Suppr超能文献

(桑佐)和(班德罗尔)抗伯氏疏螺旋体有效提取物的草药-药物相互作用潜力评估。

Herb⁻Drug Interaction Potential of Anti-Borreliae Effective Extracts from (Samento) and (Banderol) Assessed In Vitro.

机构信息

Department of Clinical Pharmacology and Pharmacoepidemiology, Heidelberg University Hospital, Im Neuenheimer Feld 410, 69120 Heidelberg, Germany.

出版信息

Molecules. 2018 Dec 31;24(1):137. doi: 10.3390/molecules24010137.

Abstract

Samento (extract from ) and Banderol (extract from ) have been demonstrated to have anti-inflammatory and antimicrobial properties, e.g., against different morphological forms of . However, there is hardly any data on the pharmacological safety of these two herbal medicines. This in vitro study aimed at scrutinizing their possible characteristics as perpetrators in pharmacokinetic herbal⁻drug interactions. Inhibition of cytochrome P450 enzymes (CYPs) was quantified by commercial kits and inhibition of drug transporters by use of fluorescent probe substrates. Induction was quantified by real-time RT-PCR and activation of pregnane x receptor (PXR) and aryl hydrocarbon receptor (AhR) by reporter gene assays. Organic anion transporting polypeptide 1B1 (OATP1B1) (IC = 0.49 ± 0.28%) and OATP1B3 (IC = 0.65 ± 0.29%) were potently inhibited by Banderol, but only weakly by Samento. CYP3A4 was inhibited about 40% at a Samento concentration of 1%. Samento significantly induced mRNA expression of , , , , and and strongly activated PXR, but hardly AhR. In conclusion, the perpetrator profiles of Samento and Banderol for herb⁻drug interactions completely differ. Clinical studies are strongly recommended to clarify whether the effects observed in vitro are of clinical relevance.

摘要

桑莫()和班卓琴()已被证明具有抗炎和抗菌特性,例如,对不同形态的有作用。然而,几乎没有关于这两种草药药理学安全性的数据。这项体外研究旨在仔细研究它们作为药代动力学草药-药物相互作用的肇事者的可能特征。细胞色素 P450 酶(CYPs)的抑制作用通过商业试剂盒进行量化,药物转运蛋白的抑制作用通过荧光探针底物进行量化。实时 RT-PCR 用于量化诱导作用,报告基因测定用于激活孕烷 X 受体(PXR)和芳烃受体(AhR)。有机阴离子转运多肽 1B1(OATP1B1)(IC = 0.49 ± 0.28%)和 OATP1B3(IC = 0.65 ± 0.29%)被班卓琴强烈抑制,但桑莫只被弱抑制。在 1%的桑莫浓度下,CYP3A4 被抑制约 40%。桑莫显著诱导 、 、 、 、 和的 mRNA 表达,并强烈激活 PXR,但几乎不激活 AhR。总之,桑莫和班卓琴在草药-药物相互作用中的肇事者特征完全不同。强烈建议进行临床研究,以阐明体外观察到的效果是否具有临床相关性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3124/6337116/acab05010761/molecules-24-00137-g001.jpg

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型,支持多种主流文档格式。

立即体验