Antineoplastic activity and pharmacokinetics of adriamycin and daunomycin in tumor bearing mice.
Antineoplastic activity and pharmacokinetics of adriamycin and daunomycin in tumor bearing mice.
复制标题
阿霉素和道诺霉素在荷瘤小鼠中的抗肿瘤活性和药代动力学。
作者：
A. Martini;N. G. Donelli;A. Mantovani;M. A. Pacciarini;E. F. Fogar;L. Morasca;S. Garattini;F. Spreafico
在肌肉注射Lewis肺癌的C57B1/6小鼠中，单次静脉注射阿霉素对原发肿瘤及其肺转移的抗肿瘤活性高于同等剂量的类似物柔红霉素。柔红霉素与上述肿瘤细胞的体外结合力高于阿霉素，但两者的细胞毒作用无明显差异。药代动力学研究表明，阿霉素(和/或其代谢物)在肿瘤组织中的蓄积比柔红霉素更快、数量更多、持续时间更长。讨论了这些发现在解释阿霉素在实验动物中的更大治疗活性方面的可能重要性。
In C57B1/6 mice bearing the intramuscular Lewis lung carcinoma, single intravenous doses of Adriamycin showed an higher antineoplastic effectiveness on the primary tumor and its lung metastasis than equal doses of its analog Daunomycin. The in vitro cell-binding of Daunomycin to these tumor cells was higher than that of Adriamycin, but no differences in cytotoxicity were found between the two agents. Pharmacokinetic studies revealed that Adriamycin (and/or its metabolites) accumulated in the neoplastic tissue more promptly, in significantly greater quantities and for longer periods than Daunomycin. The possible importance of these findings in explaining the greater therapeutic activity of Adriamycin in experimental animals is discussed.