Development of rapid functional assay system of OATP and screening of OATP inhibitor contained in food and drink

2016 Fiscal Year Final Research Report

• Project/Area Number: 15K18930
• Research Category: Grant-in-Aid for Young Scientists (B)
• Allocation Type: Multi-year Fund
• Research Field: Medical pharmacy
• Research Institution: Kinjo Gakuin University (2016); Nagoya City University (2015)
• Principal Investigator: OHTA Kinya 金城学院大学, 薬学部, 准教授 (90448704)
• Project Period (FY): 2015-04-01 – 2017-03-31
• Keywords: OATP2B1 / トランスポーター / 5-carboxyfluorescein / 小腸 / 吸収 / スクリーニング / 薬物相互作用

Outline of Final Research Achievements

5-carboxyfluorescein (5-CF) was found to be a fluorescent probe substrate of OATP2B 1, and it was clarified that it can be used for the quick and simple functional evaluation of OATP2B1. We evaluated the effect of various beverages on OATP2B1 function using 5-CF, and revealed that coffee (extract) has potent and sustained inhibitory activity. As a causative substrate, chlorogenic acid, which is a coffee-containing component having the inhibitory activity like the extract solution, was suggested. These results suggest that caution is required for ingestion of coffee when taking medicine which is a substrate of OATP2B1.

Free Research Field

薬物動態学