Chetty C S, Cooper A, McNeil C, Rajanna B
Division of Natural Sciences, Selma University, Alabama 36701.
Arch Environ Contam Toxicol. 1992 May;22(4):456-8. doi: 10.1007/BF00212567.
Cadmium (Cd) inhibited the activities of Na(+)-K+ ATPase (IC50 = 5.0 x 10(-5) M), K(+)-p-nitrophenyl phosphatase (PNPPase) (IC50 = 4.0 x 10(-5) M) and 3H-ouabain binding (IC50 = 7.5 x 10(-5) M) in rat brain microsomes. Monothiols (cysteine but not glutathione and D-penicillamine) and dithiols (dimercaprol, dimercaptosuccinic acid and dithiothreitol) offered varied levels of protection against Cd-inhibition of Na(+)-K+ ATPase. Protection of Na(+)-K+ ATPase by these sulfhydryl (SH) agents was higher at 7.5 as compared to 8.5 pH. The present data suggest that Cd-inhibited Na(+)-K+ ATPase, by interfering with phosphorylation of enzyme molecule and dephosphorylation of the enzyme-phosphoryl complex and exerts a similar effect to that of SH-blocking agents.
镉(Cd)抑制大鼠脑微粒体中钠钾ATP酶(IC50 = 5.0×10⁻⁵ M)、钾对硝基苯磷酸酶(PNPPase)(IC50 = 4.0×10⁻⁵ M)的活性以及³H-哇巴因结合(IC50 = 7.5×10⁻⁵ M)。单硫醇(半胱氨酸而非谷胱甘肽和D-青霉胺)和二硫醇(二巯丙醇、二巯基琥珀酸和二硫苏糖醇)对镉抑制钠钾ATP酶提供了不同程度的保护。与pH 8.5相比,这些巯基(SH)试剂在pH 7.5时对钠钾ATP酶的保护作用更高。目前的数据表明,镉通过干扰酶分子的磷酸化和酶-磷酰复合物的去磷酸化来抑制钠钾ATP酶,并发挥与SH阻断剂类似的作用。