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Information × Registration Number 0223U001055, 0122U002052 , R & D reports Title The use of calix[4]arens as selective and affine modulators of transport activity of membrane vector electroenzymes in order to regulate the contraction - relaxation of smooth muscles popup.stage_title Head Kosterin Serhii O., д.б.н. Registration Date 25-01-2023 Organization Palladin Institute of Biochemistry of the National Academy of Sciences of Ukraine popup.description2 In accordance with the goal of the Project, new results were obtained regarding the study of the effect of calix[4]arenes on myometrial cells. This cycle of research is traditionally carried out in close creative cooperation of the employees of the Dep. of Muscle Biochemistry of the Palladin Inst. of Biochemistry of the NAS of Ukraine (Acad. of the NAS of Ukraine, Prof. S.O.Kosterin) with colleagues from the Department of Macrocyclic Compound Chemistry of the Inst. of Organic Chemistry of the NAS of Ukraine (Acad. of the NAS of Ukraine, Prof. V.I.Kalchenko). Thus, it was shown that thiacalix[4]arene C-1087 (5,11,17,23-tetra(trifluoro)methyl(phenylsulfonylimino)methylamino-25,27-dihexyloxy-26,28-dihydroxythiacalix[4]arene) at a concentration of 100µM, exerts the most significant inhibitory effect on Ca2+,Mg2+-ATPase activity in the plasma membrane of myometrial cells compared to other analogues of C-90 calix[4]arene, and practically does not affect the specific activity of other membrane ATPases. The calculated value of the inhibition coefficient I0.5 is 9.4±0.6µM, the value of the Hill coefficient nH is 0.58±0.03(M±m; n=5). With the help of confocal microscopy using the Ca2+-sensitive fluorescent probe fluo-4, it was shown that the application of thiacalyx[4]arene C-1087 to immobilized uterine myocytes leads to an increase in the intracellular concentration of Ca ions. Sulfur-containing calix[4]arene C-1193 inhibits Ca2+ accumulation, FADH2 oxidation, and nitric oxide synthesis in uterine smooth muscle mitochondria. Sulfur-containing calix[4]arene C-1192 at a concentration of 10μM increases the hydrodynamic diameter of rat myometrial mitochondria. Incubation of digitonin-perforated rat myometrial cells with 1μM C-1191 or 1μM C-1192 increases TMRM fluorescence intensity compared to control, indicating hyperpolarization of mitochondrial membranes. 1μM calix[4]arene C-1191 and C-1192 do not affect the concentration of ionized Ca in the matrix of myometrial mitochondria Product Description popup.authors Babich Lidiya Grygorivna Veklich Tetiana Oleksiivna Danylovych Hanna Victorivna Danylovuch Yuriy Volodymyrosych Karakhim Sergii O Chunikhin Oleksandr Yu. Shlykov Serhiy Georgiyovich popup.nrat_date 2023-01-25 Close