Effects of diosmin, a flavonoid glycoside in citrus fruits, on P-glycoprotein-mediated drug efflux in human intestinal Caco-2 cells.

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Yoo HH, Lee M, Chung HJ, Lee SK, Kim DH

Effects of diosmin, a flavonoid glycoside in citrus fruits, on P-glycoprotein-mediated drug efflux in human intestinal Caco-2 cells.

J Agric Food Chem. 2007 Sep 5;55(18):7620-5. doi: 10.1021/jf070893f. Epub 2007 Aug 4.

PubMed ID

17676865 [ View in PubMed

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Abstract

The effects of citrus flavonoids on P-glycoprotein (P-gp)-mediated drug efflux were examined in human intestinal Caco-2 cells. The cellular accumulation of rhodamine-123 was measured using 10 citrus flavonoids for preliminary screening. Among the flavonoids tested, diosmin significantly increased the accumulation of rhodamine-123 in Caco-2 cells. In the bidirectional transport of digoxin, diosmin increased the apical-to-basal (A-to-B) transport but decreased the basal-to-apical (B-to-A) transport in both concentration- and time-dependent manners. The digoxin transport ratio (B-A/A-B) was estimated to be 2.3 at a concentration of 50 microM of diosmin, which was significantly lower than the 15.2 found in the control. The apparent Ki values for P(app,A-B) and P(app,B-A) were 16.1 and 5.7 microM, respectively. These results demonstrated that diosmin effectively inhibited the P-gp-mediated efflux in Caco-2 cells. Diosmin is one of the main components in citrus fruits, and the intake of food supplements containing this compound may potentially increase the absorption of drugs able to act as P-gp substrates. The clinical relevance of this interaction should be further evaluated using in vivo experiments.

DrugBank Data that Cites this Article

Drug Transporters

Drug	Transporter	Kind	Organism	Pharmacological Action	Actions
Diosmin	P-glycoprotein 1	Protein	Humans	Unknown	Inhibitor	Details