Effect of Oregon grape root extracts on P-glycoprotein mediated transport in in vitro cell lines.
Effect of Oregon grape root extracts on P-glycoprotein mediated transport in in vitro cell lines.
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DOI：
10.3389/jpps.2023.11927
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发表时间：
2023
影响因子：
2.7
通讯作者：
Zhang, Lei
中科院分区：
文献类型：
--
作者：
Fan, Ying;Zhou, Zhu;Zhang, Lei
关键词：
目的：研究俄勒冈州葡萄根提取物对P-糖蛋白活性的调节作用。方法：在Caco-2和MDCKII-MDR1细胞中，分别加入或不含两种不同来源的俄勒冈葡萄根提取物(E_1和E_2)，分别进行~3H-环孢素A和~3H-地高辛转运实验。此外，通过实时定量聚合酶链式反应(RT-PCR)对Caco-2和LS-180细胞P-糖蛋白的调控机制进行了研究。结果：在Caco-2细胞中，俄勒冈葡萄根提取物(E_1和E_2)(0.1~1 mg/mL)以剂量依赖的方式抑制CsA和地高辛的外排。0.05 mg/mLE1可显著增加地高辛的吸收。10微米小檗碱和30微米小檗胺显著减少环孢素A的外排，而地高辛对小檗碱的影响不明显。在MDCKII-MDR1细胞中，10微米小檗碱和30微米小檗胺抑制环孢素A和地高辛的外流。在实时RT-PCR研究中，俄勒冈葡萄根提取物(0.1 mg/mL)在24小时上调Caco-2和LS-180细胞中人多药耐药基因mdr1的表达。结论：俄勒冈葡萄根提取物可调节P-糖蛋白，从而影响作为P-糖蛋白底物的药物的生物利用度。
Purpose: This study aims to investigate the potential of Oregon grape root extracts to modulate the activity of P-glycoprotein. Methods: We performed 3H-CsA or 3H-digoxin transport experiments in the absence or presence of two sources of Oregon grape root extracts (E1 and E2), berberine or berbamine in Caco-2 and MDCKII-MDR1 cells. In addition, real time quantitative polymerase chain reaction (RT-PCR) was performed in Caco-2 and LS-180 cells to investigate the mechanism of modulating P-glycoprotein. Results: Our results showed that in Caco-2 cells, Oregon grape root extracts (E1 and E2) (0.1–1 mg/mL) inhibited the efflux of CsA and digoxin in a dose-dependent manner. However, 0.05 mg/mL E1 significantly increased the absorption of digoxin. Ten µM berberine and 30 µM berbamine significantly reduced the efflux of CsA, while no measurable effect of berberine was observed with digoxin. In the MDCKII-MDR1 cells, 10 µM berberine and 30 µM berbamine inhibited the efflux of CsA and digoxin. Lastly, in real time RT-PCR study, Oregon grape root extract (0.1 mg/mL) up-regulated mRNA levels of human MDR1 in Caco-2 and LS-180 cells at 24 h. Conclusion: Our study showed that Oregon grape root extracts modulated P-glycoprotein, thereby may affect the bioavailability of drugs that are substrates of P-glycoprotein.
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