Ukr.Biochem.J. 2018; Volume 90, Issue 5, Sep-Oct, pp. 34-42

doi: https://doi.org/10.15407/ubj90.05.034

Calix[4]arene С-956 selectively inhibits plasma membrane Са(2+),Mg(2+)-АТРase in myometrial cells

24.09.2018   Uncategorized   No comments

Т. O. Veklich1, O. A. Skrabak1, Yu. V. Nikonishyna1, R. V. Rodik2, V. I. Kalchenko2, S. O. Kosterin1

1Palladin Institute of Biochemistry, National Academy of Sciences of Ukraine, Kyiv;
2Institute of Organic Chemistry, National Academy of Sciences of Ukraine, Kyiv;
e-mail: veklich@biochem.kiev.ua; manli@ioch.kiev.ua

Using enzymatic assays and kinetic analysis, we demonstrated that 100 µM calix[4]arene C-956 (5,11,17,23-tetra(trifluoro)methyl-(phenylsulfonylimino) methylamino-25,27-dioctyloxy-26,28-dipropoxycalix[4]arene) had the most significant inhibitory effect on the plasma membrane Са2+,Mg2+-АТРase activity compared to effects of other calix[4]arenes, and had no effect on specific activities of other membrane ATPases. Using confocal microscopy and fluorescent probe fluo-4, we observed an increase of the intracellular level of Ca2+ after application of calix[4]arene C-956 to immobilized myocytes. Analysis of the effect of calix[4]arene C-956 on the hydrodynamic diameter of myocytes demonstrated that application of calix[4]arene C-956 solution decreased this parameter by 45.5 ± 9.4% compared to control value similarly to the action of uterotonic drug oxytocin.

Keywords: , , , , ,

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