Effects of 5-fluorouracil on the drug-metabolizing enzymes of the small intestine and the consequent drug interaction with nifedipine in rats

Journal of Pharmacology and Experimental Therapeutics

Volumn 297, Issue 3, 2001, Pages 1166-1175

  Yoshisue, Kunihiro ^a   Nagayama, Sekio ^a   Shindo, Takashi ^a   Kawaguchi, Yasuro ^a  

^a TAIHO PHARMACEUTICAL CO LTD   (Japan)

Author keywords

[No Author keywords available]

Indexed keywords

1 CHLORO 2,4 DINITROBENZENE GLUTATHIONE TRANSFERASE; 4 METHYLUMBELLIFERONE GLUCURONYLTRANSFERASE; 5 CHLORO 2,4 DIHYDROXYPYRIDINE; CYTOCHROME P450 3A4; DRUG METABOLIZING ENZYME; ETHOXYRESORUFIN DEETHYLASE; FLUOROURACIL; GLUCURONOSYLTRANSFERASE; GLUTATHIONE TRANSFERASE; NIFEDIPINE; OXONATE POTASSIUM; REDUCED NICOTINAMIDE ADENINE DINUCLEOTIDE PHOSPHATE FERRIHEMOPROTEIN REDUCTASE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; CONTROLLED STUDY; DRUG BLOOD LEVEL; DRUG METABOLISM; ENZYME ACTIVITY; FIRST PASS EFFECT; GASTROINTESTINAL TOXICITY; INTESTINE MUCOSA; NONHUMAN; PRIORITY JOURNAL; PROTEIN CONTENT; RAT;

ADMINISTRATION, ORAL; ANIMALS; ANTIMETABOLITES, ANTINEOPLASTIC; BIOTRANSFORMATION; CALCIUM CHANNEL BLOCKERS; CYTOCHROME P-450 CYP1A1; CYTOCHROME P-450 ENZYME SYSTEM; DRUG INTERACTIONS; ENZYME ACTIVATION; ENZYME INHIBITORS; FLUOROURACIL; GLUCURONOSYLTRANSFERASE; GLUTATHIONE TRANSFERASE; IMMUNOBLOTTING; INTESTINAL MUCOSA; INTESTINE, SMALL; MALE; MICROSOMES; NADPH-FERRIHEMOPROTEIN REDUCTASE; NIFEDIPINE; OXONIC ACID; PENTOSYLTRANSFERASES; PYRIDINES; RATS; RATS, INBRED STRAINS; TEGAFUR;

EID: 0035007719     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (40)

1. Afsar A, Lee C and Riddick DS (1996) Modulation of the expression of constitutive rat hepatic cytochrome P450 isozymes by 5-fluorouracil. Can J Physiol Pharmacol 74:150-156.
2. Arlotto MP, Trant JM and Estabrook RW (1991) Measurement of steroid hydroxylation reactions by high-performance liquid chromatography as indicator of P450 identity and function. Methods Enzymol 206:454-462.
3. Bailey DG, Malcolm L, Arnold O and Spence JD (1998) Grapefruit juice - drug interactions. Br J Clin Pharmacol 46:101-110.
4. Barbounis VP, Kalofonos HP, Munro AJ, McKenzie CG, Sackier JM and Epenetos AA (1989) Treatment of colorectal cancer and other malignancies with continuous infusion of 5-fluorouracil. Anticancer Res 9:33-39.
5. Bradford M (1976) A rapid and sensitive method for the quantitation of microgram quantities of protein utilizing the principle of protein-dye binding. Anal Biochem 72:248-254.
6. Danenberg PV and Lockshin A (1982) Thymidylate synthetase - substrate complex formation. Mol Cell Biochem 43:49-57.
7. Edwards DJ, Fitzsimmons ME, Schuetz EG, Yasuda K, Ducharme MP, Warbasse LH, Woster PM, Schuetz JD and Watkins P (1999) 6′,7′-Dihydroxybergamottin in grapefruit juice and Seville orange juice: effects on cyclosporine disposition, enterocyte CYP3A4, and P-glycoprotein. Clin Pharmacol Ther 65:237-244.
8. Fukushima M, Shimamoto Y, Kato T, Uchida J, Yonekura R, Ohshimo H and Shirasaka T (1998) Anticancer activity and toxicity of S-1, an oral combination of tegafur and two biochemical modulators, compared with continuous i.v. infusion of 5-fluorouracil. Anticancer Drugs 9:817-823.
9. Grundy JS, Kherani R and Foster RT (1994a) Photostability determination of commercially available nifedipine oral dosage formulations. J Pharm Biomed Anal 12:1529-1535.
10. Grundy JS, Kherani R and Foster RT (1994b) Sensitive high-performance liquid chromatographic assay for nifedipine in human plasma utilizing ultraviolet detection. J Chromatogr B Biomed Appl 654:146-151.
11. Habig WH, Pabst MJ and Jakoby WB (1974) Glutathione S-transferases. The first enzymatic step in mercapturic acid formation. J Biol Chem 249:7130-7139.
12. Houghton JA, Houghton PJ and Wooten RS (1979) Mechanism of induction of gastrointestinal toxicity in the mouse by 5-fluorouracil and 5-fluoro-2′-deoxyuridine. Cancer Res 39:2406-2413.
13. Huan S, Pazdur R, Singhakowinta A, Samal B and Vaitkevicius VK (1989) Low-dose continuous infusion 5-fluorouracil. Evaluation in advanced breast carcinoma. Cancer 63:419-422.
14. Iatsimirskaia E, Tulebaev S, Storozhuk E, Utkin I, Smith D, Gerber N and Koudriakova T (1997) Metabolism of rifabutin in human enterocyte and liver microsomes: kinetic parameters, identification of enzyme systems, and drug interaction with macrolides and antifungal agents. Clin Pharmacol Ther 61:554-562.
15. Kolars JC, Awni WM, Merion RM and Watkins PB (1991) First-pass metabolism of cyclosporin by the gut. Lancet 338:1488-1490.
16. Laemmli UK (1970) Cleavage of structural proteins during the assembly of the head of bacteriophage T4. Nature (Lond) 227:680-685.
17. Lokich JJ, Ahlgren JD, Gullo JJ, Philips JA and Fryer JG (1989) A prospective randomized comparison of continuous infusion fluorouracil with a conventional bolus schedule in metastatic colorectal carcinoma: a mid-Atlantic oncology program study. J Clin Oncol 7:425-432.
18. Matsubara T, Otsubo S and Yoshihara E (1983) Liver microsomal cytochrome P-450-dependent O-dealkylation reaction in various animals. Jpn J Pharmacol 33:1065-1075.
19. McLeod HL, Sludden J, Hardy SC, Lock RE, Hawksworth GM and Cassidy J (1998) Autoregulation of 5-fluorouracil metabolism. Eur J Cancer 34:1623-1627.
20. Moynihan T, Hansen R, Anderson T, Quebbeman E, Beatty P, Ausman R, Ritch P, Chitambar C and Vukelich M (1988) Continuous 5-fluorouracil infusion in advanced gastric carcinoma. Am J Clin Oncol 11:461-464.
21. Murray M, Wilkinson CF and Dube CE (1983) Effects of dihydrosafrole on cytochrome P-450 and drug oxidation in hepatic microsomes from control and induced rats. Toxicol Appl Pharmacol 68:66-76.
22. Nakamura J, Takada S, Ohtsuka N, Heya T, Yamamoto A, Kimura T and Sezaki H (1983) An assessment of indomethacin-induced gastrointestinal mucosal damage in-vivo: enhancement of urinary recovery after oral administration of phenolsulfonphthalein in rats. J Pharm Pharmacol 35:369-372.
23. Paine MF, Khalighi M, Fisher JM, Shen DD, Kunze KL, Marsh CL, Perkins JD and Thummel KE (1997) Characterization of interintestinal and intraintestinal variations in human CYP3A-dependent metabolism. J Pharmacol Exp Ther 283:1552-1562.
24. Rich KJ, Sesardic D, Foster JR, Davies DS and Boobis AR (1989) Immunohistochemical localization of cytochrome P450b/e in hepatic and extrahepatic tissues of the rat. Biochem Pharmacol 38:3305-3322.
25. Sesardic D, Cole KJ, Edwards RJ, Davies DS, Thomas PE, Levin W and Boobis AR (1990) The inducibility and catalytic activity of cytochromes P450c (P450IA1) and P450d (P450IA2) in rat tissues. Biochem Pharmacol 39:499-506.
26. Shimada M, Murayama N, Yamazoe Y, Hashimoto H, Ishikawa H and Kato R (1995) Age- and sex-related alterations of microsomal drug- and testosterone-oxidizing cytochrome P450 in Sprague-Dawley strain-derived dwarf rats. J Pharmacol Exp Ther 275:972-977.
27. Shirasaka T, Shimamoto Y and Fukushima M (1993) Inhibition by oxonic acid of gastrointestinal toxicity of 5-fluorouracil without loss of its antitumor activity in rats. Cancer Res 53:4004-4009.
28. Shirasaka T, Shimamato Y, Ohshimo H, Yamaguchi M, Kato T, Yonekura K and Fukushima M (1996) Development of a novel form of an oral 5-fluorouracil derivative (S-1) directed to the potentiation of the tumor selective cytotoxicity of 5-fluorouracil by two biochemical modulators. Anticancer Drugs 7:548-557.
29. Stupans I, Richards DA and McClure MT (1995) Effects of 5-fluorouracil treatment on rat liver microsomal enzymes. Xenobiotica 25:1-8.
30. Tatsumi K, Fukushima M, Shirasaka T and Fujii S (1987) Inhibitory effects of pyrimidine, barbituric acid and pyridine derivatives on 5-fluorouracil degradation in rat liver extracts. Jpn J Cancer Res 78:748-755.
31. Towbin H, Staehelin T and Gordon J (1979) Electrophoretic transfer of proteins from polyacrylamide gels to nitrocellulose sheets: procedure and some applications. Proc Natl Acad Sci USA 76:4350-4354.
32. Ullman B and Kirsch J (1979) Metabolism of 5-fluorouracil in cultured cells. Protection from 5-fluorouracil cytotoxicity by purines. Mol Pharmacol 15:357-366.
33. van Laar JA, van der Wilt CL, Rustum YM, Noordhuis P, Smid K, Pinedo HM and Peter GJ (1996) Therapeutic efficacy of fluoropyrimidines depends on the duration of thymidylate synthase inhibition in the murine colon 26-B carcinoma tumor model. Clin Cancer Res 2:1327-1333.
34. Watkins PB, Wrighton SA, Schuetz EG, Molowa DT and Guzelian PS (1987) Identification of glucocorticoid-inducible cytochromes P-450 in the intestinal mucosa of rats and man. J Clin Invest 80:1029-1036.
35. Waxman DJ (1991) Rat hepatic P450IIA and P450IIC subfamily expression using catalytic, immunochemical, and molecular probes. Methods Enzymol 206:249-267.
36. Williams CH and Kamin H (1962) Microsomal triphosphopyridine nucleotide-cytochrome c reductase of liver. J Biol Chem 237:587-595.
37. Yoshisue K, Hironaga K, Yamaguchi Y, Yamamoto A, Nagayama S and Kawaguchi Y (2000a) Reduction of 5-fluorouracil (5-FU) gastrointestinal (GI) toxicity resulting from the protection of thymidylate synthase (TS) in GI tissue by repeated simultaneous administration of potassium oxonate (Oxo) in rats. Cancer Chemother Pharmacol 46:51-56.
38. Yoshisue K, Masuda H, Matsushima E, Ikeda K, Nagayama S and Kawaguchi Y (2000b) Tissue distribution and biotransformation of potassium oxonate after oral administration of a novel antitumor agent (drug combination of tegafur, 5-chloro-2,4-dihydroxypyridine, and potassium oxonate) to rats. Drug Metab Dispos 28: 1162-1167.
39. You L, Chan SK, Bruce JM, Archibeque-Engle S, Casanova M, Corton JC and Heck H (1999) Modulation of testosterone-metabolizing hepatic cytochrome P-450 enzymes in developing Sprague-Dawley rats following in utero exposure to p, p'-DDE Toxicol Appl Pharmacol 158:197-205.
40. Zhang QY, Wikoff J, Dunbar D and Kaminsky L (1996) Characterization of rat small intestinal cytochrome P450 composition and inducibility. Drug Metab Dispos 24: 322-328.