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阿霉素和柔红霉素在荷瘤小鼠体内的抗肿瘤活性及药代动力学

Antineoplastic activity and pharmacokinetics of adriamycin and daunomycin in tumor bearing mice.

作者信息

Martini A, Donelli N G, Mantovani A, Pacciarini M A, Fogar-Ottaviano E F, Morasca L, Garattini S, Spreafico F S

出版信息

Oncology. 1977;34(4):173-8. doi: 10.1159/000225216.

DOI:10.1159/000225216
PMID:917449
Abstract

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.

摘要

在携带肌肉内Lewis肺癌的C57B1/6小鼠中,单剂量静脉注射阿霉素对原发性肿瘤及其肺转移的抗肿瘤效果高于同等剂量的类似物柔红霉素。柔红霉素与这些肿瘤细胞的体外细胞结合率高于阿霉素,但两种药物的细胞毒性没有差异。药代动力学研究表明,与柔红霉素相比,阿霉素(和/或其代谢物)在肿瘤组织中积累得更快、数量更多、时间更长。讨论了这些发现对于解释阿霉素在实验动物中具有更大治疗活性的可能重要性。

相似文献

1
Antineoplastic activity and pharmacokinetics of adriamycin and daunomycin in tumor bearing mice.阿霉素和柔红霉素在荷瘤小鼠体内的抗肿瘤活性及药代动力学
Oncology. 1977;34(4):173-8. doi: 10.1159/000225216.
2
A differential interaction of daunomycin, adriamycin, and N-trifluoroacetyladriamycin 14-valerate with mouse peritoneal macrophages.
Cancer Res. 1978 Nov;38(11 Pt 1):3944-9.
3
In vitro uptake and cytotoxicity of adriamycin in primary and metastatic Lewis lung carcinoma.阿霉素在原发性和转移性Lewis肺癌中的体外摄取及细胞毒性
Eur J Cancer (1965). 1979 Sep;15(9):1121-9. doi: 10.1016/0014-2964(79)90128-2.
4
In vitro and in vivo cytotoxicity of adriamycin and daunomycin for murine macrophages.阿霉素和柔红霉素对小鼠巨噬细胞的体外和体内细胞毒性。
Cancer Res. 1977 Mar;37(3):815-20.
5
[Distribution and chemotherapeutic activity of daunomycin and adriamycin in spontaneous mammary carcinoma of mice].
Tumori. 1972 Jul-Aug;58(4):213-8. doi: 10.1177/030089167205800404.
6
Interaction between heparin and adriamycin in mice bearing the Lewis lung carcinoma.荷Lewis肺癌小鼠中肝素与阿霉素的相互作用
Biomedicine. 1981 Dec;34(3):124-8.
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The covalent binding of daunomycin and adriamycin to antibodies, with retention of both drug and antibody activities.
Cancer Res. 1975 May;35(5):1175-81.
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Role of host defense merchanisms in the antitumor activity of adriamycin and daunomycin in mice.宿主防御机制在阿霉素和柔红霉素对小鼠的抗肿瘤活性中的作用。
J Natl Cancer Inst. 1979 Jul;63(1):61-6.
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Pharmacokinetic, toxicologic, and chemotherapeutic properties of detorubicin in mice: a comparative study with daunorubicin and adriamycin.去甲柔红霉素在小鼠体内的药代动力学、毒理学及化疗特性:与柔红霉素和阿霉素的比较研究
Cancer Treat Rep. 1979 May;63(5):861-7.
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Pharmacological and therapeutic efficacy of rubidazone in mice. Comparison with daunomycin and adriamycin.
Eur J Cancer (1965). 1979 Mar;15(3):363-71. doi: 10.1016/0014-2964(79)90048-3.

引用本文的文献

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Distribution and antitumoral activity of adriamycin combined with warfarin in mice.阿霉素与华法林联合用药在小鼠体内的分布及抗肿瘤活性
Cancer Chemother Pharmacol. 1980;5(1):43-7. doi: 10.1007/BF00578561.
2
Doxorubicin pharmacokinetics after intravenous and intraperitoneal administration in the nude mouse.
Cancer Chemother Pharmacol. 1981;5(4):267-70. doi: 10.1007/BF00434396.
3
Prevention of adriamycin toxicity.阿霉素毒性的预防
Cancer Chemother Pharmacol. 1983;11(2):91-3. doi: 10.1007/BF00254252.