| 摘要: |
| 研究甘草(Glycyrrhiza uralensis)和连翘(Forsythia suspensa)对牙鲆(Paralichthys olivaceus)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30 mg/kg 和连翘100 mg/kg, 连续口灌6 d, 第7 天时, 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36.8%(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(Glycyrrhiza uralensis) 连翘(Forsythia suspensa) 氨苯砜 牙鲆(Paralichthys olivaceus) |
| DOI： |
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| 基金项目:公益性行业专项 (nyhyzx07-046); 国家自然科学基金资助项目(30700617) |
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| Effects of Glycyrrhiza uralensis and Forsythia suspensa on cytochrome CYP3A in Paralichthys olivaceus |
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| Abstract: |
| The effects ofGlycyrrhiza uralensis (GU) and Forsythia suspensa (FS) on activities of cytochrome CYP3A in Paralichthys olivaceus were studied. Fishes were divided into three groups as follows: GU and FS group were administered orally for six days at 30mg/kg·bw and 100mg/kg·bw, respectively; fish in the control group were given an equal volume of normal saline (0.9%). Seven day after the injection, the activities of CYP3A were measured directly and indirectly. We found that on the level of liver microsomes, GU and FS both increased erythromycin N-demethylase activity significantly by 1.79 times and 4.87 times respectively. Compared with the normal saline-treated control group, metabolism 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), respectively. Area under the concentration-time curve were shortened by 8.28% (P>0.05) and 32.3% (P<0.01), respectively; and the total body clearances were increased by 5.63% (P>0.05) and 99.3% (P<0.01), respectively. The results showed that GU and FS can significantly induced the activity of CYP3A; and the induction effect of FS is higher than GU. A drug’s efficacy and safety may be affected by other drugs used concomitantly. |
| Key words: CYP3A activity Glycyrrhiza uralensis Forsythia suspensa Dapsone Paralichthys olivaceus |
