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首页> 外文期刊>Life sciences >Selective inhibition of human erythrocyte Na+/K+ ATPase by cardiac glycosides and by a mammalian digitalis like factor
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Selective inhibition of human erythrocyte Na+/K+ ATPase by cardiac glycosides and by a mammalian digitalis like factor

机译：强心苷和哺乳动物洋地黄样因子对人红细胞Na + / K + ATPase的选择性抑制

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摘要

Na+/K(+)ATPase is a transport membrane protein which contains the functional receptor for digitalis compounds, In this work we compare the inhibition curves of Na+/K(+)ATPase measured by the inhibition of Rb-86 uptake in human red blood cells by cardiac glycosides and by an endogenous digitalis like factor (EDLF) extracted from human newborn cord blood. The curves of Na+/K(+)TPase inhibition show a monophasic shape for ouabain, strophantidin, digitoxin, proscillaridin and EDLF whereas a biphasic shape for ouabagenin, digoxin, digoxigenin and digitoxigenin. All the drugs are potent inhibitors of erythrocyte Na+/K(+)ATPase with an IC50 ranging from 1.8x10(-9)M to 1.4x10(-11)M for the higher affinity binding site and from 1.8X10(-6)M to 5.5X10(-9)M for the lower affinity site. Digitoxigenin is the most active showing the higher active site at 1.4X10(-11)M. Ouabain and digoxin have higher affinity compared with their corresponding genins, while digitoxigenin shows a binding site with higher affinity than the respective cardiac glycosides, The increased affinity of the drugs to Na+/K(+)ATPase may be related to a lipophilic region in correspondence of the carbons 10, 9, 11, 12, 13 of the steroid nucleus, situated in the opposite side with respect of the C-OH-14. The comparison of the inhibition curves and the HPLC profile of newborn EDLF and of the investigated cardenolides suggest that EDLF may be a compound identical or very similar to ouabain. (C) 2000 Elsevier Science Inc. All rights reserved. [References: 21]
机译：Na + / K（+）ATPase是一种转运膜蛋白，包含洋地黄类化合物的功能性受体，在这项工作中，我们比较了通过抑制人红血球中Rb-86摄入量测得的Na + / K（+）ATPase的抑制曲线从人新生儿脐带血中提取的强心苷和内源性洋地黄样因子（EDLF） Na + / K（+）TPase抑制曲线显示，哇巴因，链霉抗生物素，洋地黄毒苷，前螺旋体和EDLF呈单相形状，而哇巴因，地高辛，洋地黄毒苷和洋地黄毒苷则呈双相形状。所有这些药物都是红细胞Na + / K（+）ATPase的有效抑制剂，IC50范围从1.8x10（-9）M到1.4x10（-11）M（对于更高的亲和力结合位点）和1.8X10（-6）M较低亲和力位点为5.5X10（-9）M。 Digitoxigenin是最活跃的，在1.4X10（-11）M处显示较高的活性位点。瓦巴因和地高辛与其相应的genins相比具有更高的亲和力，而洋地黄毒苷显示的结合位点比相应的强心苷具有更高的亲和力。相应地，药物对Na + / K（+）ATPase的亲和力增加可能与亲脂性区域有关。类固醇核的碳原子10、9、11、12、13中的一部分位于相对于C-OH-14的相对侧。新生儿EDLF和所研究的烯属内酯的抑制曲线和HPLC谱的比较表明，EDLF可能是与哇巴因相同或非常相似的化合物。 （C）2000 Elsevier Science Inc.保留所有权利。 [参考：21]

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