呋喃西林代谢产物在中国对虾(Fenneropenaeus chinensis)体内的消除规律及其对代谢酶活性的影响

The Elimination Rules of Nitrofurazone Metabolites and Its Effects on Activities of Metabolic Enzymes in Fenneropenaeus chinensis

中文关键词: 中国对虾  呋喃西林  氨基脲  消除规律  细胞色素P450

英文关键词: Fenneropenaeus chinensis  Nitrofurazone  Semicarbazide  Elimination rules  CYP450s

中文摘要:

      中国对虾(Fenneropenaeus chinensis)以30 mg/kg体重剂量投喂呋喃西林药饵5 d后，检测对虾各组织中呋喃西林代谢物氨基脲(Semicarbazide, SEM)浓度和肝胰腺中的药物代谢酶活性。结果显示，肝胰腺中药物起始和达峰浓度最大，远远高于其他各组织。20 d实验结束时，SEM浓度依次为肌肉>鳃>甲壳>血淋巴>肝胰腺，消除半衰期为肌肉(5.89 d)>甲壳(4.66 d) >鳃(2.95 d) >血淋巴(2.70 d) >肝胰腺(1.47 d)，肝胰腺中SEM消除最快，肌肉中消除最慢，药物残留时间较长。与对照组相比，给药组肝胰腺中乙氧基香豆素-O-脱乙基酶(ECOD)和氨基比林-N-脱甲基酶(APND)活性均呈现先下降后上升的趋势，停药3 h时，ECOD活性极显著低于对照组(P<0.01)，酶活性被最大程度抑制，随后出现上升趋势，并分别于48、72、96、120、240 h时，ECOD活性均极显著高于对照组(P<0.01)；APND在停药6 h和9 h时活性最低，被抑制效应最大(P<0.01)，240 h时极显著高于对照组(P<0.01)，之后APND活性降低并趋向对照组水平。结果表明，SEM在中国对虾体内消除缓慢，消除半衰期较长，并对ECOD、APND酶活性有影响，推测ECOD、APND参与呋喃西林在中国对虾体内的代谢消除。

英文摘要:

      In this study we explored the elimination rules of semicarbazide (SEM) and its effect on the activities of hepatopancreas enzymes in Fenneropenaeus chinensis. Experimental shrimps were fed with a diet supplemented with nitrofurazone for five days before they were randomly selected from the tank and sampled in different days after the last oral administration. The concentrations of SEM in the hemolymph，hepatopancreas, gill, muscle and carapace were measured with LC-MS/MS, and the activities of ethoxylcumarin odethylase (ECOD) and aminopyrine N-demethylase (APND) in the hepatopancreas were examined with UV spectrophotometry and fluorospectrophotometry. The results showed that 1 h post treatment, the mean concentrations of SEM in the shrimp tissues were in the order of hepatopancreas>gill>carapace>muscle>plasma. At the end of the 20th day post treatment, SEM was still detectable in all tissues and the order of the concentration was muscle>gill>carapace>plasma> hepatopancreas. The half life of the elimination phase in the muscle, carapace, gill, plasma and hepatopancreas was 5.89 d, 4.66 d, 2.95 d, 2.70 d and 1.47 d respectively. Our results indicated that the elimination of SEM was the fastest in the hepatopancreas and the slowest in the muscle, and that SEM remained in the body of F. chinensis for long. Compared to the control, the activities of ECOD and APND in the experimental group were first reduced, followed by an increase, and finally returned to the normal levels. The activity of ECOD in the experimental group was significantly lower than the control 1 h post treatment (P<0.05), and the statistical significance was even greater than 3 h post treatment (P<0.01). Afterward the activity was enhanced and became significantly higher than the control at 48 h, 72 h, 96 h, 120 h, and 240 h (P<0.01) post treatment. The activity of APND was significantly lower than the control at 6 h and 9 h (P<0.01) but obviously higher at 96 h (P<0.05) and 240 h (P<0.01), and the final level was lower than the control at 480 h. These data suggested that SEM was eliminated slowly in F. chinensis and had an impact on the activities of ECOD and APND. Moreover, ECOD and APND may be involved in the metabolism of nitrofurazone.