Department of Clinical Pharmacology and Pharmacoepidemiology, Heidelberg University Hospital, Im Neuenheimer Feld 410, 69120 Heidelberg, Germany.
Molecules. 2018 Dec 31;24(1):137. doi: 10.3390/molecules24010137.
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.
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。