Identification of novel dietary phytochemicals inhibiting the efflux transporter breast cancer resistance protein (BCRP/ABCG2) |
| |
Authors: | Kee W. Tan Yan Li James W. Paxton Nigel P. Birch Arjan Scheepens |
| |
Affiliation: | 1. Food Innovation, The New Zealand Institute for Plant & Food Research Limited, Private Bag 92169, Auckland, New Zealand;2. Department of Pharmacology and Clinical Pharmacology, Faculty of Medical and Health Sciences, The University of Auckland, Private Bag 92019, Auckland, New Zealand;3. School of Biological Sciences, Faculty of Science, The University of Auckland, Private Bag 92019, Auckland, New Zealand;4. Centre for Brain Research, The University of Auckland, Private Bag 92019, Auckland, New Zealand |
| |
Abstract: | Breast cancer resistance protein (BCRP/ABCG2) plays an important role in determining the absorption and disposition of consumed xenobiotics including various drugs and dietary phytochemicals and is also one of the prominent efflux transporters involved in multidrug resistance (MDR). In this study, we have investigated the interactions between ABCG2 and 56 naturally-occurring phytochemicals including phenolic acids, flavonoids, triterpenes and other common dietary phytochemicals, as well as two non plant-based compounds (hippuric acid and propyl gallate) using cell- and membrane-based transport inhibition assays. Of the non-flavonoid phytochemicals tested, berberine, celastrol, ellagic acid, limonin, oleanolic acid, propyl gallate, sinapic acid and ursolic acid demonstrated significant inhibition of ABCG2-mediated transport. Chrysoeriol, laricitrin, myricetin 3′,4′,5′-trimethylether, pinocembrin, quercitrin, tamarixetin, tricetin and tricetin 3′,4′,5′-trimethylether were also identified as novel flavonoid ABCG2 inhibitors. The identified inhibitory activity of dietary phytochemicals on ABCG2 provides a framework for further investigation of ABCG2-modulated phytochemical bioavailability, MDR, and possible food–drug interactions. |
| |
Keywords: | ABC transporters Bioavailability Food&ndash drug interactions Multidrug resistance Polyphenols |
本文献已被 ScienceDirect 等数据库收录! |
|