异诺霉素是一种P-糖蛋白功能抑制剂，它与磷脂酰乙醇胺特异性相互作用。
Inostamycin, an inhibitor of P-glycoprotein function, interacts specifically with phosphatidylethanolamine.
作者信息
Kawada M, Umezawa K
机构信息
Department of Applied Chemistry, Faculty of Science and Technology, Keio University, Yokohama.
出版信息
Jpn J Cancer Res. 1995 Sep;86(9):873-8. doi: 10.1111/j.1349-7006.1995.tb03099.x.
The mechanism of inostamycin action was further studied. When multidrug-resistant KB-C4 cells were preincubated with inostamycin for 30 min, the accumulation of [3H]vinblastine was increased for as long as 48 h thereafter. Inostamycin inhibited azidopine binding to P-glycoprotein, even after KB plasma membranes had been preincubated with inostamycin and washed. Carbon 14-labeled inostamycin bound to KB plasma membranes irreversibly, but the binding capacity did not parallel the amount of P-glycoprotein in three KB cell lines. Inostamycin was found to interact specifically with purified phosphatidylethanolamine. These results suggest that inostamycin can inhibit P-glycoprotein irreversibly by binding to plasma membranes irreversibly through phosphatidylethanolamine.
对肌苷霉素的作用机制进行了进一步研究。当多药耐药的KB - C4细胞与肌苷霉素预孵育30分钟后，在此后的长达48小时内，[3H]长春碱的蓄积量增加。即使在KB质膜与肌苷霉素预孵育并洗涤后，肌苷霉素仍能抑制叠氮平与P - 糖蛋白的结合。碳14标记的肌苷霉素不可逆地结合到KB质膜上，但在三种KB细胞系中，其结合能力与P - 糖蛋白的量并不平行。研究发现肌苷霉素能与纯化的磷脂酰乙醇胺特异性相互作用。这些结果表明，肌苷霉素可通过磷脂酰乙醇胺与质膜不可逆结合，从而不可逆地抑制P - 糖蛋白。
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