王青秀1, 4#,雷荣辉1, 2#,吴纯启1,廖明阳1,肖小河3,王全军1*.大黄素对大鼠肝脏CYP450酶的诱导研究[J].药物评价研究,2015,38():1-4
大黄素对大鼠肝脏CYP450酶的诱导研究
Induction of cytochrome P450 enzymes by emodin in liver tissue of rats
投稿时间:2014-11-03  
DOI:
中文关键词:  大黄素;细胞色素P450;红霉素脱甲基酶;氨基比啉-N-脱甲基酶;CYP1A;CYP2B;CYP2E1
英文关键词:emodin; cytochrome P450 enzyme; CYP3A; aminopyrine N-demethylase; CYP1A; CYP2B; CYP2E1
基金项目:重大新药创制科技重大专项(2013ZX09302303,2012ZX09301-003-001-008)
作者单位
王青秀1, 4#,雷荣辉1, 2#,吴纯启1,廖明阳1,肖小河3,王全军1* 1. 军事医学科医学院毒物药物研究所,抗毒药物与毒理学国家重点实验室(军事医学科学院),国家北京药物安全评价研究中心,北京 100850
2. 西安交通大学医学部公共卫生学院,西安 710061
3. 解放军302 医院全军中药研究所,北京 100039
4. 北京市海淀区卫生局卫生监督所,北京 100037 
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中文摘要:
      目的 探讨大黄素对大鼠肝脏细胞色素P450酶(CYP450)及其主要亚型的影响。方法 20只雄性SD大鼠,随机分成4组,每组5只,分别为溶剂对照组,170、500和1 500 mg/kg大黄素染毒组,大黄素蒸馏水混悬后连续经口给药16 d,结束后次日取大鼠肝脏组织制作微粒体,分别采用CO还原差示光谱法、分光光度法及化学发光法检测大鼠肝脏微粒体总CYP450水平,红霉素脱甲基酶(CYP3A)、氨基比啉-N-脱甲基酶,CYP1A、CYP2B和CYP2E1酶活性变化。结果 大黄素连续经口给药16 d,能够引起大鼠肝脏微粒体总CYP450显著升高、可轻度诱导CYP3A、CYP1A、CYP2E1和CYP2B酶,500 mg/kg剂量组最明显。结论 大黄素对大鼠肝脏中CYP3A、CYP1A、CYP2B和CYP2E1酶均有诱导作用。
英文摘要:
      Objective To explore the effects of emodin on cytochrome P450 enzyme (CYP450) and elucidate the toxicity mechanism of emodin. Methods Twenty male SD rats were randomly divided into four groups. The extracts of the liver tissues of rats treated with emodin at different doses (170, 500, 1 500 mg/kg for 16 d) were in preparation of microsomes, the activities of total CYP450, CYP3A, aminopyrine N-demethylase, CYP1A, CYP2B, and CYP2E1 were respectively determined by the reduction of CO difference spectroscopy, spectrophotometer, and chemiluminescence method. Results Induction of the total cytochrome P450 enzyme, CYP3A, CYP1A, CYP2E1, and CYP2B were observed in the liver tissues of rats treated with emodin for 16 d, the induction effect was most obvious in the liver tissues of rats in 500 mg/kg group. Conclusion Emodin could induce the cytochrome P450 enzyme including CYP3A, CYP1A, CYP2B, and CYP2E1 in the liver tissues of rats.
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