异莲心碱对大鼠CYP3A酶活性的影响
R972.9; 目的:探讨异莲心碱对CYP3A酶活性的影响,以了解异莲心碱与CYP3A酶底物合用药时可能产生的相互作用.方法:①建立体外肝微粒体混合酶代谢体系；②以睾酮作为底物探针,用HPLC建立检测CYP3A酶代谢活性的方法,考察体外代谢体系的最佳孵育条件；③将不同浓度异莲心碱分别与睾酮共同孵育于肝微粒体代谢体系中,测定在有或无异莲心碱存在下睾酮的减少量,以评估异莲心碱对CYP3A酶代谢的影响.结果:在肝微粒体孵育体系中,睾酮体外代谢的最佳孵育条件为底物浓度200μmol/L,代谢时间210 min.异莲心碱对CYP3A酶抑制作用较弱,IC50＞1 000 μmol/L.结论:异莲心碱对CY...
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| Published in | 浙江大学学报（医学版） Vol. 41; no. 2; pp. 178 - 182 |
|---|---|
| Main Authors | , |
| Format | Journal Article |
| Language | Chinese |
| Published |
浙江大学药学院,浙江杭州310058
2012
浙江大学城市学院,浙江杭州310015%浙江大学城市学院,浙江杭州,310015 |
| Subjects | |
| Online Access | Get full text |
| ISSN | 1008-9292 |
| DOI | 10.3785/j.issn.1008-9292.2012.02.009 |
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| Abstract | R972.9; 目的:探讨异莲心碱对CYP3A酶活性的影响,以了解异莲心碱与CYP3A酶底物合用药时可能产生的相互作用.方法:①建立体外肝微粒体混合酶代谢体系；②以睾酮作为底物探针,用HPLC建立检测CYP3A酶代谢活性的方法,考察体外代谢体系的最佳孵育条件；③将不同浓度异莲心碱分别与睾酮共同孵育于肝微粒体代谢体系中,测定在有或无异莲心碱存在下睾酮的减少量,以评估异莲心碱对CYP3A酶代谢的影响.结果:在肝微粒体孵育体系中,睾酮体外代谢的最佳孵育条件为底物浓度200μmol/L,代谢时间210 min.异莲心碱对CYP3A酶抑制作用较弱,IC50＞1 000 μmol/L.结论:异莲心碱对CYP3A酶无显著影响,可以与其底物联合用药. |
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| AbstractList | R972.9; 目的:探讨异莲心碱对CYP3A酶活性的影响,以了解异莲心碱与CYP3A酶底物合用药时可能产生的相互作用.方法:①建立体外肝微粒体混合酶代谢体系；②以睾酮作为底物探针,用HPLC建立检测CYP3A酶代谢活性的方法,考察体外代谢体系的最佳孵育条件；③将不同浓度异莲心碱分别与睾酮共同孵育于肝微粒体代谢体系中,测定在有或无异莲心碱存在下睾酮的减少量,以评估异莲心碱对CYP3A酶代谢的影响.结果:在肝微粒体孵育体系中,睾酮体外代谢的最佳孵育条件为底物浓度200μmol/L,代谢时间210 min.异莲心碱对CYP3A酶抑制作用较弱,IC50＞1 000 μmol/L.结论:异莲心碱对CYP3A酶无显著影响,可以与其底物联合用药. |
| Author | 宣贵达 南李 |
| AuthorAffiliation | 浙江大学药学院,浙江杭州310058;浙江大学城市学院,浙江杭州310015%浙江大学城市学院,浙江杭州,310015 |
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| Author_FL | XUAN Gui-da NAN Li |
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| DocumentTitle_FL | Influence of isoliensinine on activity of CYP3A in rats |
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| Keywords | CYP3A 异莲心碱 苄异喹啉类/药理学 药物相互作用 微粒体,肝 细胞色素P450酶系统/代谢 |
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| Title | 异莲心碱对大鼠CYP3A酶活性的影响 |
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