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Planta Med 2013; 79(02): 137-141
DOI: 10.1055/s-0032-1328055
Pharmacokinetic Investigations
Letters
Georg Thieme Verlag KG Stuttgart · New York

In Vitro Inhibition of Cytochrome P450 3A4 by Aronia melanocarpa Constituents

Marie Bräunlich
1   School of Pharmacy, Department of Pharmaceutical Chemistry, University of Oslo, Blindern, Oslo, Norway
,
Hege Christensen
2   School of Pharmacy, Department of Pharmaceutical Biosciences, University of Oslo, Blindern, Oslo, Norway
,
Siri Johannesen
2   School of Pharmacy, Department of Pharmaceutical Biosciences, University of Oslo, Blindern, Oslo, Norway
,
Rune Slimestad
3   PlantChem, Særheim Research Center, Klepp Station, Norway
,
Helle Wangensteen
1   School of Pharmacy, Department of Pharmaceutical Chemistry, University of Oslo, Blindern, Oslo, Norway
,
Karl E. Malterud
1   School of Pharmacy, Department of Pharmaceutical Chemistry, University of Oslo, Blindern, Oslo, Norway
,
Hilde Barsett
1   School of Pharmacy, Department of Pharmaceutical Chemistry, University of Oslo, Blindern, Oslo, Norway
› Author Affiliations
Further Information

Publication History

received 26 September 2012
revised 07 November 2012

accepted 09 November 2012

Publication Date:
18 December 2012 (online)

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Abstract

Extracts, subfractions, isolated anthocyanins and procyanidins, and two phenolic acids from aronia [Aronia melanocarpa] were investigated for their CYP3A4 inhibitory effects, using midazolam as the probe substrate and recombinant insect cell microsomes expressing CYP3A4 as the enzyme source. Procyanidin B5 was a considerably stronger CYP3A4 inhibitor in vitro than the isomeric procyanidin B2 and comparable to bergamottin, a known CYP3A4 inhibitor from grapefruit juice. The inhibitory activity of proanthocyanidin-containing fractions was correlated to the degree of polymerization. Among the anthocyanins, cyanidin 3-arabinoside showed stronger CYP3A4 inhibition than cyanidin 3-galactoside and cyanidin 3-glucoside. Thus, the ability to inhibit CYP3A4 in vitro seems to be influenced by the sugar unit linked to the anthocyanidin.

Key words

Aronia melanocarpa – Rosaceae - anthocyanins - procyanidins - phenolic acids - cytochrome P450 3A4

Supporting Information

 

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