Maenz D D, Forsyth G W
J Membr Biol. 1982;70(2):125-33. doi: 10.1007/BF01870222.
The intestinal secretagogues ricinoleate and deoxycholate have been tested for a capacity to form complexes with Ca2+ ions and to affect the passive equilibration of Ca2+ ions across the jejunal brush border membrane. Both of these agents formed butanol-soluble Ca2+ complexes in a model phase distribution system. They also promote the passive uptake and efflux of Ca2+ across brush border vesicles in a concentration-dependent manner. The levels of ricinoleate and deoxycholate that increase the rate of transvesicular Ca2+ movement are in the 100 to 300 microM range. Concentrations as high as 1.0 mM had no significant detergent effects in vesicles as measured by release of entrapped sorbitol. The kinetics of Ca2+ uptake and efflux are similar in brush border vesicles treated with A23187, ricinoleate, or deoxycholate. The influx rates observed in this study were high enough to cause the collapse of a Ca2+ gradient, which had been generated by Ca--Mg ATPase enzyme activity in the brush border membrane. Ricinoleate did not affect Ca--Mg ATPase activity at concentrations used in this study, but deoxycholate was inhibitory, indicating two potential modes for elevation of intracellular Ca2+ content by deoxycholate. When compared with the effects of the Ca2+ ionophore, A23187, it appears that both ricinoleate and deoxycholate could have significant intestinal secretory activity due to this Ca2+ ionophore property. It is also noteworthy that, at least in this model system, potential secretory effects are expressed at concentrations significantly below levels that have been associated with detergent effects or altered epithelial morphology.
已对肠道促分泌剂蓖麻油酸酯和脱氧胆酸盐进行了测试,以检测它们与Ca2+离子形成复合物的能力,以及对Ca2+离子穿过空肠刷状缘膜的被动平衡的影响。在模型相分布系统中,这两种试剂均形成了可溶于丁醇的Ca2+复合物。它们还以浓度依赖的方式促进Ca2+穿过刷状缘小泡的被动摄取和流出。增加跨小泡Ca2+移动速率的蓖麻油酸酯和脱氧胆酸盐水平在100至300微摩尔范围内。通过被困山梨醇的释放测量,高达1.0毫摩尔的浓度对小泡没有明显的去污剂作用。在用A23187、蓖麻油酸酯或脱氧胆酸盐处理的刷状缘小泡中,Ca2+摄取和流出的动力学相似。本研究中观察到的流入速率高到足以导致由刷状缘膜中的Ca - Mg ATP酶活性产生的Ca2+梯度崩溃。在本研究中使用的浓度下,蓖麻油酸酯不影响Ca - Mg ATP酶活性,但脱氧胆酸盐具有抑制作用,这表明脱氧胆酸盐提高细胞内Ca2+含量有两种潜在模式。与Ca2+离子载体A23187的作用相比,由于这种Ca2+离子载体特性,蓖麻油酸酯和脱氧胆酸盐似乎都可能具有显著的肠道分泌活性。还值得注意的是,至少在这个模型系统中,潜在的分泌作用在浓度显著低于与去污剂作用或上皮形态改变相关的水平时就会表现出来。