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阿霉素和柔红霉素在对照小鼠及苯巴比妥预处理小鼠体内的残留与代谢

Body residue and metabolism of adriamycin and daunorubicin in control and phenobarbital-pretreated mice.

作者信息

Bolanowska W, Gessner T

出版信息

Xenobiotica. 1982 Feb;12(2):125-36. doi: 10.3109/00498258209046786.

Abstract
  1. Metabolism of adriamycin (ADR) and daunorubicin (DR) was investigated in DBA/2Ha mice after i.p. injection and compared with that in phenobarbital-pretreated animals. At 24 h after drug administration 83% of ADR and 67% of DR derived fluorescence were recovered from cadavers and excreta. Destruction of anthracyclines in excreta to non-fluorescent materials could be partly responsible for the low recoveries. 2. ADR was metabolized to a limited extent in mice. At 24 h 70% dose was detected as the unchanged drug and only 13% as its deoxyaglycones. 3. DR was metabolized more extensively. At 24 h 29% of the dose was as the unchanged drug, while 32% was present as daunorubicinol (DROL) and 16% as aglycones. Phenobarbital did not significantly affect these parameters. 4. In phenobarbital-pretreated mice there was a marked increase in the amount of ADR or DR aglycones in the liver, and a decrease in the levels of unchanged ADR or DR.
摘要
  1. 腹腔注射后,在DBA/2Ha小鼠中研究了阿霉素(ADR)和柔红霉素(DR)的代谢情况,并与经苯巴比妥预处理的动物进行了比较。给药后24小时,从尸体和排泄物中回收了83%的ADR衍生荧光和67%的DR衍生荧光。排泄物中蒽环类药物被破坏为非荧光物质可能是回收率低的部分原因。2. ADR在小鼠体内代谢程度有限。24小时时,70%的剂量被检测为未变化的药物,只有13%被检测为其脱氧糖苷配基。3. DR代谢更为广泛。24小时时,29%的剂量为未变化的药物,而32%以柔红霉醇(DROL)形式存在,16%以糖苷配基形式存在。苯巴比妥对这些参数没有显著影响。4. 在经苯巴比妥预处理的小鼠中,肝脏中ADR或DR糖苷配基的量显著增加,而未变化的ADR或DR水平降低。

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