Paulson J C, McClure W O
J Cell Biol. 1975 Nov;67(2PT.1):461-7. doi: 10.1083/jcb.67.2.461.
Pharmacological evidence is presented for the involvement of microtubules in the process of fast axoplasmic transport. A quantitative measure of the inhibition of axoplasmic transport in an in vitro preparation of rat sciatic nerve is described. The alkaloids colchicine, podophyllotoxin, and vinblastine, which are known both to disrupt microtubules and to bind to the protein subunit of microtubules, are inhibitors of axoplasmic transport. Lumicolchine and picropodophyllin, unlike their respective isomers colchicine and podophyllotoxin, are poor inhibitors of axoplasmic transport. The dissociation constants for the binding of colchicine, lumicolchicine, podophyllotoxin, and picropodophyllin to purified microtubule protein from rat brain have been measured. Inhibition of axoplasmic transport by these drugs correlates favorably with their affinities of microtubule protein.
有药理学证据表明微管参与快速轴浆运输过程。本文描述了一种对大鼠坐骨神经体外制备物中轴浆运输抑制作用的定量测量方法。生物碱秋水仙碱、鬼臼毒素和长春碱,已知它们既能破坏微管又能与微管的蛋白质亚基结合,是轴浆运输的抑制剂。光秋水仙碱和苦鬼臼脂素,与其各自的异构体秋水仙碱和鬼臼毒素不同,是轴浆运输的弱抑制剂。已测量了秋水仙碱、光秋水仙碱、鬼臼毒素和苦鬼臼脂素与从大鼠脑中纯化的微管蛋白结合的解离常数。这些药物对轴浆运输的抑制作用与其对微管蛋白的亲和力密切相关。