Hill D L, Montgomery J A
Cancer Chemother Pharmacol. 1980;4(4):221-5. doi: 10.1007/BF00255265.
Considerable evidence has been accumulated to demonstrate that sensitive tumor cells in experimental animals take up and retain at least some effective anticancer drugs to a greater extent than normal tissues, thus providing a greater degree of exposure and accounting for the selective effect of the drugs. In sensitive cells, DNA synthesis is inhibited for prolonged periods, whereas in cells less sensitive the time of inhibition is shorter. In those cases examined where a metabolite, formed intracellularly, is the active form of the agent, the metabolite is produced and is retained to a greater extent than in normal tissues.
已有大量证据表明,实验动物体内的敏感肿瘤细胞比正常组织摄取并保留至少一些有效抗癌药物的程度更高,从而提供了更高程度的暴露,并解释了药物的选择性作用。在敏感细胞中,DNA合成会被长时间抑制,而在不太敏感的细胞中,抑制时间较短。在那些经检测细胞内形成的代谢物为药物活性形式的情况下,该代谢物的产生和保留程度均高于正常组织。