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Information × Registration Number 0222U000342, 0120U000183 , R & D reports Title Using of calixarenes as effectors of energy-dependent Са2+-transporting systems for directional modulation of electro- and pharmacomechanical coupling in smooth muscle. popup.stage_title Head Kosterin Serhii O., Доктор біологічних наук Registration Date 06-01-2022 Organization Palladin Institute of Biochemistry of the National Academy of Sciences of Ukraine popup.description2 Using the method of flow cytometry, it was found that 1 μm calix[4]aren C-1011 reduces the CCCP-sensitive component of polarization of mitochondrial membranes of Mock cells, but on RukUp-1 cells this figure increases. The survival of Mock and RukUp-1 cells is reduced by 45 and 11%, respectively, under conditions of incubation of cells with 1 μM calix[4]aren C-1011 for 24 hours. It was also proved that chalcone-containing calix[4]arenes (C-138, C-1012, C-1021, C-1023, C-1024 and C-1011) with varying efficiency inhibit the oxidation of endogenous nucleotides in the electron transport chain in the presence of respiratory substrates and cause increased generation of reactive oxygen species, which can lead to intensification of oxidative processes in mitochondria and mediated by reactive oxygen species decrease in the intensity of oxidative phosphorylation. It was found that the calix[4]aren C-1193 inhibited the oxidation of NADH in the respiratory chain and the generation of reactive oxygen species by mitochondria under conditions of a moderate increase in the volume of organelles. It is shown that calix[4]arenes - C-97 and C-107 are the most effective inhibitors (I0.5 ≈ 30 - 60 nM), their use at a concentration of 10 μm guarantees complete inhibition of Na+,K+-ATPase activity. At the same time, calix[4]aren C-99 (I0.5 ≈ 100 nM) and oubain (I0.5 ≈ 20 μM) completely inhibit the activity of the enzyme at a concentration of 1 mM. It is proved that the introduction of ATP into the incubation medium is accompanied by an approximately 3-fold increase in the concentration of Ca in the mitochondrial matrix. This increase is accompanied by an increase in Ca2+ release from mitochondria. The concentration of Ca2+ in Mg2+,ATP-medium is approximately 19 times higher than in Mg2+-medium. Cyclosporine A, ruthenium red or oligomycin did not affect either the concentration of Ca2+ in the matrix or the release of cations from mitochondria. Product Description popup.authors Babich Lidiya Grygorivna Veklich Tetiana Oleksandrivna Danylovych Hanna Victorivna Danylovuch Yuriy Volodymyrosych Karakhim Sergii O Чуніхін Олександр Юрієвич Shlykov Serhiy Georgiyovich popup.nrat_date 2022-03-09 Close