链芳烃磺酰基胺对质膜Сa(2+),Mg(2+)-АТРase的抑制作用。结构与活性关系

O. A. Shkrabak, T. O. Veklich, R. Rodik, V. Kalchenko, S. Kosterin
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引用次数: 1

摘要

之前我们已经证明,四磺酰酰胺二羧基arene C-90选择性地抑制平滑肌细胞的质膜Са2+,Mg2+-АТРаse对质膜其他atp酶的抑制作用。为了增强杯芳烃的抑制作用,合成了几种结构类似杯芳烃C-90的烷氧基杯芳烃磺酰基胺,并检测了它们对上述酶活性的影响,以及离体平滑肌细胞的细胞质Ca2+浓度水平和水动力直径。结果表明,磺胺基对Са2+、Mg2+-АТРаse的抑制作用至关重要,抑制效果取决于它们在杯芳烃大环上缘的数量和空间取向。上环引入苯基或叔丁基,下环引入长烷基链,抑制效率仅略有提高。杯芳烃对Са2+、Mg2+-АТРаse的抑制作用与细胞内Ca2+浓度和平滑肌细胞水动力直径的影响相关。所获得的结果对于创建更有效和选择性的质膜抑制剂Са2+,Mg2+-АТРаse作为平滑肌收缩性的调节剂具有重要意义。关键词:杯脲磺酰胺,胞内Ca(2+)浓度,质膜Са(2+), Mg(2+)-АТРаse,平滑肌
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Inhibition of plasma membrane Сa(2+),Mg(2+)-АТРase by сalixarene sulfonylamidines. Structure-activity relationship
Previously we have already shown that tetrasulfonylamidinecalixarene C-90 inhibited plasma membrane Са2+,Mg2+-АТРаse of smooth muscle cells selectively to other ATPases of plasma membrane. To inhance the inhibitory effect of calixarenes several alkoxycalixarene sulfonylamidines structurally similar to calixa­rene C-90 were synthesized and their effects on the mentioned enzyme activity, the level of cytoplasmic Ca2+ concentration and hydrodynamic diameter of isolated smooth muscle cells were checked. It was shown that sulfonylamidino groups are crucial for Са2+,Mg2+-АТРаse inhibition, the efficiency of inhibition depends on their quantity and spatial orientation at the upper rim of calixarene macrocycle. Introduction of phenyl or tert-butyl groups into the upper rim and of long alkyl chains into the lower rim led to only slightl increase of inhibition efficiency. The inhibitory effect of studied calixarenes on Са2+,Mg2+-АТРаse correlated with effects on cytosolic Ca2+ concentration and hydrodynamic diameter of smooth muscle cells. The obtained results are important for creation of more effective and selective inhibitors of plasma membrane Са2+,Mg2+-АТРаse as regulators of smooth muscle contractility. Keywords: calixa­rene sulfonylamidines, intracellular Ca(2+) concentration, plasma membrane Са(2+);Mg(2+)-АТРаse, smooth muscle
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