Ukr.Biochem.J. 2018; Volume 90, Issue 1, Jan-Feb, pp. 25-33

doi: https://doi.org/10.15407/ubj90.01.025

Cаlіx[4]аrene С-956 is effective inhibitor of Н(+)-Сa(2+)-exchanger in smooth muscle mitochondria

G. V. Danylovych1, О. V. Kоlomiets1, Yu. V. Danylovych1, R. V. Rodik2, V. I. Kаlchenko2, S. О. Kоsterin1

1Palladin Institute of Biochemistry, National Academy of Science of Ukraine, Kyiv;
e-mail: danylovych@biochem.kiev.ua;
2Institute of Organic Chemistry, National Academy of Science of Ukraine, Kyiv

It was shown that calix[4]arene C-956 exhibited a pronounced concentration-dependent (10-100 μM) inhibitory effect on the H+-Ca2+-exchanger of the inner mitochondrial membrane of rat uterine myocytes (Ki 35.1 ± 7.9 μM). The inhibitory effect of calix[4]arene C-956 was accompanied by a decrease in the initial rate (V0) and an increase in the magnitude of the characteristic time (τ1/2) of the ΔрН-induced Са2+ release. At the same time, it did not affect the potential-dependent accumulation of Ca2+ in mitochondria. Thus, the action of calix[4]arene C-956 might be directed on increasing the concentration of Ca ions in the mitochondrial matrix. The calculation of basic kinetic parameters of the Ca2+ transport from isolated organelles (in the case of its non-zero stationary level), based on changes in fluorescence of Ca2+-sensitive dye Fluo-4 AM in mitochondria was performed. The proposed approach can be used for the kinetic analysis of the exponential decrease of the fluorescence response of any probes under the same experimental conditions.

Keywords: , , , ,


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