Metabolism of adriamycin in hepatocytes isolated from the rat and the rabbit.
Metabolism of adriamycin in hepatocytes isolated from the rat and the rabbit.
复制标题
阿霉素在大鼠和兔肝细胞中的代谢。
DOI：
10.1016/0006-2952(87)90240-1
复制
发表时间：
1987
影响因子：
5.8
通讯作者：
Yanovich,S
中科院分区：
文献类型：
--
作者：
Gewirtz,DA;Yanovich,S
阿霉素（一种蒽环类抗生素）的代谢在需氧条件下在大鼠和兔肝细胞中进行了表征。阿霉素是大鼠和兔肝细胞中细胞内的主要荧光物质。在大鼠肝细胞中，主要的细胞内代谢产物是脱氧阿霉素糖苷配基，同时也合成了显着水平的脱氧阿霉素糖苷配基;在细胞或孵育培养基中观察到很少的阿霉素。相比之下，在兔肝细胞中，形成了显著水平的阿霉素以及脱氧阿霉素糖苷配基;脱氧阿霉素糖苷配基是主要的细胞内代谢产物，而观察到低水平的脱氧阿霉素糖苷配基。相对形成的脱氧阿霉素苷元和脱氧阿霉素苷元表明，阿霉素可以更有效地代谢为脱氧苷元衍生物比母体药物。在大鼠或家兔肝细胞或孵育培养基中均未观察到阿霉素结合物。
Metabolism of adriamycin, an anthracycline antibiotic, was characterized in both rat and rabbit hepatocytes under aerobic conditions. Adriamycin was the predominant fluorescent species within the cell in hepatocytes from both the rat and the rabbit. In the rat hepatocyte, the primary intracellular metabolite was deoxyadriamycin aglycone, while significant levels of deoxyadriamycinol aglycone were also synthesized; little adriamycinol was observed in the cells or the incubation medium. In contrast, in the rabbit hepatocyte, significant levels of adriamycinol as well as deoxyadriamycinol aglycone were formed; deoxyadriamycinol aglycone was the primary intracellular metabolite while low levels of deoxyadriamycin aglycone were observed. The relative formation of deoxyadriamycinol aglycone and deoxyadriamycin aglycone suggests that adriamycinol may be metabolized more effectively to the deoxyaglycone derivative than the parent drug. Conjugates of adriamycin were not observed in hepatocytes from either the rat or the rabbit or in the incubation medium.