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芍药苷和白花芍药苷对人细胞色素P450 3A4和细胞色素P450 2D6的比较。

Comparison of Paeoniflorin and Albiflorin on Human CYP3A4 and CYP2D6.

作者信息

Gao Li-Na, Zhang Ye, Cui Yuan-Lu, Akinyi Olunga Mary

机构信息

Tianjin State Key Laboratory of Modern Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China ; Research Center of Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China.

Tianjin State Key Laboratory of Modern Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China ; Department of Pharmaceutical Sciences, Zibo Vocational Institute, Zibo, Shandong 255314, China.

出版信息

Evid Based Complement Alternat Med. 2015;2015:470219. doi: 10.1155/2015/470219. Epub 2015 May 19.

Abstract

Peony (Paeonia lactiflora Pall-) is a plant medicine and a functional food ingredient with wide application for more than 2000 years. It can be coadministrated with many other drugs, composed of traditional Chinese medicine compound such as shaoyao-gancao decoction. In order to explore the efficacy and safety of peony, effects of paeoniflorin and albiflorin (the principal components of peony) on cytochrome P450 (CYP) 3A4 and CYP2D6 were analyzed in human hepatoma HepG2 cells and evaluated from the level of recombinant CYP enzymes in vitro. The findings indicated that albiflorin possessed stronger regulation on the mRNA expression of CYP3A4 and CYP2D6 than paeoniflorin. For the protein level of CYP3A4, albiflorin showed significant induction or inhibition with the concentration increasing from 10(-7) M to 10(-5) M, but no remarkable variation was observed in paeoniflorin-treated group. Enzyme activity assay implied that both paeoniflorin and albiflorin could regulate CYP3A4 and CYP2D6 with varying degrees. The results showed that albiflorin should be given more attention because it may play a vital role on the overall efficacy of peony. The whole behavior of both paeoniflorin and albiflorin should be focused on ensuring the rationality and effectiveness of clinical application.

摘要

芍药(Paeonia lactiflora Pall-)是一种植物药和功能性食品成分,已有2000多年的广泛应用历史。它可与许多其他药物联合使用,是诸如芍药甘草汤等中药复方的组成成分。为了探究芍药的功效和安全性,在人肝癌HepG2细胞中分析了芍药苷和芍药内酯苷(芍药的主要成分)对细胞色素P450(CYP)3A4和CYP2D6的影响,并从体外重组CYP酶水平进行了评估。研究结果表明,芍药内酯苷对CYP3A4和CYP2D6 mRNA表达的调控作用比芍药苷更强。对于CYP3A4的蛋白水平,随着芍药内酯苷浓度从10(-7)M增加到10(-5)M,其表现出显著的诱导或抑制作用,但芍药苷处理组未观察到明显变化。酶活性测定表明,芍药苷和芍药内酯苷均可不同程度地调节CYP3A4和CYP2D6。结果表明,芍药内酯苷应受到更多关注,因为它可能对芍药的整体功效起着至关重要的作用。应关注芍药苷和芍药内酯苷的整体行为,以确保临床应用的合理性和有效性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0218/4452296/81fe3c20970f/ECAM2015-470219.001.jpg

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