生物消除大鼠和豚鼠尿液中 3-溴苯并蒽酮的结合代谢物。

Bio-elimination of conjugated metabolites of 3-bromobenzanthrone in urine of rats and Guinea pigs.

机构信息

Department of Biochemistry, Lucknow University, Lucknow, India.

出版信息

Toxicol Mech Methods. 2004;14(6):345-54. doi: 10.1080/15376520490434719.

DOI:10.1080/15376520490434719

PMID:20021101

Abstract

The profile of urinary metabolites of 3-bromobenzanthrone (3-BBA), an extensively used anthraquinone dye intermediate, in rats and guinea pigs was investigated using HPTLC system. A total of 10 fluorescent metabolites were detected in the urine of guinea pigs as compared to 8 in rats including the parent compound 3-BBA. The elimination of metabolites increased in a dose dependent manner in rats. The Rf values of metabolites in rats were 0.14, 0.29, 0.42, 0.52, 0.58, 0.64, 0.77 and 0.91 while that in guinea pigs were 0.23, 0.26, 0.34, 0.37, 0.44, 0.54, 0.56, 0.68, 0.76 and 0.95. The urine of 3-BBA (50 mg/kg b.wt) treated guinea pigs when digested with acid showed the disappearance of metabolite 1, 2, 5 and 7 indicating these to be the conjugated metabolites. Further, digestion of urine of 3-BBA treated guinea pigs with glucuronidase showed disappearance of metabolite 5 and 7 suggesting these as glucuronide conjugates. Digestion of urine with sulfatase enzyme resulted in disappearance of metabolite 1 which could be a sulfate conjugate. Urinary metabolite 2 which was found to be present even after digestion with glucuronidase or sulfatase but disappeared following acid treatment appears to be glutathione conjugate(s) which resulted in formation of metabolite 3 and 6. These results suggest that conjugated fluorescent metabolites of 3-BBA are excreted in urine of rats and guinea pigs.

摘要

采用 HPTLC 系统研究了广泛用于蒽醌染料中间体的 3-溴苯并蒽酮（3-BBA）在大鼠和豚鼠尿液中的代谢产物谱。与大鼠相比，豚鼠尿液中检测到 10 种荧光代谢产物，而大鼠中则检测到 8 种，包括母体化合物 3-BBA。代谢产物的消除在大鼠中呈剂量依赖性增加。大鼠中代谢产物的 Rf 值为 0.14、0.29、0.42、0.52、0.58、0.64、0.77 和 0.91，而豚鼠中的 Rf 值为 0.23、0.26、0.34、0.37、0.44、0.54、0.56、0.68、0.76 和 0.95。用酸消化 3-BBA（50mg/kg b.wt）处理的豚鼠尿液中，代谢产物 1、2、5 和 7 消失，表明这些是结合代谢产物。此外，用葡萄糖醛酸苷酶消化 3-BBA 处理的豚鼠尿液，代谢产物 5 和 7 消失，提示这些是葡萄糖醛酸苷缀合物。用硫酸酯酶消化尿液导致代谢产物 1 消失，可能是硫酸盐缀合物。即使在用葡萄糖醛酸苷酶或硫酸酯酶消化后仍发现存在的尿液代谢产物 2 在酸处理后消失，似乎是谷胱甘肽缀合物，导致代谢产物 3 和 6 的形成。这些结果表明，3-BBA 的结合荧光代谢产物通过尿液从大鼠和豚鼠中排泄。