| 李燕娜1,2 郭峰1,2 代卉2 毛玉昌2 沈智杰3 侴桂新4
王肖龙3△ 胡卓汉2△.降脂中药复方的转运性相互作用———体外MDR1 转运研究 *[J].,2014,14(10):1813-1815 |
| 降脂中药复方的转运性相互作用———体外MDR1 转运研究 * |
| Transporter-mediated Interaction of Lipid-lowering Traditional ChineseMedicine - In Vitro MDR1 Transport Study* |
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| DOI： |
| 中文关键词: 降脂中药；MDR1；体外；ATP 酶分析法；转运性相互作用 泽泻 |
| 英文关键词: Cholesterol-reducing TCM MDR1 ATPase assay In vitro Transporter-mediated interaction Alisma orientalis |
| 基金项目:十一五科技重大专项（2008AX10501） |
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| 中文摘要: |
| 摘要 目的：药物相互作用是影响药物安全和药效的重大因素之一。本文旨在通过体外 MDR1 研究方法———ATP 酶法，评价降脂
中药复方(Fang-2)及其单方6 个饮片水提物与P-gp 的相互作用，为临床中西药转运性相互作用提供参考。方法：应用标准化制备
技术，制备降脂中药复方及其6 个饮片水提物。利用基于MDR1 膜的ATP酶法，计算MDR1细胞膜的ATP 酶活性，考察药物与
P-gp的相互作用。结果：1 mg·mL-1、10 mg·mL-1两个浓度中药复方的ATP酶活性分别为27.2、40.0 nmol Pi·min-1·mg-1protein, 呈
浓度依赖性。6 个单方中，泽泻、厚朴、夏枯草与P-gp 作用显著，其强弱顺序为：泽泻> 夏枯草>厚朴（50.6 >42.6 > 40.0 nmol Pi·
min-1·mg-1 protein）。泽泻单体23-乙酰泽泻醇B、24- 乙酰泽泻醇A 均与P-gp 有较强的相互作用，ATP 酶动力学研究显示其Km
值和Vmax 值分别为0.79± 0.28 μM，2.01± 0.67 μM 和50.57± 3.72 nmol Pi·min-1·mg-1 protein，56.28± 29.6 nmol Pi·min-1·mg-1
protein。结论：Fang-2与MDR1 存在相互作用，其中泽泻为主要被MDR1 转运的饮片，泽泻的有效组分23- 乙酰泽泻醇B 和24-
乙酰泽泻醇A 均是MDR1 底物。表明该降脂中药与临床上其他降脂药物的联用时应充分考虑MDR1 介导的转运行相互作用，为
临床用降脂药物提供参考和依据。 |
| 英文摘要: |
| ABSTRACT Objective：Drug interaction is one of the major factors that affect the drug safety and efficacy. This paper is aim to
evaluate the transporter-mediated interaction of the lipid-lowering Traditional Chinese medicine (Fang-2) and its 6 simple prescriptions
through in vitro MDR1 transport research method- ATPase assay, providing a reference for clinical practice in herbal-drug interaction.
Methods：TCM and its 6 simple prescriptions were prepared using a standardized method. ATPase assay based on H-MDR1 membrane
were conducted to calculate the ATPase activity, thus to investigate the interaction between drugs and P-gp.Results：The ATPase activity
of P-gp at 1 mg·mL-1, 10 mg·mL-1of TCMwas 27.2, 40.0 nmol Pi·min-1·mg-1 protein respectively and showed a concentration-dependent
manner. In the 6 simple prescriptions, Alisma orientalis, Mangnolia officinalis and Prunella vulgaris had a significantly effect on P-gp.
The sequence fromstrong to weak of this effect is: Alisma orientalis > Prunella vulgaris > Mangnolia officinalis (50.6 > 42.6 > 40.0 nmol
Pi·min-1·mg-1 protein). Two monomers of Alisma orientalis, Alisol B 23-acetate and Alisol A 24-acetate, have a strong interaction with
P-gp. The Km and Vmax values were 0.79 ± 0.28 μM, 2.01 ± 0.67μM and 50.57 ± 3.72 nmol Pi·min-1·mg-1 protein, 56.28 ± 29.6
nmol Pi·min-1·mg-1 protein respectively extracted through kinetics studies. Conclusion：Both Fang-2 and its simple prescription-Alisma
orientalis are proved to be transported by MDR1. Two monomers of Alisma orientalis, Alisol B 23-acetate and Alisol A 24-acetate, are
also verified to be the substrates of MDR1, indicating that MDR1-mediated interaction should be fully considered in combination of
Fang-2 and other clinical lipid-lowering drugs, thus, providing the reference and basis for the clinical use of lipid-lowering drugs. |
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