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.
Georg Thieme Verlag KG Stuttgart · New York.
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Animals
-
Anthocyanins / chemistry
-
Anthocyanins / isolation & purification
-
Anthocyanins / pharmacology*
-
Biflavonoids / chemistry
-
Biflavonoids / isolation & purification
-
Biflavonoids / pharmacology
-
Catechin / chemistry
-
Catechin / isolation & purification
-
Catechin / pharmacology
-
Cytochrome P-450 CYP3A
-
Cytochrome P-450 CYP3A Inhibitors*
-
Fruit / chemistry
-
Furocoumarins / pharmacology
-
Glycosylation
-
Humans
-
Hydroxybenzoates / chemistry
-
Hydroxybenzoates / isolation & purification
-
Hydroxybenzoates / pharmacology*
-
Inhibitory Concentration 50
-
Insecta
-
Microsomes
-
Midazolam / metabolism
-
Photinia / chemistry*
-
Plant Extracts / chemistry
-
Plant Extracts / isolation & purification
-
Plant Extracts / pharmacology
-
Proanthocyanidins / chemistry
-
Proanthocyanidins / isolation & purification
-
Proanthocyanidins / pharmacology*
Substances
-
Anthocyanins
-
Biflavonoids
-
Cytochrome P-450 CYP3A Inhibitors
-
Furocoumarins
-
Hydroxybenzoates
-
Plant Extracts
-
Proanthocyanidins
-
Catechin
-
Cytochrome P-450 CYP3A
-
CYP3A4 protein, human
-
phenolic acid
-
bergamottin
-
Midazolam
-
procyanidin B5