Fernandez H L, Duell M J
J Neurochem. 1980 Nov;35(5):1166-71. doi: 10.1111/j.1471-4159.1980.tb07872.x.
The effects of certain protease inhibitors on end-plate acetylcholinesterase (AChE) activity, as well as on wet weight and total protein, were studied in vivo in intact and denervated anterior gracilis muscles from the rat. A combination of leupeptin, pepstatin, and aprotinin, administered intraarterially, partly prevented the early (24 h) denervation-induced decrease in muscle weight and protein content. In turn, leupeptin and aprotinin, either alone or in combination, markedly reduced the decay of AChE activity in the denervated muscles, whereas pepstatin alone was ineffective. Such effects were additive in that the inhibitors in combination were more effective than when they were used separately. Additional experiments indicated that none of the inhibitors, at the concentrations used, affected AChE activity directly, nor did they have a significant effect during processing of the muscle samples. These findings indicate that the initial decay of AChE activity with denervation was effectively reduced by the inhibitors, probably through inactivation of proteolytic enzymes which, otherwise, would be increase in denervated muscle.
在大鼠完整和去神经支配的股薄肌中，研究了某些蛋白酶抑制剂对终板乙酰胆碱酯酶（AChE）活性以及湿重和总蛋白的影响。动脉内给予亮抑酶肽、胃蛋白酶抑制剂和抑肽酶的组合，部分预防了早期（24小时）去神经支配引起的肌肉重量和蛋白质含量的下降。相应地，亮抑酶肽和抑肽酶单独或联合使用，均显著降低了去神经支配肌肉中AChE活性的衰减，而单独使用胃蛋白酶抑制剂则无效。这些作用是相加的，即抑制剂联合使用比单独使用更有效。额外的实验表明，在所使用的浓度下，没有一种抑制剂直接影响AChE活性，在肌肉样本处理过程中它们也没有显著影响。这些发现表明，抑制剂有效地减少了去神经支配时AChE活性的初始衰减，可能是通过使蛋白水解酶失活，否则这些酶在去神经支配的肌肉中会增加。
