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Belosludtsev 2018 Biochim Biophys Acta
Additional label Labels  + , 2018-08  +
Coupling states OXPHOS  +
Enzyme Complex I  + , Complex II;succinate dehydrogenase  + , Complex III  + , Complex IV;cytochrome c oxidase  +
Has abstract The paper considers the effects of bedaqui
The paper considers the effects of bedaquiline (BDQ), an antituberculous preparation of the new generation, on rat liver mitochondria. It was shown that 50 μM BDQ inhibited mitochondrial respiration measured with substrates of complexes I and II (glutamate/malate and succinate/rotenone systems respectively) in the states V<sub>3</sub> and V<sub>DNP</sub>. At the same time, at concentrations below 50 μM, BDQ slightly stimulated respiration with substrates of complex I in the state V<sub>2</sub>. BDQ was also found to suppress, in a dose-dependent manner, the activity of complex II and the total activity of complexes II + III of the mitochondrial transport chain. It was discovered that at concentrations up to 10 μM, BDQ inhibited H<sub>2</sub>O<sub>2</sub> production in mitochondria. BDQ (10-50 μM) suppressed the opening of Ca<sup>2+</sup>-dependent CsA-sensitive mitochondrial permeability transition pore. The latter was revealed experimentally as the inhibition of Ca<sup>2+</sup>/P<sub>i</sub>-dependent swelling of mitochondria, suppression of cytochrome c release, and an increase in the Ca<sup>2+</sup> capacity of the organelles. BDQ also decreased the rate of mitochondrial energy-dependent K<sup>+</sup> transport, which was evaluated by the energy-dependent swelling of mitochondria in a K<sup>+</sup> buffer and DNP-induced K<sup>+</sup> efflux from the organelles. The possible mechanisms of BDQ effect of rat liver mitochondria are discussed.
t of rat liver mitochondria are discussed.  +
Has editor [[Plangger M]]  + , [[Kandolf G]]  +
Has info [https://www.ncbi.nlm.nih.gov/pubmed/29920239 PMID: 29920239]  +
Has publicationkeywords Bedaquiline  + , K(+) transport  + , MPT pore  + , Mitochondria  + , Mitochondrial respiration  + , Oxidative phosphorylation  +
Has title Belosludtsev KN, Belosludtseva NV, Talanov EY, Tenkov KS, Starinets VS, Agafonov AV, Pavlik LL, Dubinin MV (2018) Effect of bedaquiline on the functions of rat liver mitochondria. Biochim Biophys Acta 1861:288-97.  +
Instrument and method Oxygraph-2k  +
Mammal and model Rat  +
MiP area Respiration  + , Pharmacology;toxicology  +
Pathways N  + , S  + , NS  +
Preparation Isolated mitochondria  +
Tissue and cell Liver  +
Was published in journal Biochim Biophys Acta +
Was published in year 2018  +
Was written by Belosludtsev K + , Belosludtseva NV + , Talanov EY + , Tenkov KS + , Starinets VS + , Agafonov AV + , Pavlik LL + , Dubinin M +
Categories Publications
Modification date
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13:34:48, 2 January 2019  +
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