Effects of morin pretreatment on the pharmacokinetics of diltiazem and its major metabolite, desacetyldiltiazem in rats

Archives of Pharmacal Research

Volumn 28, Issue 8, 2005, Pages 970-976

  Hyun, Jin Choi ^a   Choi, Jun Shik ^b  

^a Chonnam National University   (South Korea)

^b Chosun University   (South Korea)

Author keywords

CYP3A4; Desacetyldiltiazem; Diltiazem; Morin; Pharmacokinetics; Rat

Indexed keywords

EID: 30644465031     PISSN: 02536269     EISSN: 02536269     Source Type: Journal    
DOI: 10.1007/bf02973885     Document Type: Article

References (43)

1. Bhattacharya, R. K. and Firozi, P. F., Effect of plant flavonoids on microsome catalyzed reactions of aflatoxin B1 leading to activation and DNA adduct formation. Cancer Letter, 39, 85-91 (1988).
2. Buckley, M. M.- T., Grant, S. M., Goa, K. L., McTabish, D., and Sorkin, E. M., Diltiazem: A reappraisal of its pharmacological properties and therapeutic use. Drugs, 39, 757-806 (1990).
3. Na, J. H. and Choi, J. S., Effect of naringin on the pharmacokinetics of nifedifine in rabbits. J.Kor. Pharm. Sci., 35, 101-106 (2005).
4. Chaffman, M. and Brogden, R. N., Diltiazem: a review of its pharmacological properties and therapeutic efficacy. Drugs, 29, 387-454 (1985).
5. Choi, J. S., Choi, B. C., and Choi, K. E., Effect of quercetin on the pharmacokinetics of oral cyclosporine. Am. J. Health Syst. Pharm., 61, 2406-2409 (2004).
6. Choi, J. S., Jo, B. W., and Kim, Y. C., Enhanced paclitaxel bioavailability after oral administration of paclitaxel or prodrug to rats pretreated with quercetin. Eur. J. Pharm. Biopharm., 57, 313-318 (2004).
7. Choi, J. S. and Han, H. K., The effect of quercetin on the pharmacokinetics of verapamil and its major metabolite, norverapamil, in rabbits. J. Pharm. Pharmacol., 56,1537-1542 (2004).
8. Choi, J. S. and Shin, S. C., Enhanced paclitaxel bioavailability after oral coadministration of paclitaxel prodrug with naringin to rats. Int. J. Pharm., 292, 149-156 (2005).
9. Dixon, R. A. and Steele, C. L., Flavonoids andisoflavonoids-a gold mine for metabolic engineering. Trends Plant Sci., 4, 394-400 (1999).
10. Dupuy, J., Larrieu, G., Sutra, J. F., Lespine, A., and Alvinerie, M., Enhancement of moxidectin bioavailability in lamb by a natural flavonoid: quercetin. Vet. Parasitol., 112, 337-347 (2003).
11. Fang, S. H., Hou, Y. C., Chang, W. C., Hsiu, S. L., Chao P. D., and Chiang, B. L., Morin sulfates/glucuronides exert antiinflammatory activity on activated macrophages and decreased the incidence of septic shock. Life Sci., 74, 743-756 (2003).
12. Fraile, L. J., Aramayona, J. J., Bregante, M. A., Garcia, M. A., and Aradia, A. R., Deacetylation of diltiazem by several rabbit tissues. Pharm. Res., 13. 1875-1880 (1996).
13. Francis, A. R., Shetty, T. K., and Bhattacharya, R. K., Modulating effect of plant flavonoids on the mutagenicity of N-methyl-N-nitro-N-nitrosoguanidine. Carcinogenesis, 10, 1953-1955 (1989).
14. Goebel, K. J. and Kolle, E. U., High performance liquid chromatographic dertermination of diltiazem and four of its metabolites in plasma. J. Chromatogr., 345, 355-363 (1985).
15. Gottesman, M. M. and Pastan, I., Biochemistry of multidrug resistance mediated by the multidrug transporter. Annu. Rev. Biochem., 62, 385-427 (1993).
16. Hanasaki, Y., Ogawa S., and Fukui, S., The correlation between active oxygens scavenging and antioxidative effects of flavonoids. Free Radic. Biol. Med., 16, 845-850 (1994).
17. Han, H. K. and Choi, J. S., Enhanced diltiazem bioavailability after oral administration of diltiazem with naringin in rats. Int. J. Pharm., Submitted for publication (2005).
18. Hodek, P., Trefil, P., and Stiborova, M., Flavonoids-potent and versaltile biologically active compounds interacting with cytochromes P450. Chem..Biol. interact., 139, 1-21 (2002).
19. Homsy, W., Caille, G., and du Souich, P., The site of absorption in the small intestine determines diltiazem bioavailability in the rabbit. Pharm. Res., 12, 1722-1726 (1995a).
20. Homsy, W., Lefebvre, M., Caille, G., and du Souich, P., Metabolism of diltiazem in hepatic and extrahepatic tissues of rabbits: in vitro studies. Pharm. Res., 12, 609-614 (1995b).
21. Kim, H. K., Cheon, B. S., Kim, Y. H., Kim S. Y., and Kim, H. P., Effects of naturally occurring flavonoids on nitric oxide production in the macrophage cell line RAW 264.7 and their structure-activity relationships. Biochem. Pharmacol., 58, 759-765 (1999).
22. Kim, H. S., Choi, J. S., and Choi, I., Effect of naringin on tamoxifen pharmacokinetics in rats. Kor. J. Clin. Pharm., 15, 55-60 (2005).
23. Kim, H. J. and Choi, J. S., Effect of pretreatmemt of naringin on the bioavailability of diltiazem and deacetylditiazem in rabbits. Yakhak Hoeji, 49, 230-236 (2005).
24. Kok, L. D., Wong, Y. P., Wu, T. W., Chan, H. C., Kwok, T. T., and Fung, K. P., Morin hydrate: a potential antioxidant in minimizing the free-radicals-mediated damage to cardiovascular cells by anti-tumor drugs. Life Sci., 67, 91-99 (2000).
25. Kolars, J. C., Schmiedlin-Ren, P., Dobbins, W. O. 3rd, Schuetz, J., Wrighton, S. A., and Watkins, P. B., Heterogeneity of cytochrome P450IIIA expression in rat gut epithelia. Gastroenterology, 102, 1186-1198 (1992).
26. Lefebvre, M., Homsy, W., Caille, G., and du Souich, P., Firstpass metabolism of diltiazem in anesthetized rabbits: role of extrahepatic organs. Pharm. Res.,13, 124-128 (1996).
27. Li, X. and Choi, J. S., Enhanced diltiazem bioavailability after oral administration of diltiazem with quercetin to rabbits. Int. J. Pharm., 297,1-8 (2005).
28. Molden, E., Asberg, A., and Christensen, H., CYP2D6 is involved in O-demethylation of diltiazem-an in vitro study with transfected human liver cells. Eur. J. Clin. Pharmacol., 56, 575-579 (2000a).
29. Molden, E., Christensen, H., and Sund, R. B., Extensive metabolism of diltiazem and P-glycoprotein-mediated efflux of desacetyl-diltiazem (M1) by rat jejunum in vitro. Drug Metab. Dispos., 28, 107-109 (2000b).
30. Nguyen, H., Zhang, S., and Morris, M. E., Effect of flavonoids on MRP1-mediated transport in Panc-1 cells. J. Pharm. Sci.,92, 250-257 (2003).
31. Pichard, L. G., Gillet, G., Fabre, I., Dalet-Beluche, I., Bonfils, C., and Thenot, J. P., et al., Identification of the rabbit and human cytochromes P-450IIIA as the major enzymes involved in the N-demethylation of diltiazem. Drug Metab. Dispos.,18, 711-719 (1990).
32. Pool, P. E., Diltiazem. In: F. H. Messerli Editor, Cardiovascular Drug Therapy (2nd ed.) Saunders Philadelphia, pp. 931-971, (1996).
33. Ramanathan, L., Das, N. P., and Li, Q. T., Studies on lipid oxidation in fish phospholipid liposomes. Biol. Trace Elem. Res., 40, 59-70 (1994).
34. Raso, G.M., Meli, R., Di Carlo, G., Pacilio, M., and Di Carlo, R., Inhibition of inducible nitric oxide synthase and cyclooxygenase-2 expression by flavonoids in macrophage J774A.1. Life Sci., 68, 921-931 (2001).
35. Rocci, M.L. and Jusko, W.J., LAGRAN program for area and moments in pharmacokinetic analysis. Computer Programs in Biomedicine, 16, 203 (1983).
36. Saeki, T., Ueda, K., Tanigawara, Y., Hori, R., and Komano,T., P-glycoprotein-mediated transcellular transport of MDR-reversing agents. FEBS Lett., 324, 99-102 (1993).
37. Vaclavikova, R., Horsky, S., Simek, P., and Gut, I., Paclitaxel metabolism in rat and human liver microsomes is inhibited by phenolic antioxidants. Naunyn. Schmiedebergs. Arch. Pharmacol., 368, 200-209 (2003).
38. Wacher, V. J., Salphati, L., and Benet, L. Z., Active secretion and enterocytic drug metabolism barriers to drug absorption. Adv. Drug Deliv. Rev., 46, 89-102 (2001).
39. Watkins, P. B., Wrighton, S. A., Schuetz, E. G., Molowa, D. T., and Guzelian, P. S., Identification of glucocorticoid-inducible cytochromes P-450 in the intestinal mucosa of rats and man. J. Clin. Invest., 80, 1029-1036 (1987).
40. Weir, M. R., Diltiazem: ten years of clinical experience in the treatment of hypertension. J. Clin. Pharmacol., 35, 220-232 (1995).
41. Yeung, P. K., Feng, J. D. Z., and Buckley, S. J., Pharmacokinetics and hypotensive effect of diltiazem in rabbits: Comparison of diltiazem with its major metabolites. J. Pharm. Pharmacol., 50, 1247-1253 (1998).
42. Yusa, K. and Tsuruo, T., Reversal mechanism of multidrug resistance by verapamil: direct binding of verapamil to Pglycoprotein on specific sites and transport of verapamil outward across the plasma membrane of K562/ADM cells. Cancer Res., 49, 5002-5006 (1989).
43. Zhang, S. and Morris, M. E., Effects of the flavonoids biochanin A, morin, phloretin, and silymarin on P-glycoprotein-mediated transport. J. Pharmacol. Exp. Ther., 304, 1258-1267 (2003).