Yoo, Hye Hyun Lee, Mijin Chung, Hye Jin Lee, Sang Kyu Kim, Dong-Hyun 2024-01-21T00:32:10Z 2024-01-21T00:32:10Z 2021-08-31 2007-09-05 0021-8561 https://pubs.kist.re.kr/handle/201004/134110 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. English AMER CHEMICAL SOC HUMAN-LIVER-MICROSOMES GRAPEFRUIT JUICE ORANGE JUICE POLYMETHOXYLATED FLAVONES TRANSPORT ACTIVATION INHIBITION LINE BIOAVAILABILITY VINBLASTINE Effects of diosmin, a flavonoid glycoside in citrus fruits, on P-glycoprotein-mediated drug efflux in human intestinal Caco-2 cells Article 10.1021/jf070893f 1 JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY, v.55, no.18, pp.7620 - 7625 JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY 55 18 7620 7625 scie scopus 000249150900055 2-s2.0-34848835701 Agriculture, Multidisciplinary Chemistry, Applied Food Science & Technology Agriculture Chemistry Food Science & Technology Article HUMAN-LIVER-MICROSOMES GRAPEFRUIT JUICE ORANGE JUICE POLYMETHOXYLATED FLAVONES TRANSPORT ACTIVATION INHIBITION LINE BIOAVAILABILITY VINBLASTINE P-glycoprotein diosmin flavonoid citrus fruit Caco-2 cells