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An analysis of the mechanism by which cetiedil inhibits sickling.

机译:cetiedil抑制镰状化的机制分析。

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A study has been carried out into the effects of cetiedil on the activities of Na+, K+ and Ca2+, Mg2+-ATPases of the normal human erythrocyte membrane. In general, cetiedil inhibits both ATPases activities but with characteristic inhibition profiles and varying degrees of efficacy. The activities were inhibited non-competitively at the cetiedil concentration which caused 50% inhibition of each enzyme. In addition, the effects of cetiedil on the transport of K+ and phosphate ions across the membrane were monitored and compared. Cetiedil was found to stimulate K+ release and to inhibit phosphate uptake. At low concentrations, both processes were concentration dependent. Stimulation of K+ efflux reached a plateau at a concentration of 1.2 mM. The antisickling effect of cetiedil is explained mainly in the light of the changes it induces in the activities of membrane-bound ATPases and the permeability properties of the erythrocyte membrane to cations and anions.
机译:cetiedil对正常人红细胞膜Na +,K +和Ca2 +,Mg2 + -ATPase活性的影响已进行了研究。通常,cetiedil抑制两种ATPase活性,但具有特征性的抑制曲线和不同程度的功效。在cetiedil浓度下,该活性被非竞争性地抑制,这导致每种酶的50%抑制。此外,监测并比较了cetiedil对跨膜转运K +和磷酸根离子的影响。发现Cetiedil可刺激K +释放并抑制磷酸盐吸收。在低浓度下,两个过程均取决于浓度。 K +外排的刺激在1.2mM的浓度达到平稳。 cetiedil的抗病菌作用主要是根据其对膜结合ATPase活性的诱导以及红细胞膜对阳离子和阴离子的渗透性的变化来解释的。

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