Veklich T O
Ukr Biochem J. 2016 Mar-Apr;88(2):5-15. doi: 10.15407/ubj88.02.005.
Our study on the plasma membrane vesicles and myometrium cells treated with 0.1% digitonin showed that inhibitory effect of calix[4]arene C-90 (5,11,17,23-tetra(trifluoro)methyl(phenylsulphonylimino)-methylamino- 25,26,27,28-tetrapropoxy-calix[4]arene) on the plasma membrane Ca2+,Mg2+-ATPase was more significant than on the Ca2+,Mg2+-ATPase in sarcoplasmic reticulum (the inhibition coefficient I0.5 values were 20.2 ± 0.5 μM and 57.0 ± 1.4 μM for the plasma membrane Ca2+,Mg2+-ATPase and Ca2+,Mg2+-ATPase in sarcoplasmic reticulum, respectively (n = 5)). Inhibition kinetics of calix[4]arene C-90 effect on the Ca2+,Mg2+- ATPase activities in plasma membrane and sarcoplasmic reticulum were studied. This substance inhibited both pumps as complete noncompetitive inhibitor. Calix[4]arene C-90 caused the increase of intracellular Ca2+ concentration and decrease of hydrodynamic diameter in smooth muscle cells similar to the action of uterotonic drug oxytocin.
我们对用0.1%洋地黄皂苷处理的质膜囊泡和子宫肌层细胞的研究表明,杯[4]芳烃C-90(5,11,17,23-四(三氟)甲基(苯磺酰亚氨基)-甲基氨基-25,26,27,28-四丙氧基杯[4]芳烃)对质膜Ca2 +,Mg2 + -ATP酶的抑制作用比对肌浆网中Ca2 +,Mg2 + -ATP酶的抑制作用更显著(质膜Ca2 +,Mg2 + -ATP酶和肌浆网中Ca2 +,Mg2 + -ATP酶的抑制系数I0.5值分别为20.2±0.5μM和57.0±1.4μM(n = 5))。研究了杯[4]芳烃C-90对质膜和肌浆网中Ca2 +,Mg2 + -ATP酶活性的抑制动力学。该物质作为完全非竞争性抑制剂抑制两种泵。杯[4]芳烃C-90导致平滑肌细胞内Ca2 +浓度升高和流体动力学直径减小,类似于宫缩剂催产素的作用。