Spontaneous reversal of small molecule-induced mitochondrial uncoupling: the case of anilinothiophenes.

Tissue specificity can render mitochondrial uncouplers more promising as leading compounds for creating drugs against serious diseases. In search of tissue-specific uncouplers, we address anilinothiophenes as possible glutathione-S-transferase substrates (GST). Earlier, 'cyclic' uncoupling activity was reported for 5-bromo-N-(4-chlorophenyl)-3,4-dinitro-2-thiophenamine (BDCT) in isolated rat liver mitochondria (RLM).

Rhodamine 19 Alkyl Esters as Effective Antibacterial Agents.

Mitochondria-targeted antioxidants (MTAs) have been studied quite intensively in recent years as potential therapeutic agents and vectors for the delivery of other active substances to mitochondria and bacteria. Their most studied representatives are MitoQ and SkQ1, with its fluorescent rhodamine analog SkQR1, a decyl ester of rhodamine 19 carrying plastoquinone. In the present work, we observed a pronounced antibacterial action of SkQR1 against Gram-positive bacteria, but virtually no effect on Gram-negative bacteria.

Synthesis of Triphenylphosphonium-Linked Derivative of 3,5-Di-butyl-4-hydroxybenzylidene-malononitrile (SF6847) via Knoevenagel Reaction Yields an Effective Mitochondria-Targeted Protonophoric Uncoupler.

Mitochondrial uncouplers are actively sought as potential therapeutics. Here, we report the first successful synthesis of mitochondria-targeted derivatives of the highly potent uncoupler 3,5-di-butyl-4-hydroxybenzylidene-malononitrile (SF6847), bearing a cationic alkyl(triphenyl)phosphonium (TPP) group. As a key step of the synthesis, we used condensation of a ketophenol with malononitrile via the Knoevenagel reaction.

One-Stage Process of Reduction, Fluorination, and Doping with Nitrogen of Graphene Oxide Films.

The possibility of chemical modification of a graphene oxide film deposited on a Si/SiO substrate during a one-stage hydrothermal process in the presence of fluorine ions and reducing agents, such as ascorbic acid or hydrazine, is shown. The proposed technique makes it possible to obtain reduced fluorinated graphene nitride oxide (RGOFN) in the form of a thin film with a controlled composition of functional groups by changing the type and concentration of the reducing agent and then transferring the obtained films to any substrate. XPS and IR spectroscopy of the obtained films revealed controlled changes in the structure and composition of graphene oxide associated with the removal of oxygen groups and the incorporation of fluorine ions as well as the reduction of conjugated double bonds and the controlled incorporation of nitrogen into thin RGOFN films.

Selectivity of cation transport across lipid membranes by the antibiotic salinomycin.

The ionophoric antibiotic salinomycin is in the phase of preclinical tests against several types of malignant tumors including breast cancer. Notwithstanding, the data on its ion selectivity, although being critical for its therapeutic activity, are rather scarce. In the present work, we studied the ability of salinomycin to exert cation/H-exchange across artificial bilayer lipid membranes (BLM) by measuring electrical potential on planar BLM in the presence of a protonophore and fluorescence responses of the pH-sensitive dye pyranine entrapped in liposomes.