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

Title
Effects of diosmin, a flavonoid glycoside in citrus fruits, on P-glycoprotein-mediated drug efflux in human intestinal Caco-2 cells
Author
유혜현
Keywords
P-glycoprotein; diosmin; flavonoid; citrus fruit; Caco-2 cells
Issue Date
2007-09
Publisher
AMER CHEMICAL SOC
Citation
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY, v. 55, No. 18, Page. 7620-7625
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 mu M of diosmin, which was significantly lower than the 15.2 found in the control. The apparent K-i values for P-app,P-A-B and P-app,P-B-A were 16.1 and 5.7 mu m, 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.
URI
https://pubs.acs.org/doi/abs/10.1021/jf070893fhttps://repository.hanyang.ac.kr/handle/20.500.11754/106931
ISSN
0021-8561; 1520-5118
DOI
10.1021/jf070893f
Appears in Collections:
COLLEGE OF PHARMACY[E](약학대학) > PHARMACY(약학과) > Articles
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