[Comparative studies on anti-tumor effects of nitrosoureas, ACNU and MCNU, on experimental brain tumors (author's transl)].
[Comparative studies on anti-tumor effects of nitrosoureas, ACNU and MCNU, on experimental brain tumors (author's transl)].
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[亚硝基脲、ACNU和MCNU对实验性脑肿瘤抗肿瘤作用的比较研究（作者译）]。
DOI：
10.2176/nmc.21.1017
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发表时间：
1981
影响因子：
1.9
通讯作者：
T. Uozumi
中科院分区：
文献类型：
--
作者：
K. Harada;K. Kiya;H. Okamoto;T. Uozumi
比较了ACNU和MCNU对20-甲基胆蒽诱发的C57黑鼠恶性胶质瘤(MG-细胞)和大鼠神经胶质瘤(C6-细胞)的体内外抗肿瘤作用。ACNU和MCNU的体外抑制作用具有剂量和时间依赖性。抑制作用浓度大于10μg/ml，阿昔洛韦的抑制作用略强于甲硝唑。当浓度大于10μg/ml时，ACNU对DNA合成有明显抑制作用，但对蛋白质和核糖核酸合成无明显影响。MCNU对DNA合成的抑制作用与ACNU相似，但小于ACNU。在第5天一次给药，阿糖胞苷和甲硝唑组小鼠的寿命(ILS)分别增加了120.3%和100.4%。两种药物的最佳剂量均为25 mg/kg/d。ACNU和MCNU的治疗比分别为4.17和6.67。在第5天给予ACNU 25 mg/kg/天，10只小鼠中有2只存活超过60天。在MCNU的情况下，十分之一的小鼠存活下来。与间歇给药相比，单次给药ACNU或MCNU在延长寿命方面更有效。这些结果表明，新的水溶性亚硝脲MCNU可以作为脑肿瘤的化疗药物，与ACNU一样。
Comparative anti-tumor effects of ACNU and MCNU were studied on 20-methylcholanthrene-induced C57 black mouse malignant gliomas (MG-cells) and rat glial tumors (C6-cells) in vitro and in vivo. The inhibitory effects of ACNU and MCNU in vitro were dependent on dose and time. The concentration showing inhibitory effect was more than 10 μg/ml. ACNU was a slightly more effective than MCNU. ACNU significantly inhibited DNA synthesis at concentrations higher than 10 μg/ml, but had no such effect on RNA and protein syntheses. MCNU also inhibited DNA synthesis similar to but less than that of ACNU. By a single intraperitoneal administration on day 5, an increased life span (ILS) was observed with ACNU (120.3 % increase) and with MCNU (100.4%). The optimal dosis was 25 mg/kg/day for both drugs. The therapeutic ratio, or optimal dose divided by the dose producing an increased life span of 30% over controls, of ACNU was 4.17 and that of MCNU was 6.67. When 25 mg/kg/day of ACNU was administered intraperitoneally on day 5, two out of 10 mice survived over 60 days. In case of MCNU, one out of 10 mice survived. A single administration of ACNU or MCNU was more effective for the increased life span compared with intermittent administration. From these results, it is suggested that the new water soluble nitrosourea, MCNU, can be utilized as a chemotherapeutic agent against brain tumors as in the case of ACNU.