Genna J M, Coffe G, Pudles J
Eur J Biochem. 1980 Sep;110(2):457-64. doi: 10.1111/j.1432-1033.1980.tb04887.x.
From kinetic and electron microscopy studies on the effects of procaine, tetracaine and dibucaine on the polymerization and depolymerization of the microtubules isolated from pig and rat brains the following results were obtained. 1. Procaine or tetracaine, at the concentration range of 0.5--20 mM and of 0.5--5 mM respectively, increases the rate of tubulin polymerization (24 degrees C or 37 degrees C) and of microtubule depolymerization (4 degrees C) as a linear function of the concentration of the anesthetics, while identical amounts of microtubules are formed. In the absence of microtubule-associated proteins the polymerization of tubulin is not induced by 10 mM procaine, furthermore, the critical concentration of microtubule proteins necessary for assembly into microtubules is not affected at this concentration level of the anesthetic. This suggests that procaine affects not the nucleation, but rather the elongation process. 2. Dibucaine, from 0.5 mM to 3 mM increases the lag time of the polymerization reaction, while from 0.5 mM to 2 mM it linearly decreases both tubulin polymerization (24 degrees C) and microtubule depolymerization (4 degrees C) rates. Dibucaine, up to mM concentration, does not affect the extent of tubulin polymerization; however, above this concentration it induces the formation of amorphous aggregates. 3. Procaine or tetracaine enhances the depolymerizing effect of calcium on microtubules. The half-maximal values for the depolymerizing effect of calcium were 0.96, 0.71 and 0.51 mM for the control, in the presence of 10 mM procaine and 5 mM tetracaine respectively.
通过对普鲁卡因、丁卡因和布比卡因对从猪脑和大鼠脑分离出的微管聚合和解聚作用的动力学及电子显微镜研究，得到了以下结果。1. 普鲁卡因或丁卡因，浓度范围分别为0.5 - 20 mM和0.5 - 5 mM时，可增加微管蛋白聚合速率（24℃或37℃）以及微管解聚速率（4℃），且与麻醉剂浓度呈线性关系，同时形成的微管量相同。在没有微管相关蛋白的情况下，10 mM普鲁卡因不会诱导微管蛋白聚合，此外，在此麻醉剂浓度水平下，组装成微管所需的微管蛋白临界浓度不受影响。这表明普鲁卡因影响的不是成核过程，而是延长过程。2. 布比卡因，浓度从0.5 mM到3 mM会增加聚合反应的延迟时间，而从0.5 mM到2 mM会使微管蛋白聚合速率（24℃）和微管解聚速率（4℃）呈线性下降。布比卡因在达到mM浓度之前，不影响微管蛋白聚合程度；然而，高于此浓度会诱导无定形聚集体的形成。3. 普鲁卡因或丁卡因增强了钙对微管的解聚作用。钙解聚作用的半数最大值，对照组为0.96 mM，在存在10 mM普鲁卡因和5 mM丁卡因时分别为0.71 mM和0.51 mM。
