Tag Archives: alix[4]arene C-1130
A new selective inhibitor of the Mg(2+), ATP-dependent sodium pump calix[4]aren С-1130 as a modulator of myometrial contraction energy
S. O. Kosterin1*, O. V. Tsymbalyuk2, R. V. Rodik3, V. I. Kalchenko3
1Palladin Institute of Biochemistry, National Academy of Sciences of Ukraine, Kyiv;
*e-mail: kinet@biochem.kiev.ua;
2Taras Shevchenko National University of Kyiv, Ukraine;
e-mail: otsymbal@knu.ua;
3Institute of Organic Chemistry, National Academy of Sciences of Ukraine, Kyiv;
e-mail: manli@ioch.kiev.ua
Received: 19 November 2025; Revised: 23 January 2026;
Accepted: 03 April 2026; Available on-line: April 2026
It is known, that the functioning of non-electrogenic 2Na+-Ca2+-exchange system, localized in the myometrium cells plasma membrane, is ensured by the energy of the transmembrane sodium gradient, created by the Mg2+, ATP-dependent sodium pump. The aim of the study was to determine how the inhibitor of this pump calix[4]arene С-1130 affects the mechanokinetics and energy of myometrium contraction-relaxation. The experiments were conducted using female Wistar rats. The contractile activity of the longitudinal smooth muscles of the uterine horns was studied tensometrically. The method of determining the mechanical work А and power N at any time moment t of the of smooth muscle isotonic contraction-relaxation complete cycle was developed and tested in the tensometric experiments. Calix[4]arene С-1130 was dissolved in dimethylsulfoxide and introduced into the working solutions in a 10-5 М concentration. It was found that under calix[4]arene С-1130 treatment, the relative values of the mechanical work A were achieved at a time when the contraction-relaxation cycle under control conditions was practically completed, while the maximum values of power N were reached faster than in the control. These results indicate that calix[4]arene С-1130 was capable of inducing the increase in the maximal value of the smooth muscle mechanical work, promoting its relaxation without a considerable change in the contraction power. The developed methodology may be useful for the comparative study of the pharmacological drugs effect on the smooth muscles contractile activity in the “norm-pathology” format.