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两种蒽二酮与阿霉素对大鼠心脏毒性的比较。

Comparison of cardiotoxicity of two anthracenediones and doxorubicin in rats.

作者信息

Zbinden G, Beilstein A K

出版信息

Toxicol Lett. 1982 May;11(3-4):289-97. doi: 10.1016/0378-4274(82)90163-1.

DOI:10.1016/0378-4274(82)90163-1
PMID:7101322
Abstract

Two new anthracenediones with antineoplastic activities resembling those of the anthracycline antibiotics were studied in a rat cardiotoxicity model system. NCS-196473 was approx. 10-fold less toxic than doxorubicin and caused only minor electrocardiogram (ECG) changes. Its dihydroxyanalog NSC-279836 was somewhat more toxic than doxorubicin, caused marked leukopenia and induced ECG changes and moderate elevation of serum GOT, LDH and creatine phosphokinase (CK). Both anthracenediones induced marked alterations of mitochondrial structure in the heart but no dilatation of the sarcoplasmic reticulum and distortion of the contractile elements. It is concluded that the cardiotoxic effects of the anthracenediones are of a less specific nature than those caused by doxorubicin.

摘要

在大鼠心脏毒性模型系统中研究了两种具有类似于蒽环类抗生素抗肿瘤活性的新型蒽二酮。NCS-196473的毒性约比阿霉素低10倍,仅引起轻微的心电图(ECG)变化。其二羟基类似物NSC-279836的毒性比阿霉素略高,导致明显的白细胞减少,并引起心电图变化以及血清谷草转氨酶(GOT)、乳酸脱氢酶(LDH)和肌酸磷酸激酶(CK)的中度升高。两种蒽二酮均引起心脏线粒体结构的明显改变,但未引起肌浆网扩张和收缩成分扭曲。结论是,蒽二酮的心脏毒性作用比阿霉素引起的心脏毒性作用特异性更低。

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Mitoxantrone. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in the chemotherapy of cancer.米托蒽醌。对其药效学和药代动力学特性以及在癌症化疗中的治疗潜力的综述。
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