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Information × Registration Number 0214U002197, 0113U007570 , R & D reports Title The effect properties of calixarenes relative to plasma membrane ATP-hydrolysing ion-transporting systems of smooth muscles. popup.stage_title Head Shkrabak Alexandr, Registration Date 24-01-2014 Organization A.V.Palladin Institute of Biochemistry of National Academy of Sciences popup.description2 The aim of the investigation is to research the mechanisms of calixarene inhibitory action on ion-transporting ATP-hydrolysing systems of myocytes plasma membrane. We have shown that number of phenylsulfonylamidine groups on the upper rim of calixarene is crucial for inhibition of plasma membrane Ca2+,Mg2+-ATPase activity by calixarens. Namely, four described groups of calixarene C-90 are the reason of more efficient inhibition of Ca2+,Mg2+-ATPase activity, comparing to calixarenes C-176, C-772, which posses only two residue of phenylsulfonylamidine groups. Moreover, phenylsulfonylamidine groups location on the calixarene upper rim also effects on inhibition properties of calixarenes relative to Ca2+,Mg2+-ATPase activity. The inhibition efficiency of calixarene C-716 with phenylsulfonylamidine groups positioned on opposite phenyl residue is higher than the same of calixarene C-772 with phenylsulfonylamidine groups located on nearby phenyl residue. Calixarenes C-107 and C-90 decrease maximal fluorescence level of ANS probe without any influence on binding constant of mentioned probe with membrane fraction of myocytes plasma membrane. That is the evidence of change of liquid-crystal membrane state induced by mentioned calixarenes and also ability of calixarenes C-90 and C-107 to build in lipid bilayer of membrane and to interact with transmembrane domains of integral proteins, such as Ca2+,Mg2+-ATPase and Na+,K+-ATPase. Thus, our results may be useful for creation of efficient inhibitors of Ca2+,Mg2+-ATPase and Na+,K+-ATPase on the basis of calixarene C-90 and C-107 respectively. These inhibitors will highly matter in the investigation of membrane mechanism of cation exchange in smooth muscle, particularly in study of plasma membrane role in providing electromechanical coupling, as well as in regulation of ion homeostasis in smooth muscle cells. Also calixarene C-107 and C-90 are perspective for creation of pharmacological drug on their foundation which can modulate pointed enzyme activities and corresponding physiological functions in case of pathological conditions. Product Description popup.authors Мазур Юлія Юріївна popup.nrat_date 2020-04-02 Close