Abstract
The supramolecular compound calix[4]arene C-90 (5,11,17,23-tetra(trifluoro)methyl(phenylsulfonylimino)-methylamino-25,26,27,28-tetrapropoxycalix[4]arene) is shown to efficiently inhibit the ATP hydrolase activity of Ca2+,Mg2+-ATPase in the myometrium cell plasma membrane fraction and also in a preparation of the purified enzyme solubilized from this subcellular fraction. The inhibition coefficient I 0.5 values were 20.2 ± 0.5 and 58.5 ± 6.4 μM for the membrane fraction and the solubilized enzyme, respectively. The inhibitory effect of calix[4]arene C-90 was selective comparatively to other ATPases localized in the plasma membrane: calix[4]arene C-90 did not influence the activities of Na+,K+-ATPase and “basal” Mg2+-ATPase. The inhibitory effect of calix[4]arene C-90 on the Ca2+,Mg2+-ATPase activity was associated with the cooperative action of four trifluoromethylphenyl sulfonylimine (sulfonylamidine) groups oriented similarly on the upper rim of the calix[4]arene macrocycle (the calix[4]arene “bowl”). The experimental findings seem to be of importance for studies, using calix[4]arene C-90, of membrane mechanisms of regulation of calcium homeostasis in smooth muscle cells and also for investigation of the participation of the plasma membrane Ca2+-pump in control of electro- and pharmacomechanical coupling in myocytes.
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Abbreviations
- PM:
-
plasma membrane
- SMC:
-
smooth muscular cells
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Original Russian Text © T. A. Veklich, A. A. Shkrabak, N. N. Slinchenko, I. I. Mazur, R. V. Rodik, V. I. Boyko, V. I. Kalchenko, S. A. Kosterin, 2014, published in Biokhimiya, 2014, Vol. 79, No. 5, pp. 532–540.
Originally published in Biochemistry (Moscow) On-Line Papers in Press, as Manuscript BM13-319, March 30, 2014.
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Veklich, T.A., Shkrabak, A.A., Slinchenko, N.N. et al. Calix[4]arene C-90 selectively inhibits Ca2+,Mg2+-ATPase of myometrium cell plasma membrane. Biochemistry Moscow 79, 417–424 (2014). https://doi.org/10.1134/S0006297914050058
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DOI: https://doi.org/10.1134/S0006297914050058