恩诺沙星在凡纳滨对虾体内和体外肝微粒体中的代谢产物比较分析  

Analysis of the metabolites of enrofloxacin from Litopenaeus vannamei in vivoand in vitrousing UPLC/Q-TOF MS

作　　者：周帅[1] 胡琳琳[1] 孙贝贝[1] 房文红[1] 

机构地区：[1]中国水产科学研究院东海水产研究所农业部海洋与河口渔业资源及生态重点开放实验室,上海200090

出　　处：《海洋渔业》2012年第3期342-349,共8页Marine Fisheries

基　　金：中央级公益性科研院所基本科研业务费专项资金(中国水产科学研究院东海水产研究所2007M06)

摘　　要：采用超高效液相色谱-四级杆-飞行时间质谱(UPLC/Q-TOF MS)对恩诺沙星在凡纳滨对虾(Litopenaeus vannamei)体内和体外肝胰腺微粒体孵育下的代谢产物进行定性分析。体内试验为凡纳滨对虾口灌30 mg.kg-1恩诺沙星,24 h后采集血浆用于代谢产物分析。体外试验为在含有肝微粒体的NADPH体系中加入恩诺沙星(100μM)进行孵育,检测孵育液中的代谢产物;肝胰腺采集自未给药的凡纳滨对虾,超速离心法制备而得。凡纳滨对虾血淋巴中除以恩诺沙星原形药物为主外,还可检测到少量的N-去乙基代谢产物环丙沙星、环丙沙星哌嗪环开环代谢物及其同分异构体;而在肝胰腺微粒体体外孵育体系中除检测到原形药物外,只有少量的N-去乙基代谢物环丙沙星。无论是体内还是体外,代谢产物生成量都很少,但环丙沙星是主要代谢产物。推测恩诺沙星在凡纳滨对虾体内的代谢反应主要是脱乙基反应和加氢还原反应,而在体外肝胰腺微粒体恩诺沙星代谢的反应主要是脱乙基反应。An ultraperformance liquid chromatography coupled with Q-TOF mass spectrometry（UPLC/Q-TOF MS） was used for the identification of metabolites of enrofloaxcin in white shrimp（Litopenaeus vannamei） in vivo and in vitro.Enrofloxacin was orally administrated to shrimp at a dose of 30 mg·kg-1,and plasma was sampled after 24h and used for metabolite analysis.Hepatopancreas was collected from enrofloxacin-free shrimps and used for microsome preparation by ultracentrifugation.Hepatopancreas microsomes in NADPH system with added enrofloxacin（100 μM） were incubated for 2 h and metabolites in the incubation were detected by UPLC/Q-TOF MS.The results showed that three metabolites were detected in the white shrimp hemolymph after oral administration of enrofloxacin,among which the peak area of ciprofloxacin was the biggest,and the others were piperazine ring-opening ciprofloxacin and its isomer.In the white shrimp hepatopancreas microsome incubation in vitro,just a small amount of ciprofloxacin metabolite was found.Very little amount of metabolites were biotransformed in vivo nor in vitro,but ciprofloxacin was the main metabolite.It was speculated that enrofloxacin metabolism in white shrimp in vivo might be deethylation and hydrogenation,while in hepatopancreas in vitro be deethylation.

关 键 词：恩诺沙星 代谢产物 凡纳滨对虾 体内和体外 超高效液相色谱-四级杆-飞行时间质谱 

分 类 号：S948[农业科学—水产养殖]