Veklich T O, Shkrabak O A, Cherenok S O, Kal'chenko V I, Kosterin S O
Ukr Biokhim Zh (1999). 2012 Nov-Dec;84(6):49-57.
The aim of our investigation was to determine structural features of calix[4]arene C-99 which are important for its inhibition properties relative to Na+,K(+)-ATPase of uterus myocite plasma membrane. Therefore we studied the effect of calix[4]arenes C-296, C-297, C-424, C-425, C-426, C-427, which are structurally similar to this inhibitor, on the mentioned enzyme activity. We have shown that calixarenes C-296 and C-297 which have two additional propoxy groups on the lower rim of macrocycle are less effective inhibitors of Na+,K(+)-ATPase relative to calixarene C-99. Calixarenes C-425 and C-427 which have on the upper rim of macrocycle three and four phosponic residues, respectively, also inhibit Na+,K(+)-ATPase activity less effectively as compared to calixarene C-99. Both calixarenes: C-424, which has only two carbonate residues on the upper rim, and C-426, which has on the upper rim ketomethilphosphonate residues instead of hydroxymethilphosphonate residues of calixarene C-99, do not affect Na+,K(+)-ATPase activity. We have made respective conclusions concerning the role of certain chemical groups of calixarene C-99 during its interaction with Na+,K(+)-ATPase.
我们研究的目的是确定杯[4]芳烃C - 99的结构特征,这些特征对于其对子宫肌细胞质膜Na +,K(+)-ATP酶的抑制特性很重要。因此,我们研究了结构与该抑制剂相似的杯[4]芳烃C - 296、C - 297、C - 424、C - 425、C - 426、C - 427对上述酶活性的影响。我们已经表明,相对于杯芳烃C - 99,在大环下缘有两个额外丙氧基的杯芳烃C - 296和C - 297是效果较差的Na +,K(+)-ATP酶抑制剂。在大环上缘分别有三个和四个膦酸残基的杯芳烃C - 425和C - 427,与杯芳烃C - 99相比,对Na +,K(+)-ATP酶活性的抑制效果也较差。两种杯芳烃:在上缘只有两个碳酸残基的C - 424,以及在上缘有酮甲基膦酸酯残基而非杯芳烃C - 99的羟甲基膦酸酯残基的C - 426,均不影响Na +,K(+)-ATP酶活性。我们已经就杯芳烃C - 99的某些化学基团在其与Na +,K(+)-ATP酶相互作用过程中的作用得出了相应结论。