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Absorption, disposition, and pharmacokinetics of saponins from Chinese medicinal herbs: what do we know and what do we need to know more?中草药中皂苷的吸收、分布和药代动力学:我们知道什么,还需要了解什么?
Curr Drug Metab. 2012 Jun 1;13(5):577-98. doi: 10.2174/1389200211209050577.
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Rapid screening of commercially available herbal products for the inhibition of major human hepatic cytochrome P450 enzymes using the N-in-one cocktail.使用N合一鸡尾酒对市售草药产品抑制主要人类肝细胞色素P450酶进行快速筛选。
Xenobiotica. 2010 Apr;40(4):245-54. doi: 10.3109/00498251003592683.
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An evaluation of the cytochrome P450 inhibition potential of selected pesticides in human hepatic microsomes.评价部分农药对人肝微粒体细胞色素 P450 的抑制作用。
J Environ Sci Health B. 2009 Aug;44(6):553-63. doi: 10.1080/03601230902997766.
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Inhibitory effects of polyphenols on human cytochrome P450 3A4 and 2C9 activity.多酚对人细胞色素 P450 3A4 和 2C9 活性的抑制作用。
Food Chem Toxicol. 2010 Jan;48(1):429-35. doi: 10.1016/j.fct.2009.10.041. Epub 2009 Oct 31.
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Cytochrome P450 2C19 inhibitory activity of common berry constituents.常见浆果成分对细胞色素 P450 2C19 的抑制活性。
Phytother Res. 2010 Feb;24(2):304-7. doi: 10.1002/ptr.2910.
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Toxicol In Vitro. 2009 Jun;23(4):748-53. doi: 10.1016/j.tiv.2009.03.008. Epub 2009 Mar 26.
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Immunomodulatory effect of extracts of Hibiscus sabdariffa L. (Family Malvaceae) in a mouse model.木槿(锦葵科)提取物在小鼠模型中的免疫调节作用。
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8
In vitro interaction cocktail assay for nine major cytochrome P450 enzymes with 13 probe reactions and a single LC/MSMS run: analytical validation and testing with monoclonal anti-CYP antibodies.采用13种探针反应和单次液相色谱/串联质谱分析对9种主要细胞色素P450酶进行体外相互作用混合测定:分析验证及单克隆抗CYP抗体检测
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Effects of water extract of Hibiscus sabdariffa, Linn (Malvaceae) 'Roselle' on excretion of a diclofenac formulation.锦葵科植物玫瑰茄水提取物对双氯芬酸制剂排泄的影响。
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Cytochrome P450 (CYP) inhibition screening: comparison of three tests.细胞色素P450(CYP)抑制筛选:三种测试方法的比较。
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木槿(锦葵科)提取物对选定细胞色素P450同工酶的体外抑制活性。

In vitro inhibitory activities of the extract of Hibiscus sabdariffa L. (family Malvaceae) on selected cytochrome P450 isoforms.

作者信息

Johnson Showande Segun, Oyelola Fakeye Titilayo, Ari Tolonen, Juho Hokkanen

机构信息

Department of Clinical Pharmacy and Pharmacy Administration, Faculty of Pharmacy, University of Ibadan, Ibadan. Nigeria.

出版信息

Afr J Tradit Complement Altern Med. 2013 Apr 12;10(3):533-40. eCollection 2013.

PMID:24146485
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3777597/
Abstract

Literature is scanty on the interaction potential of Hibiscus sabdariffa L., plant extract with other drugs and the affected targets. This study was conducted to investigate the cytochrome P450 (CYP) isoforms that are inhibited by the extract of Hibiscus sabdariffa L. in vitro. The inhibition towards the major drug metabolizing CYP isoforms by the plant extract were estimated in human liver microsomal incubations, by monitoring the CYP-specific model reactions through previously validated N-in-one assay method. The ethanolic extract of Hibiscus sabdariffa showed inhibitory activities against nine selected CYP isoforms: CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1 and CYP3A4. The concentrations of the extract which produced 50% inhibition of the CYP isoforms ranged from 306 µg/ml to 1660 µg/ml, and the degree of inhibition based on the IC50 values for each CYP isoform was in the following order: CYP1A2 > CYP2C8 > CYP2D6 > CYP2B6 > CYP2E1 > CYP2C19 > CYP3A4 >> CYP2C9 >> CYP2A6. Ethanolic extract of Hibiscus sabdariffa caused inhibition of CYP isoforms in vitro. These observed inhibitions may not cause clinically significant herb-drug interactions; however, caution may need to be taken in co-administering the water extract of Hibiscus sabdariffa with other drugs until clinical studies are available to further clarify these findings.

摘要

关于玫瑰茄植物提取物与其他药物的相互作用潜力及其影响靶点的文献较少。本研究旨在调查体外条件下玫瑰茄提取物对细胞色素P450(CYP)同工酶的抑制作用。通过预先验证的N合一检测方法监测CYP特异性模型反应,在人肝微粒体孵育中评估该植物提取物对主要药物代谢CYP同工酶的抑制作用。玫瑰茄乙醇提取物对九种选定的CYP同工酶具有抑制活性:CYP1A2、CYP2A6、CYP2B6、CYP2C8、CYP2C9、CYP2C19、CYP2D6、CYP2E1和CYP3A4。产生50% CYP同工酶抑制作用的提取物浓度范围为306 µg/ml至1660 µg/ml,基于每种CYP同工酶IC50值的抑制程度顺序如下:CYP1A2 > CYP2C8 > CYP2D6 > CYP2B6 > CYP2E1 > CYP2C19 > CYP3A4 >> CYP2C9 >> CYP2A6。玫瑰茄乙醇提取物在体外引起CYP同工酶抑制。这些观察到的抑制作用可能不会导致临床上显著的药草-药物相互作用;然而,在将玫瑰茄水提取物与其他药物联合使用时可能需要谨慎,直到有临床研究进一步阐明这些发现。