摘要: |
研究甘草和连翘对牙鲆肝细胞色素P4503A(CYP3A)活性的影响。将牙鲆随机分为3组,即对照组、甘草组和连翘组,对照组每日口灌0.9%的生理盐水,试验组每日1次口灌甘草30mg/kg•bw和连翘100mg/kg•bw,连续口灌6d,第7d时,采用直接测定法和间接测定法(探针药物)进行CYP3A酶活性的测定。结果显示:在肝微粒体水平上,甘草和连翘均可明显提高红霉素-N-脱甲基酶活性,分别提高了1.79倍、4.87倍。与对照组相比,甘草组和连翘组氨苯砜的半衰期分别降低了4.51%(P>0.05)和6.8%(P<0.01);药时曲线下面积分别减小了8.28%(P>0.05)和32.3%(P<0.01);总清除率(CL)分别增加了5.63%(P>0.05)和99.3%(P<0.01)。说明连翘对牙鲆CYP3A的活性具有极显著诱导作用,甘草诱导作用不显著。提示其他药物与连翘合用时,其有效性和安全性可能会受到影响。 |
关键词: CYP3A活性 甘草 连翘 氨苯砜 牙鲆 |
DOI: |
分类号:945.1 |
基金项目:国家自然科学基金项目(面上项目,重点项目,重大项目) |
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Effect of Glycyrrhiza uralensis Fisc and Fisch FructusForsythiae on cytochrome CYP3A in Paralichthys olivaceus |
hanxianqin, lijian
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Yellow sea fisheries research institute Chinese academy of fishery sciences
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Abstract: |
The effects of Glycyrrhiza uralensis Fisch(GU)and Fisch Fructus Forsythiae(FS)on the activities of cytochrome CYP3A in Paralichthys olivaceus were studied .Fishes were divided into 3 groups as follows: GU and FS group were administered orally for 6 days at 30mg/kg•bw and 100mg/kg•bw,control fishes were given an equal volume of normal saline (0.9%)only.On 7th day,,the activities of CYP3A were measured directly and indirectly by probe drug. The results showed that on liver microsomes GU and FS were all increased significantly by 1.79 times and 4.87times respectively. Compared with the normal saline-treated control group, metabolizability of dapsone in FS and GU group were higher than that in the control group, the elimination half -lives were shortened by 4.51%(P>0.05) and 36.8%(P<0.01);.Area under the curve were shortened by 8.28%(P>0.05) and 32.3%(P<0.01);and the total clearances were increased by 5.63%(P>0.05) and 99.3%(P<0.01).The results showed that GU and FS can significantly induced the activity of CYP3A, the induction effect of FS is higher than GU. A drug's efficacy and safety may be affected when concomitantly used with them. |
Key words: CYP3Aactivity Glycyrrhiza uralensis Fisc Fisch Fructus Forsythiae Dapsone Paralichthys olivaceus |