field, the exposure of mussels to air and re-submersion, simulating the tidal oscillations, and in mussels collected at different seasons. Both oxidative damage levels and antioxidant defense systems were strongly affected by the different environmental stress. This review summarizes the data obtained in some studies carried out in bivalves from the Brazilian coast.


Subject(s)
Antioxidants/metabolism , Bivalvia/physiology , DNA Damage , Lipid Peroxidation , Oxidative Stress , Animals , Brazil , Ecology , Marine Biology , Perna/physiology , Reactive Oxygen Species/metabolism
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