Alberts D S, Van Daalen Wetters T
Br J Cancer. 1976 Jul;34(1):64-8. doi: 10.1038/bjc.1976.123.
Rubidazone, the new semi-synthetic benzol hydrazone hydrochloride derivative of dauorubicin, has proved on a molecular weight basis to be less toxic than adriamycin and similar to daunorubicin in cardiac toxicity studies in the hamster as well as in other in vivo and in vitro test systems. It has proven effectiveness against several animal tumours and human acute leukaemias. We have compared the inhibitory effect of rubidazone to that of adriamycin on P388 leukaemia and normal bone marrow colony-forming units (CFU) using the spleen colony assay system in male DBA2 mice. The efficacy ratios (i.e., the ratio of the slopes of the normal bone marrow CFU to leukaemic CFU dose-survival curves) in the spleen colony assay system for rubidazone and adriamycin were 7-8 and 7-5 respectively. This near identity of efficacy ratios fro rubidazone and adriamycin correlated with the results of median survival time studies in the leukaemic mice. Their dose-median survival time curves were almost parallel, having nearly identical slopes. Rubidazone's equal therapeutic index as compared to adriamycin in the spleen colony assay system together with its known decreased toxicity to cardiac muscle cells makes it an extremely promising new anthracycline derivative to study in comparison to adriamycin in human malignancies.
鲁比达唑，一种新的柔红霉素半合成苯腙盐酸盐衍生物，在仓鼠的心脏毒性研究以及其他体内和体外测试系统中，以分子量为基础已证明其毒性低于阿霉素，且在心脏毒性方面与柔红霉素相似。它已被证明对多种动物肿瘤和人类急性白血病有效。我们使用雄性DBA2小鼠的脾集落测定系统，比较了鲁比达唑和阿霉素对P388白血病和正常骨髓集落形成单位（CFU）的抑制作用。在脾集落测定系统中，鲁比达唑和阿霉素的疗效比（即正常骨髓CFU与白血病CFU剂量-存活曲线的斜率之比）分别为7 - 8和7 - 5。鲁比达唑和阿霉素的疗效比几乎相同，这与白血病小鼠的中位生存时间研究结果相关。它们的剂量-中位生存时间曲线几乎平行，斜率几乎相同。在脾集落测定系统中，鲁比达唑与阿霉素具有相同的治疗指数，以及其已知的对心肌细胞毒性降低，这使得它成为一种极具前景的新蒽环类衍生物，可与阿霉素相比用于人类恶性肿瘤的研究。
