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흰쥐에서 나린진이 타목시펜의 약물동태에 미치는 영향

Effect of Naringin on Tamoxifen Pharmacokinetics in Rats

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Abstract

The aim of this study is to investigate the effect of naringin on the pharmacokinetics of tamoxifen in rats. Tamoxifen (10 mg/kg) was administered orally 0.5 h and 3 days after oral administration of naringin (5 mg/kg). The plasma concentrations of tamoxifen were increased significantly by naringin compared to control. Absorption rate constant (Ka) of tamoxifen with naringin was increased significantly compared to that of the control. The areas under the plasma concentration-time curve (AUC) and the peak concentrations (Cmax) of tamoxifen with naringin were significantly higher than those of the control. Consequently, the relative bioavailability (R.B%) of tamoxifen with naringin was 2-3-fold higher than the control, and absolute bioavailability (A.B%) of tamoxifen were significantly higher (p<0.05 with coadministration,p<0.01 with pretreatment) than those of the control. The increased bioavailability of tamoxifen in rats with naringin might be associated with the inhibition by naringin of an efflux pump P-glycoprotein and the first-pass metabolizing enzyme CYP3A4.

참고문헌 (39)

  1. Powles, "The case for clinical trials of tamoxifen forprevention of breast cancer", pp.1145~1147 (1992)
  2. I, "Use of tamoxifen for breast cancer", pp.513~529 (1995)
  3. Lim, "A comparative study of tamoxifenmetabolism in female rat", carci(genesis), pp.589~593 (1994)
  4. Mani, "Metabolism of the antimammary cancerantiestrogenic agent tamoxifen", pp.645~656 (1993)
  5. Mani, "Involvement of cytochrome P4503A in catalysis of tamoxifenactivation and covalent binding to rat and human livermicrosomes", carci(genesis), pp.2715~2720 (1994)
  6. Kangas, "Involvement of cytochrome P4503A enzyme family in the major metabolic pathways oftoremifene in human liver microsomes", drea
  7. Kupfer, "Cytochrome P-450 3A and2D6 catalyze ortho hydroxylation of 4-hydroxytamoxifenand 3-hydroxytamoxifen involvement of catechols in covalent binding tohepatic proteins", 27, pp.681~688 (1999)
  8. Mani, "Metabolism of the antimammary cancerantiestrogenic agent tamoxifen", pp.645~656 (1993)
  9. Crewe, "Variable contribution of cytochromes P450 2D6 2C9 and3A4 to the 4-hydroxylation of tamoxifen by human livermicrosomes", 53, pp.171~178 (1997)
  10. Daniel, "Determination of tamoxifen and biologicallyactive metabolites in human breast tumour and plasma", pp.1183~1189 (1981)
  11. Jordan, "A monohydroxylated metabolite of tamoxifen with potentantioestrogenic activity", endocri(l), pp.305~316 (1977)
  12. DeGregorio, "Tumor and serum tamoxifen concentrations in the athymicnude mice", pp.68~70 (1989)
  13. Robinson, "Implications of tamoxifen metabolism in the athymicmouse for the study of antitumor effects upon human breastcancer xenografts", pp.1769~1776 (1989)
  14. Gant, "In vivo induction of liver P-glycoproteinexpression by xenobiotics in monkeys", 133, pp.269~276 (1995)
  15. U, "substrates of the human Pglycoprotein", pp.287~292 (1994)
  16. Berman, "Effect of tamoxifenon cell lines displaying the multidrug-resistant phenotype", pp.818~825 (1991)
  17. Jacobson, "Effect of tamoxifen on themultidrug-resistant phenotype in human breast cancercells", pp.441~447 (1994)
  18. Hamada, "Cellular localization of themultidrug-resistance gene product P-glycoprotein in normalhuman tissues", pp.7735~7738 (1987)
  19. O'Brien, "is expressedby endothelial cells at blood-brain barrier sites", pp.695~698 (1989)
  20. I, "Tissue distribution of Pglycoproteinencoded by a multidrug-resistant gene asrevealed by a monoclonal antibody", pp.~16
  21. Gottesman, "Biochemistry of multidrugresistance mediated by the multidrug transporter", pp.385~427 (1993)
  22. Gan, "CYP3ALikecytochrome P450-mediated metabolism and polarizedefflux of cyclosporin A in Caco-2 cells interactionbetween the two biochemical barriers to intestinal transport", pp.344~349 (1996)
  23. Watkins, "The barrier function of CYP3A4 and Pglycoproteinin the small bowel", 27, pp.161~170 (1996)
  24. A, "Role of P-glycoprotein and cytochrome P450 3A in limitingoral absorption of peptides and peptidomimetics", pp.1322~1330 (1998)
  25. Ito, "Effects of intestinalCYP3A4 and P-glycoprotein on oral drug absorptiontheoretical approach", 16, pp.225~231 (1999)
  26. Miller, "P-glycoprotein expression inmalignant lymphoma and reversal of clinical drug resistancewith chemotherapy plus high-dose verapamil", pp.17~24 (1991)
  27. Wishart, "Adequate tumour quinidine levels formultidrug resistance modulation can be achieved in vivo", pp.28~31 (1992)
  28. A, "PhaseI", II trial of cyclosporine as a chemotherapy-resistance modifierin acute leukemia, 1993, 1652~1660
  29. A, "Flavonoids and isoflavonoidsgoldmine for metabolic engineering", pp.394~400 (1999)
  30. van Nood, "a review of probable mechanisms of action andpotential applications", flavo(ids), pp.418~425 (2001)
  31. Burke, "selective substrates and inhibitors for cytochrome P450CYP1A and CYP1B1", bioflavo(ids), pp.31~38 (2000)
  32. Dupuy, "Enhancement of moxidectin bioavailability inlamb by a natural flavonoid", 112, pp.337~347 (2003)
  33. A, "Increased oral bioavailability of paclitaxel by GF120918in mice through selective modulation of P-glycoprotein", (oijen), pp.4416~4421 (2000)
  34. Kim, "Intestinal bacterial metabolism of flavonoidsand its relation to some biological activities", pp.17~23 (1998)
  35. Zhang, "Effect of the grapefruit flavonoid naringin on pharmacokineticsof quinine in rats", 17, pp.351~363 (2000)
  36. Ho, "Inhibition ofhuman CYP3A4 activity by grapefruit flavonoids", fura(coumarinsand related compounds), pp.217~27 (2001)
  37. A, "Inhibition of vinblastine efflux mediated by P-glycoproteinby grapefruit juice components in caco-2 cells", 21, pp.1062~1066 (1998)
  38. A, "Inhibition of theCYP3A4-mediated metabolism and P-glycoprotein-mediatedtransport of the HIV-1 protease inhibitor saquinavirby grapefruit juice components", 48, pp.543~552 (1999)
  39. Fried, "Direct determination oftamoxifen and its four major metabolites in plasma usingcoupled column high-performance liquid chromatography", pp.261~268 (1994)

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