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

• Published in: The Ukrainian Biochemical Journal
• Main Authors: Т. O. Veklich, O. A. Skrabak, Yu. V. Nikonishyna, R. V. Rodik, V. I. Kalchenko, S. O. Kosterin
• Format: Article
• Language: English
• Published: National Academy of Sciences of Ukraine, Palladin Institute of Biochemistry 2018-10-01
• Subjects: Ca(2+)-Mg(2+)-ATPase; calix[4]arenes; enzymatic hydrolysis of ATP; myometrium; plasma membrane; smooth muscle cells
• Online Access: http://ukrbiochemjournal.org/2018/09/calix4arene-%d1%81-956-selectively-inhibits-plasma-membrane-%d1%81%d0%b02mg2-%d0%b0%d1%82%d1%80ase-in-myometrial-cells.html
• ISSN: 2409-4943; 2409-4943

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.