525
Views
33
CrossRef citations to date
0
Altmetric
Reviews

The effects of flavonoids on the ABC transporters: consequences for the pharmacokinetics of substrate drugs

, PhD (Senior Lecturer) & , PhD (Associate-Professor)
Pages 267-285 | Published online: 06 Jan 2013

Bibliography

  • Hooper L, Kroon PA, Rimm EB, Flavonoids, flavonoid-rich foods, and cardiovascular risk: a meta-analysis of randomized controlled trials. Am J Clin Nutr 2008;88(1):38-50
  • Dembinska-Kiec A, Mykkanen O, Kiec-Wilk B, Antioxidant phytochemicals against type 2 diabetes. Br J Nutr 2008;99 E(Suppl 1):ES109-17
  • Surh YJ. Cancer chemoprevention with dietary phytochemicals. Nat Rev Cancer 2003;3(10):768-80
  • Aruoma OI, Bahorun T, Jen L-S. Neuroprotection by bioactive components in medicinal and food plant extracts. Mutat ResRev Mutat Res 2003;544(2-3):203-15
  • Zhou S, Gao Y, Jiang W, Interactions of herbs with cytochrome P450. Drug Metab Rev 2003;35(1):35-98
  • Li Y, Revalde JL, Reid G, Interactions of dietary phytochemicals with ABC transporters: possible implications for drug disposition and multidrug resistance in cancer. Drug Metab Rev 2010;42(4):590-611
  • Alvarez AI, Real R, Perez M, Modulation of the activity of ABC transporters (P-glycoprotein, MRP2, BCRP) by flavonoids and drug response. J Pharm Sci 2010;99(2):598-617
  • Petri N, Tannergren C, Holst B, Absorption/metabolism of sulforaphane and quercetin, and regulation of phase II enzymes, in human jejunum in vivo. Drug Metab Dispos 2003;31(6):805-13
  • Moon YJ, Wang X, Morris ME. Dietary flavonoids: effects on xenobiotic and carcinogen metabolism. Toxicol in vitro 2006;20(2):187-210
  • Brand W, Schutte ME, Williamson G, Flavonoid-mediated inhibition of intestinal ABC transporters may affect the oral bioavailability of drugs, food-borne toxic compounds and bioactive ingredients. Biomed Pharmacother 2006;60(9):508-19
  • Borst P, Elferink RO. Mammalian ABC transporters in health and disease. Annu Rev Biochem 2002;71:537-92
  • Faber KN, Muller M, Jansen PL. Drug transport proteins in the liver. Adv Drug Deliv Rev 2003;55(1):107-24
  • Shitara Y, Horie T, Sugiyama Y. Transporters as a determinant of drug clearance and tissue distribution. Eur J Pharm Sci 2006;27(5):425-46
  • Sarkadi B, Homolya L, Szakacs G, Human multidrug resistance ABCB and ABCG transporters: participation in a chemoimmunity defense system. Physiol Rev 2006;86(4):1179-236
  • Stanley LA, Horsburgh BC, Ross J, Drug transporters: gatekeepers controlling access of xenobiotics to the cellular interior. Drug Metab Rev 2009;41(1):27-65
  • Szakacs G, Paterson JK, Ludwig JA, Targeting multidrug resistance in cancer. Nat Rev Drug Discov 2006;5(3):219-34
  • Xia C, Smith PG. Drug efflux transporters and multidrug resistance in acute leukemia: therapeutic impact and novel approaches to mediation. Mol Pharmacol 2012;82(6):1008-21
  • Pietta PG. Flavonoids as antioxidants. J Nat Prod 2000;63(7):1035-42
  • Harborne JB, Williams CA. Advances in flavonoid research since 1992. Phytochemistry 2000;55(6):481-504
  • Ignat I, Stingu A, Volf I, Characterization of grape seed aqueous extract and possible applications in biological systems. Cellulose Chem Technol 2011;45(3-4):205-9
  • Havsteen BH. The biochemistry and medical significance of the flavonoids. Pharmacol Ther 2002;96(2-3):67-202
  • Walle T, Browning AM, Steed LL, Flavonoid glucosides are hydrolyzed and thus activated in the oral cavity in humans. J Nutr 2005;135(1):48-52
  • Hollman PC, Bijsman MN, van Gameren Y, The sugar moiety is a major determinant of the absorption of dietary flavonoid glycosides in man. Free Radic Res 1999;31(6):569-73
  • Hollman PC, de Vries JH, van Leeuwen SD, Absorption of dietary quercetin glycosides and quercetin in healthy ileostomy volunteers. Am J Clin Nutr 1995;62(6):1276-82
  • Walle T, Otake Y, Walle UK, Quercetin glucosides are completely hydrolyzed in ileostomy patients before absorption. J Nutr 2000;130(11):2658-61
  • Day AJ, Canada FJ, Diaz J. C, Dietary flavonoid and isoflavone glycosides are hydrolysed by the lactase site of lactase phlorizin hydrolase. FEBS Lett 2000;468(2-3):166-70
  • Chen J, Lin H, Hu M. Metabolism of flavonoids via enteric recycling: role of intestinal disposition. J Pharmacol Exp Ther 2003;304(3):1228-35
  • Li Y, Lu J, Paxton JW. The role of ABC and SLC transporters in the pharmacokinetics of dietary and herbal phytochemicals and their interactions with xenobiotics. Curr Drug Metab 2012;13(5):624-39
  • Lewis DF, Ito Y. Human cytochromes P450 in the metabolism of drugs: new molecular models of enzyme-substrate interactions. Expert Opin Drug Metab Toxicol 2008;4(9):1181-6
  • Lambert JD, Sang S, Yang CS. Biotransformation of green tea polyphenols and the biological activities of those metabolites. Mol Pharm 2007;4(6):819-25
  • Yang CS, Lambert JD, Ju J, Tea and cancer prevention: molecular mechanisms and human relevance. Toxicol Appl Pharmacol 2007;224(3):265-73
  • Janisch KM, Williamson G, Needs P, Properties of quercetin conjugates: modulation of LDL oxidation and binding to human serum albumin. Free Radic Res 2004;38(8):877-84
  • Zhang L, Zuo Z, Lin G. Intestinal and hepatic glucuronidation of flavonoids. Mol Pharm 2007;4(6):833-45
  • Lotsch J, Geisslinger G. Morphine-6-glucuronide: an analgesic of the future? Clin Pharmacokinet 2001;40(7):485-99
  • Kosoglou T, Statkevich P, Johnson-Levonas AO, Ezetimibe: a review of its metabolism, pharmacokinetics and drug interactions. Clin Pharmacokinet 2005;44(5):467-94
  • Suri S, Taylor MA, Verity A, A comparative study of the effects of quercetin and its glucuronide and sulfate metabolites on human neutrophil function in vitro. Biochem Pharmacol 2008;76(5):645-53
  • Day AJ, Bao Y, Morgan MR, Conjugation position of quercetin glucuronides and effect on biological activity. Free Radic Biol Med 2000;29(12):1234-43
  • O'Leary KA, Day AJ, Needs PW, Metabolism of quercetin-7- and quercetin-3-glucuronides by an in vitro hepatic model: the role of human beta-glucuronidase, sulfotransferase, catechol-O-methyltransferase and multi-resistant protein 2 (MRP2) in flavonoid metabolism. Biochem Pharmacol 2003;65(3):479-91
  • Shimoi K, Saka N, Nozawa R, Deglucuronidation of a flavonoid, luteolin monoglucuronide, during inflammation. Drug Metab Dispos 2001;29(12):1521-4
  • Giacomini KM, Huang SM, Tweedie DJ, Membrane transporters in drug development. Nat Rev Drug Discov 2010;9(3):215-36
  • Rees DC, Johnson E, Lewinson O. ABC transporters: the power to change. Nat Rev Mol Cell Biol 2009;10(3):218-27
  • Jones PM, George AM. The ABC transporter structure and mechanism: perspectives on recent research. Cell Mol Life Sci 2004;61(6):682-99
  • Higgins CF, Linton KJ. The ATP switch model for ABC transporters. Nat Struct Mol Biol 2004;11(10):918-26
  • Morris ME, Zhang S. Flavonoid-drug interactions: effects of flavonoids on ABC transporters. Life Sci 2006;78(18):2116-30
  • Zhang W, Tan TM, Lim LY. Impact of curcumin-induced changes in P-glycoprotein and CYP3A expression on the pharmacokinetics of peroral celiprolol and midazolam in rats. Drug Metab Dispos 2007;35(1):110-15
  • Shimabuku AM, Nishimoto T, Ueda K, P-glycoprotein. ATP hydrolysis by the N-terminal nucleotide-binding domain. J Biol Chem 1992;267(7):4308-11
  • Soldner A, Benet L, Mutschler E, Active transport of the angiotensin-II antagonist losartan and its main metabolite EXP 3174 across MDCK-MDR1 and Caco-2 cell monolayers. Br J Pharmacol 2000;129(6):1235-43
  • Gifford AJ, Kavallaris M, Madafiglio J, P-glycoprotein-mediated methotrexate resistance in CCRF-CEM sublines deficient in methotrexate accumulation due to a point mutation in the reduced folate carrier gene. Int J Cancer 1998;78(2):176-81
  • Thiebaut F, Tsuruo T, Hamada H, Cellular localization of the multidrug-resistance gene product P-glycoprotein in normal human tissues. Proc Natl Acad Sci USA 1987;84:7735-8
  • Cordon-Cardo C, O'Brein J, Casals D. Multidrug-resistance gene product (P-glycoprotein) is expressed by endothelial cells at blood-brain barrier sites. Proc Natl Acad Sci USA 1989;86:695-8
  • Ichikawa M, Yoshimura A, Sumizawa T, Interaction of organic chemicals with P-glycoprotein in the adrenal gland, kidney, and a multidrug-resistant KB cell. J Bio Chem 1991;266(2):903-8
  • Jodoin J, Demeule M, Beliveau R. Inhibition of the multidrug resistance P-glycoprotein activity by green tea polyphenols. Biochim Biophys Acta 2002;1542(1-3):149-59
  • Zhang S, Morris ME. Effect of the flavonoids biochanin A and silymarin on the P-glycoprotein-mediated transport of digoxin and vinblastine in human intestinal Caco-2 cells. Pharm Res 2003;20(8):1184-91
  • de Wet H, McIntosh DB, Conseil G, Sequence requirements of the ATP-binding site within the C-terminal nucleotide-binding domain of mouse P-glycoprotein: structure-activity relationships for flavonoid binding. Biochemistry (Mosc) 2001;40(34):10382-91
  • Conseil G, Baubichon-Cortay H, Dayan G, Flavonoids: a class of modulators with bifunctional interactions at vicinal ATP- and steroid-binding sites on mouse P-glycoprotein. Proc Natl Acad Sci USA 1998;95(17):9831-6
  • Zhang S, Morris ME. Effects of the flavonoids biochanin A, morin, phloretin, and silymarin on P-glycoprotein-mediated transport. J Pharmacol Exp Ther 2003;304(3):1258-67
  • Shapiro AB, Ling V. Positively cooperative sites for drug transport by P-glycoprotein with distinct drug specificities. Eur J Biochem 1997;250(1):130-7
  • Tran VH, Marks D, Duke RK, Modulation of P-glycoprotein-mediated anticancer drug accumulation, cytotoxicity, and ATPase activity by flavonoid interactions. Nutr Cancer 2011;63(3):435-43
  • Rumsby M, Drew L, Warr J. Protein kinases and multidrug resistance. Cytotechnology 1998;27(1-3):203-24
  • Mitsunaga Y, Takanaga H, Matsuo H, Effect of bioflavonoids on vincristine transport across blood-brain barrier. Eur J Pharmacol 2000;395(3):193-201
  • Doyle LA, Yang W, Abruzzo LV, A multidrug resistance transporter from human MCF-7 breast cancer cells. Proc Natl Acad Sci USA 1998;95(26):15665-70
  • Sarkadi B, Ozvegy-Laczka C, Nemet K, ABCG2 – a transporter for all seasons. FEBS Lett 2004;567(1):116-20
  • Jonker JW, Merino G, Musters S, The breast cancer resistance protein BCRP (ABCG2) concentrates drugs and carcinogenic xenotoxins into milk. Nat Med 2005;11(2):127-9
  • Dreiseitel A, Oosterhuis B, Vukman KV, Berry anthocyanins and anthocyanidins exhibit distinct affinities for the efflux transporters BCRP and MDR1. Br J Pharmacol 2009;158(8):1942-50
  • Imai Y, Tsukahara S, Asada S, Phytoestrogens/flavonoids reverse breast cancer resistance protein/ABCG2-mediated multidrug resistance. Cancer Res 2004;64(12):4346-52
  • Zhang SZ, Yang XN, Morris ME. Flavonoids are inhibitors of breast cancer resistance protein (ABCG2)-mediated transport. Mol Pharmacol 2004;65(5):1208-16
  • Cooray HC, Janvilisri T, van Veen HW, Interaction of the breast cancer resistance protein with plant polyphenols. Biochem Biophys Res Commun 2004;317(1):269-75
  • Zhang S, Yang X, Morris ME. Combined effects of multiple flavonoids on breast cancer resistance protein (ABCG2)-mediated transport. Pharm Res 2004;21(7):1263-73
  • Ebert B, Seidel A, Lampen A. Phytochemicals induce breast cancer resistance protein in Caco-2 cells and enhance the transport of benzo[a]pyrene-3-sulfate. Toxicol Sci 2007;96(2):227-36
  • An G, Gallegos J, Morris ME. The bioflavonoid kaempferol is an Abcg2 substrate and inhibits Abcg2-mediated quercetin efflux. Drug Metab Dispos 2011;39(3):426-32
  • Sim HM, Wu CP, Ambudkar SV, In vitro and in vivo modulation of ABCG2 by functionalized aurones and structurally related analogs. Biochem Pharmacol 2011;82(11):1562-71
  • Giri N, Agarwal S, Shaik N, Substrate-dependent breast cancer resistance protein (Bcrp1/Abcg2)-mediated interactions: consideration of multiple binding sites in in vitro assay design. Drug Metab Dispos 2009;37(3):560-70
  • Ejendal KFK, Hrycyna CA. Differential sensitivities of the human ATP-binding cassette transporters ABCG2 and P-glycoprotein to cyclosporin A. Mol Pharmacol 2005;67(3):902-11
  • Xia CQ, Liu N, Miwa GT, Interactions of Cyclosporin A with breast cancer resistance protein. Drug Metab Dispos 2007;35(4):576-82. dmd.106.011866
  • Zhang S, Yang X, Coburn RA, Structure activity relationships and quantitative structure activity relationships for the flavonoid-mediated inhibition of breast cancer resistance protein. Biochem Pharmacol 2005;70(4):627-39
  • Borst P, de Wolf C, van de Wetering K. Multidrug resistance-associated proteins 3, 4, and 5. Pflugers Arch 2007;453(5):661-73
  • Cole SPC, Bhardwaj G, Gerlach JH, Overexpression of a transporter gene in a multidrug-resistant human lung cancer cell line. Science 1992;258:1650-4
  • Cherrington NJ, Hartley DP, Li N, Organ distribution of multidrug resistance proteins 1, 2, and 3 (mrp1, 2, and 3) mRNA and hepatic induction of mrp3 by constitutive androstane receptor activators in rats. J Pharmacol Exp Ther 2002;300(1):97-104
  • Kavallaris M. The role of multidrug resistance-associated protein (MRP) expression in multidrug resistance. Anticancer Drugs 1997;8:17-25
  • Borst P, Evers R, Kool M, A family of drug transporters: the multidrug resistance-associated proteins. J Nat Cancer Inst. 2000;92(16):1295-302
  • Cullen KV, Davey RA, Davey MW. Verapamil-stimulated glutathione transport by the multidrug resistance-associated protein (MRP1) in leukaemia cells. Biochem Pharm 2001;62(4):417-24
  • Borst P, Zelcer N, van de Wetering K, On the putative co-transport of drugs by multidrug resistance proteins. FEBS Lett 2006;580(4):1085-93
  • Versantvoort CH, Rhodes T, Twentyman PR. Acceleration of MRP-associated efflux of rhodamine 123 by genistein and related compounds. Br J Cancer 1996;74(12):1949-54
  • Leslie EM, Mao Q, Oleschuk CJ, Modulation of multidrug resistance protein 1 (MRP1/ABCC1) transport and ATPase activities by interaction with dietary flavonoids. Mol Pharmacol 2001;59(5):1171-80
  • van Zanden JJ, Wortelboer HM, Bijlsma S, Quantitative structure activity relationship studies on the flavonoid mediated inhibition of multidrug resistance proteins 1 and 2. Biochem Pharmacol 2005;69(4):699-708
  • Trompier D, Baubichon-Cortay H, Chang XB, Multiple flavonoid-binding sites within multidrug resistance protein MRP1. Cell Mol Life Sci 2003;60(10):2164-77
  • Leslie EM, Deeley RG, Cole SP. Bioflavonoid stimulation of glutathione transport by the 190-kDa multidrug resistance protein 1 (MRP1). Drug Metab Dispos 2003;31(1):11-15
  • Nguyen H, Zhang S, Morris ME. Effect of flavonoids on MRP1-mediated transport in Panc-1 cells. J Pharm Sci 2003;92(2):250-7
  • Cui Y, Konig J, Buchholz JK, Drug resistance and ATP-dependent conjugate transport mediated by the apical multidrug resistance protein, MRP2, permanently expressed in human and canine cells. Mol Pharmacol 1999;55:929-37
  • Konig J, Nies AT, Cui Y, Conjugate export pumps of the multidrug resistance protein (MRP) family: localization, substrate specificity, and MRP2-mediated drug resistance. Biochim Biophys Acta 1999;1461(2):377-94
  • Borst P, Zelcer N, van de Wetering K. MRP2 and 3 in health and disease. Cancer Lett 2006;234(1):51-61
  • Ishikawa T, Bao J, Yamane Y, Coordinated induction of MRP/GS-X pump and gamma-glutamylcysteine synthetase by heavy metals in human leukemia cells. J Bio Chem 1996;271(25):14981-8
  • van Zanden JJ, de Mul A, Wortelboer HM, Reversal of in vitro cellular MRP1 and MRP2 mediated vincristine resistance by the flavonoid myricetin. Biochem Pharmacol 2005;69(11):1657-65
  • Aszalos A. Role of ATP-binding cassette (ABC) transporters in interactions between natural products and drugs. Curr Drug Metab 2008;9(10):1010-18
  • Gan LS, Moseley MA, Khosla B, CYP3A-like cytochrome P450-mediated metabolism and polarized efflux of cyclosporin A in Caco-2 cells. Drug Metab Dispos 1996;24(3):344-9
  • Watkins PB. The barrier function of CYP3A4 and P-glycoprotein in the small bowel. Adv Drug Deliv Rev 1997;27(2-3):161-70
  • Kim KA, Park PW, Park JY. Short-term effect of quercetin on the pharmacokinetics of fexofenadine, a substrate of P-glycoprotein, in healthy volunteers. Eur J Clin Pharmacol 2009;65(6):609-14
  • Mitsunaga Y, Takanaga H, Matsuo H, Effect of bioflavonoids on vincristine transport across blood-brain barrier. Eur J Pharmacol 2000;395(3):193-201
  • Choi JS, Choi HK, Shin SC. Enhanced bioavailability of paclitaxel after oral coadministration with flavone in rats. Int J Pharm 2004;275(1-2):165-70
  • Choi JS, Shin SC. Enhanced paclitaxel bioavailability after oral coadministration of paclitaxel prodrug with naringin to rats. Int J Pharm 2005;292(1-2):149-56
  • Choi JS, Jo BW, Kim YC. Enhanced paclitaxel bioavailability after oral administration of paclitaxel or prodrug to rats pretreated with quercetin. Eur J Pharm Biopharm 2004;57(2):313-18
  • Li X, Yun JK, Choi JS. Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos 2007;28(3):151-6
  • Lim SC, Choi JS. Effects of naringin on the pharmacokinetics of intravenous paclitaxel in rats. Biopharm Drug Dispos 2006;27(9):443-7
  • Fuhr U, Klittich K, Staib AH. Inhibitory effect of grapefruit juice and its bitter principal, naringenin, on CYP1A2 dependent metabolism of caffeine in man. Br J Clin Pharmacol 1993;35(4):431-6
  • Ho PC, Saville DJ, Wanwimolruk S. Inhibition of human CYP3A4 activity by grapefruit flavonoids, furanocoumarins and related compounds. J Pharm Pharm Sci 2001;4(3):217-27
  • Cermak R, Wolffram S. The potential of flavonoids to influence drug metabolism and pharmacokinetics by local gastrointestinal mechanisms. Curr Drug Metab 2006;7(7):729-44
  • Pal D, Mitra AK. MDR- and CYP3A4-mediated drug-herbal interactions. Life Sci 2006;78(18):2131-45
  • Kawashiro T, Yamashita K, Zhao XJ, A study on the metabolism of etoposide and possible interactions with antitumor or supporting agents by human liver microsomes. J Pharmacol Exp Ther 1998;286(3):1294-300
  • Wang YH, Chao PD, Hsiu SL, Lethal quercetin-digoxin interaction in pigs. Life Sci 2004;74(10):1191-7
  • Taipalensuu J, Tornblom H, Lindberg G, Correlation of gene expression of ten drug efflux proteins of the ATP-binding cassette transporter family in normal human jejunum and in human intestinal epithelial Caco-2 cell monolayers. J Pharmacol Exp Ther 2001;299(1):164-70
  • Maliepaard M, Scheffer GL, Faneyte IF, Subcellular localization and distribution of the breast cancer resistance protein transporter in normal human tissues. Cancer Res 2001;61(8):3458-64
  • Zimmermann C, Gutmann H, Hruz P, Mapping of multidrug resistance gene 1 and multidrug resistance-associated protein isoform 1 to 5 mRNA expression along the human intestinal tract. Drug Metab Dispos 2005;33(2):219-24
  • Englund G, Rorsman F, Ronnblom A, Regional levels of drug transporters along the human intestinal tract: co-expression of ABC and SLC transporters and comparison with Caco-2 cells. Eur J Pharm Sci 2006;29(3-4):269-77
  • Gutmann H, Hruz P, Zimmermann C, Distribution of breast cancer resistance protein (BCRP/ABCG2) mRNA expression along the human GI tract. Biochem Pharmacol 2005;70(5):695-9
  • Jonker JW, Buitelaar M, Wagenaar E, The breast cancer resistance protein protects against a major chlorophyll-derived dietary phototoxin and protoporphyria. Proc Natl Acad Sci USA 2002;99(24):15649-54
  • Jia X, Chen J, Lin H, Disposition of flavonoids via enteric recycling: enzyme-transporter coupling affects metabolism of biochanin A and formononetin and excretion of their phase II conjugates. J Pharmacol Exp Ther 2004;310(3):1103-13
  • Zhang S, Sagawa K, Arnold RD, Interactions between the flavonoid biochanin A and P-glycoprotein substrates in rats: in vitro and in vivo. J Pharm Sci 2010;99(1):430-41
  • Li X, Choi JS. Effect of genistein on the pharmacokinetics of paclitaxel administered orally or intravenously in rats. Int J Pharm 2007;337(1-2):188-93
  • Dresser GK, Bailey DG, Leake BF, Fruit juices inhibit organic anion transporting polypeptide-mediated drug uptake to decrease the oral availability of fexofenadine. Clin Pharmacol Ther 2002;71(1):11-20
  • Bailey DG. Fruit juice inhibition of uptake transport: a new type of food-drug interaction. Br J Clin Pharmacol 2011;70(5):645-55
  • Wang X, Wolkoff AW, Morris ME. Flavonoids as a novel class of human organic anion-transporting polypeptide OATP1B1 (OATP-C) modulators. Drug Metab Dispos 2005;33(11):1666-72
  • Wong CC, Botting NP, Orfila C, Flavonoid conjugates interact with organic anion transporters (OATs) and attenuate cytotoxicity of adefovir mediated by organic anion transporter 1 (OAT1/SLC22A6). Biochem Pharmacol 2011;81(7):942-9
  • Zhang S, Yang X, Morris ME. Flavonoids are inhibitors of breast cancer resistance protein (ABCG2)-mediated transport. Mol Pharmacol 2004;65(5):1208-16
  • Sesink AL, Arts IC, de Boer VC, Breast cancer resistance protein (Bcrp1/Abcg2) limits net intestinal uptake of quercetin in rats by facilitating apical efflux of glucuronides. Mol Pharmacol 2005;67(6):1999-2006
  • Imai Y, Asada S, Tsukahara S, Breast cancer resistance protein exports sulfated estrogens but not free estrogens. Mol Pharmacol 2003;64(3):610-18
  • An G, Morris ME. The sulfated conjugate of biochanin A is a substrate of breast cancer resistant protein (ABCG2). Biopharm Drug Dispos 2011;32(8):446-57
  • Wang X, Morris ME. Effects of the flavonoid chrysin on nitrofurantoin pharmacokinetics in rats: potential involvement of ABCG2. Drug Metab Dispos 2007;35(2):268-74
  • Lee YJ, Kusuhara H, Jonker JW, Investigation of efflux transport of dehydroepiandrosterone sulfate and mitoxantrone at the mouse blood-brain barrier: a minor role of breast cancer resistance protein. J Pharmacol Exp Ther 2005;312(1):44-52
  • Enokizono J, Kusuhara H, Sugiyama Y. Effect of breast cancer resistance protein (bcrp/abcg2) on the disposition of phytoestrogens. Mol Pharmacol 2007;72(4):967-75
  • Shukla S, Zaher H, Hartz A, Curcumin inhibits the activity of ABCG2/BCRP1, a multidrug resistance-linked ABC drug transporter in mice. Pharm Res 2009;26(2):480-7
  • Jonker JW, Smit JW, Brinkhuis RF, Role of breast cancer resistance protein in the bioavailability and fetal penetration of topotecan. J Natl Cancer Inst 2000;92(20):1651-6
  • Evseenko DA, Paxton JW, Keelan JA. ABC drug transporter expression and functional activity in trophoblast-like cell lines and differentiating primary trophoblast. Am J Physiol Regul Integr Comp Physiol 2006;290(5):R1357-65
  • Merino G, Jonker JW, Wagenaar E, The breast cancer resistance protein (BCRP/ABCG2) affects pharmacokinetics, hepatobiliary excretion, and milk secretion of the antibiotic nitrofurantoin. Mol Pharmacol 2005;67(5):1758-64
  • van Zanden JJ, van der Woude H, Vaessen J, The effect of quercetin phase II metabolism on its MRP1 and MRP2 inhibiting potential. Biochem Pharmacol 2007;74(2):345-51
  • Jager W, Gehring E, Hagenauer B, The role of hepatic Mrp2 in the interaction of flavopiridol and bilirubin: impact on therapy. Int J Clin Pharmacol Ther 2003;41(12):610-11
  • Spahn-Langguth H, Langguth P. Grapefruit juice enhances intestinal absorption of the P-glycoprotein substrate talinolol. Eur J Pharm Sci 2001;12(4):361-7
  • De Castro WV, Mertens-Talcott S, Derendorf H, Effect of grapefruit juice, naringin, naringenin, and bergamottin on the intestinal carrier-mediated transport of talinolol in rats. J Agric Food Chem 2008;56(12):4840-5
  • Shirasaka Y, Li Y, Shibue Y, Concentration-dependent effect of naringin on intestinal absorption of β1-adrenoceptor antagonist talinolol mediated by P-glycoprotein and organic anion transporting polypeptide (Oatp). Pharm Res 2009;26(3):560-7
  • Schwarz UI, Seemann D, Oertel R, Grapefruit juice ingestion significantly reduces talinolol bioavailability. Clin Pharmacol Ther 2005;77(4):291-301
  • Becquemont L, Verstuyft C, Kerb R, Effect of grapefruit juice on digoxin pharmacokinetics in humans. Clin Pharmacol Ther 2001;70(4):311-16
  • Dresser GK, Bailey DG. The effects of fruit juices on drug disposition: a new model for drug interactions. Eur J Clin Invest 2003;33:10-16
  • Kamath AV, Ming Y, Zhang YP, Effect of fruit juices on the oral bioavailability of fexofenadine in rats. J Pharm Sci 2005;94(2):233-9
  • Banfield C, Gupta S, Marino M, Grapefruit juice reduces the oral bioavailability of fexofenadine but not desloratadine. Clin Pharmacokinet 2002;41(4):311-18
  • Park JH, Hur HJ, Woo JS, Effects of silymarin and formulation on the oral bioavailability of paclitaxel in rats. European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences. 2012;45(3):296-301
  • Bansal T, Awasthi A, Jaggi M, Pre-clinical evidence for altered absorption and biliary excretion of irinotecan (CPT-11) in combination with quercetin: possible contribution of P-glycoprotein. Life Sci 2008;83(7-8):250-9
  • Li C, Choi JS. Effects of epigallocatechin gallate on the bioavailability and pharmacokinetics of diltiazem in rats. Pharmazie 2008;63(11):815-18
  • Edwards DJ, Fitzsimmons ME, Schuetz EG, 6',7'-Dihydroxybergamottin in grapefruit juice and Seville orange juice: effects on cyclosporine disposition, enterocyte CYP3A4, and P-glycoprotein. Clin Pharmacol Ther 1999;65:237-44
  • Mols R, Deferme S, Augustijns P. Sulfasalazine transport in in-vitro ex-vivo and in-vivo absorption models: contribution of efflux carriers and their modulation by co-administration of synthetic nature-identical fruit extracts. J Pharm Pharmacol 2005;57(12):1565-73
  • Kusuhara H, Furuie H, Inano A, Pharmacokinetic interaction study of sulfasalazine in healthy subjects and the impact of curcumin as an in vivo inhibitor of BCRP. Br J Pharmacol 2012;166(6):1793-803
  • Moon YJ, Morris ME. Pharmacokinetics and bioavailability of the bioflavonoid biochanin A: effects of quercetin and EGCG on biochanin A disposition in rats. Mol Pharm 2007;4(6):865-72
  • Zhang S, Wang X, Sagawa K, Flavonoids chrysin and benzoflavone, potent breast cancer resistance protein inhibitors, have no significant effect on topotecan pharmacokinetics in rats or mdr1a/1b (-/-) mice. Drug Metab Dispos 2005;33(3):341-8
  • An G, Morris ME. Effects of the isoflavonoid biochanin A on the transport of mitoxantrone in vitro and in vivo. Biopharm Drug Dispos 2010;31(5-6):340-50
  • An G, Wu F, Morris ME. 5,7-Dimethoxyflavone and multiple flavonoids in combination alter the ABCG2-mediated tissue distribution of mitoxantrone in mice. Pharm Res 2011;28(5):1090-9

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.