Ogawa M, Gale G R, Meischen S J, Cooke V A
Cancer Res. 1976 Sep;36(9 pt.1):3185-8.
We studied the effects of dinitrato (1,2,-diaminocyclohexane)platinum (NSC 239851) on murine myeloma Adj. PC-5 and hemopoietic precursor cells. The median survival time of tumor-bearing mice was significantly affected by i.p. injections of this agent. While 14 mg/kg was a toxic dose, as little as 2 mg/kg prolonged the survival for over 100 days. When cells from normal marrow and actively regenerating marrows were exposed to the agent in culture tubes, washed, and assayed for the surviving hemopoietic precursors, similar sensitivity curves were observed. This result indicates the absence of cell cycle dependency of the agent. When marrow cells were exposed to NSC 239851 at 4 degrees in culture, almost total abrogation of the cytotoxicity was noted. This observation, unlike that from the experiment with the inorganic platinum congener, cis-diamminedichloroplatinum, suggests that the transport of this agents is an active process.
我们研究了二硝酸根(1,2 - 二氨基环己烷)铂(NSC 239851)对小鼠骨髓瘤Adj.PC - 5和造血前体细胞的影响。腹腔注射该药物显著影响荷瘤小鼠的中位生存时间。14mg/kg是毒性剂量,而低至2mg/kg就能使生存期延长超过100天。当将来自正常骨髓和正在积极再生的骨髓的细胞置于培养管中,暴露于该药物,洗涤后检测存活的造血前体细胞时,观察到了相似的敏感性曲线。这一结果表明该药物不存在细胞周期依赖性。当骨髓细胞在培养中于4℃暴露于NSC 239851时,观察到细胞毒性几乎完全消除。与无机铂同类物顺二氨二氯铂的实验结果不同,这一观察结果表明该药物的转运是一个主动过程。