Effects of Diosmin, a Flavonoid Glycoside in Citrus Fruits, on P-Glycoprotein-Mediated Drug Efflux in Human Intestinal Caco-2 Cells

• DOI: 10.1021/jf070893f
• Publication Date: 2007-08-04T17:00:43Z
• Authors: Hye Hyun Yoo; Mijin Lee; Hye Jin Chung; Sang Kyu Lee; Dong-Hyun Kim
• Keywords: Diosmin; Efflux; Caco-2; P-glycoprotein

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