LONG-LASTING ACCUMULATION OF VINBLASTINE IN INOSTAMYCIN-TREATED MULTIDRUG-RESISTANT KB CELLS

被引：10

作者：

KAWADA, M

UMEZAWA, K

机构：

[1] Department of Applied Chemistry, Faculty of Science and Technology, Keio University, Yokohama, 223, 3-14-1 Hiyoshi, Kohoku-ku

来源：

JAPANESE JOURNAL OF CANCER RESEARCH | 1991年 / 82卷 / 10期

关键词：

KB CELLS; INOSTAMYCIN; MULTIDRUG RESISTANCE;

D O I：

10.1111/j.1349-7006.1991.tb01771.x

中图分类号：

R73 [肿瘤学];

学科分类号：

100214 ;

摘要：

Inostamycin, a novel polyether compound, reverses multidrug resistance in KB cells. The mechanism of its action was studied by use of radioactively labeled vinblastine. Inostamycin dose-dependently increased the accumulation of [H-3]vinblastine in multidrug-resistant KB-C4 cells at 0.5-2-mu-g/ml, while it did not enhance accumulation in the drug-sensitive KB-3-1 cells. At a concentration of 1-mu-g/ml inostamycin inhibited active [H-3]vinblastine efflux from KB-C4 cells, but not from KB-3-1 cells, and inhibited [H-3]vinblastine binding to KB-C4 membranes with an IC50 of 0.94-mu-g/ml (1.3-mu-M). Furthermore, [H-3]vinblastine accumulated by treatment with 1-mu-g/ml of inostamycin was resistant to efflux from KB-C4 cells, even after the removal of inostamycin.

引用

页码：1160 / 1164

页数：5

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