Colacicco G, Basu M K
J Pharm Sci. 1980 Apr;69(4):406-9. doi: 10.1002/jps.2600690411.
When spread from organic solvents onto electrolyte solutions, the Ca2+ ionophores A23187 (I) and X537A (II) formed films with relatively high surface pressures potentials. Ionophores I had collapse pressures between 16 and 19 dynes/cm and nearly equal surface activity on distilled water and on 1000 mEq of either sodium chloride or calcium chloride. Film pressure did not reveal appreciable ion selectivity. However, the surface potential of I on calcium chloride solution was higher than that on sodium chloride, and the potential difference, delta(deltaV), of 40 mv was independent of the electrolyte concentration. In contrast, the ion selectivity of II was dependent on the electrolyte concentrations since the delta(deltaV) value between calcium chloride and sodium chloride was maximal (130 mv) on 1000 mEq and negligible on 500- and 2000-mEq salt solutions. The isotherms of phospholipid-ionophore films were markedly different from those of the individual components, although they revealed ionophore characteristics at low film pressures and phospholipid behavior at high film pressures. The magnitude of the surface potential indicated that dipalmitoyl phosphatidylcholine enhanced, whereas mitochondrial lipid and cardiolipin reduced, the preference of the two ionophores for Ca2+ over Na+. Since the ion selectivity was manifested most at both high electrolyte and high lecithin concentrations, the ionophore probably prefers the low dielectric constant of neutral lipid membranes to complex with the selected cation.
当从有机溶剂铺展到电解质溶液上时,钙离子载体A23187(I)和X537A(II)形成具有相对较高表面压力电位的膜。离子载体I的崩溃压力在16至19达因/厘米之间,在蒸馏水以及1000毫当量的氯化钠或氯化钙溶液上具有几乎相等的表面活性。膜压力未显示出明显的离子选择性。然而,离子载体I在氯化钙溶液上的表面电位高于在氯化钠溶液上的表面电位,且40毫伏的电位差(δ(δV))与电解质浓度无关。相比之下,离子载体II的离子选择性取决于电解质浓度,因为在1000毫当量时,氯化钙和氯化钠之间的δ(δV)值最大(130毫伏),而在500毫当量和2000毫当量的盐溶液上可忽略不计。磷脂 - 离子载体膜的等温线与各单独组分的等温线明显不同,尽管它们在低膜压力下显示出离子载体特征,在高膜压力下显示出磷脂行为。表面电位的大小表明,二棕榈酰磷脂酰胆碱增强了两种离子载体对Ca2 +相对于Na +的偏好,而线粒体脂质和心磷脂则降低了这种偏好。由于离子选择性在高电解质浓度和高卵磷脂浓度下都最为明显,离子载体可能更倾向于中性脂质膜的低介电常数以与所选阳离子形成复合物。