棒曲霉素在蟋蟀血液注射后的毒代动力学。

Benzo(a)pyrene toxicokinetics in the cricket following injection into the haemolymph.

机构信息

Environmental Toxicology Program, Department of Biological Sciences, Simon Fraser University, Burnaby, BC, V5A 1S6, Canada.

出版信息

Environ Toxicol Pharmacol. 1998 Oct;6(2):81-9. doi: 10.1016/s1382-6689(98)00021-0.

DOI:10.1016/s1382-6689(98)00021-0

PMID:21781884

Abstract

The metabolic disposition of (14)C-labelled benzo(a)pyrene (BP) in the cricket (Acheta domesticus) was investigated after injection into the haemolymph. (14)C-BP was taken up rapidly by the nerve cord, malpighian tubules, reproductive organs, gut, and muscle:cuticle of the cricket. The elimination half-lives of (14)C-BP in these tissues ranged from 8.9 to 17.8 h. The haemolymph (14)C-BP concentration-time curve could be described by a one-compartment open pharmacokinetic model. (14)C-BP was metabolized by the cricket mainly to unconjugated and conjugated BP metabolites since very little unchanged (14)C-BP was found in the excreta at 48 h post-dosing. GLPC-MSD and HPLC/ES-MS analyses showed the presence of at least two BP metabolites in the excreta. The BP metabolites were identified tenatively as the diol derivatives of benzo(a)pyrene and benzo(a)pyrene quinone.

摘要

在向血淋巴中注射（14）C 标记的苯并（a）芘（BP）后，研究了其在蟋蟀（Acheta domesticus）中的代谢处置情况。（14）C-BP 被神经索、马氏管、生殖器官、肠道和肌肉-外骨骼迅速吸收。（14）C-BP 在这些组织中的消除半衰期范围为 8.9 至 17.8 小时。血淋巴（14）C-BP 浓度-时间曲线可以用单室开放药代动力学模型来描述。蟋蟀主要将（14）C-BP 代谢为未结合和结合的 BP 代谢物，因为在给药后 48 小时，粪便中几乎没有未改变的（14）C-BP。GLPC-MSD 和 HPLC/ES-MS 分析表明，粪便中至少存在两种 BP 代谢物。BP 代谢物被暂时鉴定为苯并（a）芘和苯并（a）芘醌的二醇衍生物。