...
  • 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Ukrainian Biochemical Journal >Inhibition of Na(+),K(+)-ATPase and activation of myosin ATPase by calix[4]arene C-107 cause stimulation of isolated smooth muscle contractile activity
【24h】

Inhibition of Na(+),K(+)-ATPase and activation of myosin ATPase by calix[4]arene C-107 cause stimulation of isolated smooth muscle contractile activity

机译：抑制Na（+），K（+） - ATP酶和CALIX的肌蛋白ATP酶活化[4]芳烃C-107原因刺激分离的平滑肌收缩活动

获取原文
           
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

The discovery of compounds that might modify myometrial contractility is an important area of researches. In our previous experiments, we found that some representatives of macrocyclic compounds family – calix[4]arenes – can modify the enzymatic and transport activity of membrane-bound cation-transport ATP hydrolases. The aim of this work was to study and compare the effect of calix[4]arene C-107 on the enzymatic activities of Mgsup2+/sup-dependent ATPases of the uterine smooth muscle, namely: ouabain-sensitive Nasup+/sup,Ksup+/sup-ATPase, plasma membrane Casup2+/sup-independent “basal” Mgsup2+/sup-ATPase, ATPase of the actomyosin complex and myosin subfragment-1, with effect on the contractile activity of the myometrium. It was shown that calix[4]arene C-107 efficiently inhibited myometrium Nasup+/sup,Ksup+/sup-ATPase (Isub50/sub = 54 ± 6 nM) selectively to other ATP-hydrolases of the plasma membrane and simultaneously activated the enzymatic activity of the myosin ATPase of smooth muscles (Asub50/sub = 9.6 ± 0.7 μM). Such reciprocal biochemical effects led to the stimulation of the smooth muscle contractile activity that was demonstrated by the tensometric method using different isolated smooth muscles. Calix[4]arene С-107 was shown to stimulate the increase of the tonic component of myometrium contractions induced by oxytocin, as well as contractions of the caecum muscles induced by high-potassium solution or acetylcholine, and to maintain increased tension for a long time. Thus, calix[4]arene C-107 is a prospective compound for enhancing the smooth muscle basal tone and/or contraction in case of hypotonic dysfunctions.
机译：发现可能改变肌瘤收缩力的化合物是一个重要的研究领域。在我们以前的实验中，我们发现一些宏环化合物家族的代表 - Calix [4] arenes - 可以改变膜结合阳离子转运ATP水解酶的酶促和运输活性。这项工作的目的是研究和比较Calix [4]芳烃C-107对子宫平滑肌的Mg 2 + - 依赖性ATP酶的酶活性的影响，即：威达曼敏感na + / sup>，k + -atpase，血浆膜ca 2 + - 依赖性“基底”mg 2 + - Atpase，Atpase，Atpase actomyosin复合物和肌球蛋白次蛋白-1，对肌瘤的收缩活性作用。结果表明，COLIX [4]芳烃C-107有效地抑制肌瘤NA + ，k + -Atpase（i 50 = 54±6 NM）选择性地致质子膜的其他ATP水解酶，同时活化光滑肌肉（A 50 = 9.6±0.7μm）的肌蛋白ATP酶的酶活性。这种往复生物化学效应导致刺激平滑肌收缩活动，这些肌肉收缩活性由使用不同隔离的平滑肌的张量法证明。显示CALIX [4]芳烃С-107刺激催产素诱导的肌瘤收缩的滋补成分的增加，以及由高钾溶液或乙酰胆碱诱导的盲肠肌肉的收缩，并保持较长的张力时间。因此，Calix [4]芳烃C-107是用于增强低渗功能障碍的平滑肌基调和/或收缩的前瞻性化合物。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号