Dreiseitel, A. and Oosterhuis, B. and Vukman, K. V. and Schreier, P. and Oehme, A. and Locher, S. and Hajak, G. and Sand, P. G. (2009) Berry anthocyanins and anthocyanidins exhibit distinct affinities for the efflux transporters BCRP and MDR1. BRITISH JOURNAL OF PHARMACOLOGY, 158 (8). pp. 1942-1950. ISSN 0007-1188,
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Background and purpose: Dietary anthocyanins hold great promise in the prevention of chronic disease but factors affecting their bioavailability remain poorly defined. Specifically, the role played by transport mechanisms at the intestinal and blood-brain barriers (BBB) is currently unknown. Experimental approach: In the present study, 16 anthocyanins and anthocyanidins were exposed to the human efflux transporters multidrug resistance protein 1 (MDR1) and breast cancer resistance protein (BCRP), using dye efflux, ATPase and, for BCRP, vesicular transport assays. Key results: All test compounds interacted with the BCRP transporter in vitro. Of these, seven emerged as potential BCRP substrates (malvidin, petunidin, malvidin-3-galactoside, malvidin-3,5-diglucoside, cyanidin-3-galactoside, peonidin-3-glucoside, cyanidin-3-glucoside) and 12 as potential inhibitors of BCRP (cyanidin, peonidin, cyanidin-3,5-diglucoside, malvidin, pelargonidin, delphinidin, petunidin, delphinidin-3-glucoside, cyanidin-3-rutinoside, malvidin-3-glucoside, pelargonidin-3,5-diglucoside, malvidin-3-galactoside). Malvidin, malvidin-3-galactoside and petunidin exhibited bimodal activities serving as BCRP substrates at low concentrations and, at higher concentrations, as BCRP inhibitors. Effects on MDR1, in contrast, were weak. Only aglycones exerted mild inhibitory activity. Conclusions and implications: Although the anthocyanidins under study may alter pharmacokinetics of drugs that are BCRP substrates, they are less likely to interfere with activities of MDR1 substrates. The present data suggest that several anthocyanins and anthocyanidins may be actively transported out of intestinal tissues and endothelia, limiting their bioavailability in plasma and brain.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | CANCER RESISTANCE PROTEIN; BLOOD-BRAIN-BARRIER; ABCG2 MULTIDRUG TRANSPORTER; P-GLYCOPROTEIN FUNCTION; CENTRAL-NERVOUS-SYSTEM; ATP-BINDING CASSETTE; IN-VITRO; DRUG-RESISTANCE; (ABCG2)-MEDIATED TRANSPORT; BLACKBERRY ANTHOCYANINS; anthocyanin; anthocyanidin; flavonoid; ABC transporter; MDR1; P-glycoprotein; BCRP |
| Subjects: | 600 Technology > 610 Medical sciences Medicine |
| Divisions: | Medicine > Lehrstuhl für Psychiatrie und Psychotherapie |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 27 Aug 2020 12:27 |
| Last Modified: | 27 Aug 2020 12:27 |
| URI: | https://pred.uni-regensburg.de/id/eprint/28004 |
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