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有机阴离子转运体在迷迭香酸药代动力学及药物相互作用中的作用

Involvement of Organic Anion Transporters in the Pharmacokinetics and Drug Interaction of Rosmarinic Acid.

作者信息

Kang Yun Ju, Lee Chul Haeng, Park Soo-Jin, Lee Hye Suk, Choi Min-Koo, Song Im-Sook

机构信息

College of Pharmacy and Research Institute of Pharmaceutical Sciences, Kyungpook National University, Daegu 41566, Korea.

College of Pharmacy, Dankook University, Cheonan 31116, Korea.

出版信息

Pharmaceutics. 2021 Jan 9;13(1):83. doi: 10.3390/pharmaceutics13010083.

DOI:10.3390/pharmaceutics13010083
PMID:33435470
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7828042/
Abstract

We investigated the involvement of drug transporters in the pharmacokinetics of rosmarinic acid in rats as well as the transporter-mediated drug interaction potential of rosmarinic acid in HEK293 cells overexpressing clinically important solute carrier transporters and also in rats. Intravenously injected rosmarinic acid showed bi-exponential decay and unchanged rosmarinic acid was mainly eliminated by urinary excretion, suggesting the involvement of transporters in its renal excretion. Rosmarinic acid showed organic anion transporter (OAT)1-mediated active transport with a K of 26.5 μM and a V of 69.0 pmol/min in HEK293 cells overexpressing OAT1, and the plasma concentrations of rosmarinic acid were increased by the co-injection of probenecid because of decreased renal excretion due to OAT1 inhibition. Rosmarinic acid inhibited the transport activities of OAT1, OAT3, organic anion transporting polypeptide (OATP)1B1, and OATP1B3 with IC values of 60.6 μM, 1.52 μM, 74.8 μM, and 91.3 μM, respectively, and the inhibitory effect of rosmarinic acid on OAT3 transport activity caused an in vivo pharmacokinetic interaction with furosemide by inhibiting its renal excretion and by increasing its plasma concentration. In conclusion, OAT1 and OAT3 are the major transporters that may regulate the pharmacokinetic properties of rosmarinic acid and may cause herb-drug interactions with rosmarinic acid, although their clinical relevance awaits further evaluation.

摘要

我们研究了药物转运体在迷迭香酸大鼠药代动力学中的作用，以及迷迭香酸在过表达临床重要溶质载体转运体的HEK293细胞和大鼠中转运体介导的药物相互作用潜力。静脉注射的迷迭香酸呈现双指数衰减，未变化的迷迭香酸主要通过尿液排泄消除，这表明转运体参与了其肾脏排泄过程。在过表达OAT1的HEK293细胞中，迷迭香酸表现出有机阴离子转运体（OAT）1介导的主动转运，其K值为26.5 μM，V值为69.0 pmol/min，由于OAT1抑制导致肾脏排泄减少，丙磺舒共注射使迷迭香酸的血浆浓度升高。迷迭香酸分别以60.6 μM、1.52 μM、74.8 μM和91.3 μM的IC值抑制OAT1、OAT3、有机阴离子转运多肽（OATP）1B1和OATP1B3的转运活性，迷迭香酸对OAT3转运活性的抑制作用通过抑制呋塞米的肾脏排泄并增加其血浆浓度，从而在体内与呋塞米产生药代动力学相互作用。总之，OAT1和OAT3是可能调节迷迭香酸药代动力学特性并可能导致迷迭香酸与草药-药物相互作用的主要转运体，尽管它们的临床相关性有待进一步评估。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9152/7828042/1433cdbb44f5/pharmaceutics-13-00083-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9152/7828042/0f0805f17005/pharmaceutics-13-00083-g001.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9152/7828042/1374f4e855ef/pharmaceutics-13-00083-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9152/7828042/21a5ad33c734/pharmaceutics-13-00083-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9152/7828042/1433cdbb44f5/pharmaceutics-13-00083-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9152/7828042/0f0805f17005/pharmaceutics-13-00083-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9152/7828042/e62297b3f7e3/pharmaceutics-13-00083-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9152/7828042/3f3ddf465e5a/pharmaceutics-13-00083-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9152/7828042/8b6ccc69bae7/pharmaceutics-13-00083-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9152/7828042/1374f4e855ef/pharmaceutics-13-00083-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9152/7828042/21a5ad33c734/pharmaceutics-13-00083-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9152/7828042/1433cdbb44f5/pharmaceutics-13-00083-g007.jpg

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