Calix4arene С-956, the inhibitor of Mg2-АТР-dependent calcium pump of the sarcoplasmic reticulum, induces an increase in the Са2 concentration in aortic myocytes, causes the activation of mechanical tension waves and enhances muscle preparation contractions
O. Tsymbalyuk
, T. Veklich
, O. Maliuk
, R. Rodik
, O. Karakhim
, S. Kosterin
Резюме: Objective: Sarcoplasmic reticulum is one of the most important intracellular Ca2+ depots, and in it the Ca2+,Mg2+-ATPase ensures the process of Ca2+ accumulation. A large number of pathologies are caused by a violation of Ca2+ deposition, therefore it is important to search for non-toxic compounds – modifiers of these processes. Such modifiers can be certain calixarenes, in particular calix[4]arene C-956. Materials and methods: The studies were conducted on isolated myocytes and ring preparations of the aorta of rats. The enzymatic activity of sarcoplasmic reticulum Ca2+,Mg2+-ATPase of myocytes was investigated. Changes in Ca2+ concentration in myocytes were recorded by confocal microscopy. Tensometric experiments were performed in isometric and isotonic modes. Kinetic analysis of contractions was carried out by the Kosterin-Burdyga method. Results: Calix[4]arene C-956 has the most significant inhibitory effect on Ca2+,Mg2+-ATPase activity in sarcoplasmic reticulum compared to other analogues. The application of C-956 to myocytes causes an increase in the intracellular Ca2+ concentration. Also, calix[4]arene C-956 activated tension waves and increased the amplitude of contractions, without changing their kinetic characteristics. Discussion: Since calix[4]arene C-956 inhibited the activity of sarcoplasmic reticulum Ca2+,Mg2+-ATPase, increased the concentration of Ca2+ ions in the cytoplasm, and activated the contraction of aortic rings without changing their normalized maximum velocities, it can be assumed that it acts as a selective inhibitor of this enzyme. Conclusion: Calix[4]arene C-956 is a promising compound-inhibitor of the Ca2+,Mg2+-ATPase of aortal sarcoplasmic reticulum, which may have theoretical and practical significance.
Series on Biomechanics, Vol.40, No. 1 (2026), 67-76
DOI: 10.7546/SB.01.09.2026
Ключови думи: aorta; calix4arenes; Mg2-ATPase; sarcoplasmic reticulum; smooth muscle cells; Са2
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| Дата на публикуване: 2026-03-23
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