Histone deacetylase inhibitor stimulateCYP3A4 proximal promoter activity in hepg2 cells

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• 作者：Ja Young Kim (1)
  Mee Ryung Ahn (1)
  Dae-Kee Kim (1)
  Yhun Yhong Sheen (1)
  
• 关键词：CYP3A4 ; PCN ; Rifampicin ; RU486 ; SXR ; HDAC ; IN2001 ; HepG2
• 刊名：Archives of Pharmacal Research
• 出版年：2004
• 出版时间：April 2004
• 年：2004
• 卷：27
• 期：4
• 页码：407-414
• 全文大小：1106KB
• 参考文献：1. Barwick, J. L., Quattrochi, L. C., Mills, A. S., Potenza, C., Tukey, R. H., and Guzelian, P. S., Trans-species gene transfer for analysis of glucocorticoid-inducible transcriptional activation of transiently expressed human / CYP3A4 and rabbit / CYP3A6 in primary cultures of adult rat and rabbit Hepa-ltocytes. / Mol. Pharmacol., 50, 10鈥?6 (1996).
  2. Drocourt, L., Ourlin, J. C., Pascussi, J. M., Maurel, P., and Vilarem, M. J., Expression of CYP3A4, CYP2B6, and CYP2C9 is regulated by the vitamin D receptor pathway in primary human Hepa-ltocytes. / J. Biol. Chem., 277, 25125鈥?5132 (2002). CrossRef
  3. Gibson, G. G., Regulation of the / CYP3A4 gene by hydrocortisone and xenobiotics: Role of the glucocorticoid and pregnane X receptors. / Drug Metab. Dispos., 28, 493鈥?96 (2000).
  4. Goodwin, B., Hodgson, E., and Liddle, C., The orphan human pregnane X receptor mediates the transcriptional activation of / CYP3A4 by rifampicin through a distal enhancer module. / Mol. Pharmacol., 56, 1329鈥?339 (1999).
  5. Guengerich, F. P., Cytochrome p-450 3A4: Regulation and role in drug metabolism, / Annu. Rev. Pharmacol. Toxicol., 39, 1鈥?7 (1999). CrossRef
  6. Hashimoto, H., Toide, K., Kitamura, R., Fujita, M., Tagawa, S., Itoh, S., and Kamataki, T., Gene structure of CYP3A4, an adult-specific form of cytochrome P450 in human livers, and its transcriptional control. / Eur. J. Biochem., 218, 585鈥?95 (1993). CrossRef
  7. Itoh, S., Yanagimoto, T., Tagawa, S., Hashimoto, H., Kitamura, R., Nakajima, Y., Okochi, T., Fujimoto, S., Uchino, J., and Kamataki, T., Genomic organization of human fetal specific P-450IIIA7 (cytochrome P-450HFLa)-related gene(s) and interaction of transcriptional regulatory factor with its DNA element in the 5鈥?flanking region. / Biochim. Biophys. Acta, 1130, 133鈥?38 (1992).
  8. Ketter, T. A., Flockhart, D. A., Post, R. M., Denicoff, K., Pazzaglia, P. J., Marangell, L. B., George, M. S., and Callahan, A. M., The emerging role of cytochrome P450 3A in psycho-pharmacology. / J. Clinic. Psychopharmacol., 15, 387鈥?98 (1995). CrossRef
  9. Kocarek, T. A., Schuetz, E. G., Strom, S. C., Fisher, R. A., and Guzelian, P. S., Comparative analysis of cytochrome P4503A induction in primary cultures of rat, rabbit, and human Hepa-Itocytes. / Drug Metab. Dispos., 23, 415鈥?21 (1995).
  10. Li, A. P., Kaminski, D. L., and Rasmussen, A., Substrates of human Hepa-ltic cytochrome P450 3A4. / Toxicology, 104, 1鈥? (1995). CrossRef
  11. Liddle, C., Goodwin, B. J., George, J., Tapner, M., and Farrell, G. C., Separate and interactive regulation of cytochrome P450 3A4 by triiodothyronine, dexamethasone, and growth hormone in cultured Hepa-ltocytes. / J. Clin. Endocrinol. Metab., 83, 2411鈥?416 (1998). CrossRef
  12. Luo, G., Cunningham, M., Kim S., Bum, T., Lin, J., Sinz, M., Hamilton, G., Rizzo, C., Jolley, S., Gilbert, D., Downey, A., Mudra, D., Graham, R., Carroll, K., Xie, J., Madan, A., Parkinson, A., Christ, D., Selling, B., Lecluyse, E., and Gan, L., CYP3A4 induction by drugs: Correlation between a pregnane X receptor reporter gene assay and CYP3A4 expression in human Hepa-ltocytes. / Drug Metab. Dispos., 30, 795鈥?04 (2002). CrossRef
  13. Mangelsdorf, D. J., and Evans, R. M., The RXR heterodimers and orphan receptors. / Cell, 83, 841鈥?50 (1995). CrossRef
  14. Marks, P. A., Miller, T., and Richon, V. M., Histone deacetylases. / Curr. Opin. Pharmacol., 3, 344鈥?51 (2003). CrossRef
  15. Mathur, M., Tucker P. W., and Samuels, H. H., PSF is a novel corepressor that mediates its effect through Sin3A and the DNA binding domain of nuclear hormone receptors. / Mol. Cell Biol., 21, 2298鈥?311 (2001). CrossRef
  16. Michalets, E. L., Update: clinically significant cytochrome P-450 drug interactions. / Pharmacotherapy, 18, 84鈥?12 (1998).
  17. Nakajima, A., Iwanari, M., and Yokoi, T., Effects of histone deacetylation and DNA methylation on the constitutive and TCDD-inducible expressions of the human CYP1 family in MCF-7 and HeLa cells. / Toxicol. Lett., 144, 247鈥?56 (2003). CrossRef
  18. Ogg, M. S., Williams, J. M., Tarbit, M., Goldfarb, P. S., Grays, T. J. B., and Gibson, G. G., A reporter gene assay to assess the molecular mechanisms of xenobiotic-dependent induction of the human / CYP3A4 gene / in vitro. / Xenobiotica, 29, 269鈥?79 (1999). CrossRef
  19. Pascussi, J. M., Gerbal-Chaloin, S., Drocourt, L., Maurel, P., and Vilarem, M. J., The expression of CYP2B6, CYP2C9 and CYP3A4 genes, a tangle of networks of nuclear and steroid receptors. / Biochim. Biophysic. Act., 1619, 243鈥?53 (2003).
  20. Pazin, M. J., and Kadonaga, J. T., Whats up and down with histone deacetylation and transcription? / Cell, 89, 325鈥?28 (1997). CrossRef
  21. Schuetz, E. G., Schuetz, J. D., Strom, S. C., Thompson, M. T., Fisher, R. A., Molowa, D. T., Li, D., and Guzelian, P. S., Regulation of human liver cytochromes P-450 in family 3A in primary and continuous culture of human Hepatocytes. / Hepatology 18, 1254鈥?262 (1993). CrossRef
  22. Sueyoshi, T., Kawamoto, T., Zelko, I., Honkakoski, P., and Negishi, M., The repressed nuclear receptor CAR responds to phenobarbital in activating the human CYP2B6 gene. / J. Biol. Chem., 274, 6043鈥?046 (1999). CrossRef
  23. Synold, T. W., Dussault, I., and Forman, B. M., The orphan nuclear receptor SXR coordinately regulates drug metabolism and efflux. / Nat. Med., 7, 584鈥?90 (2001). CrossRef
  24. Takeshita, A., Taguchi, M., Koibuchi, N., and Ozawa, Y., Putative role of the orphan nuclear receptor SXR in the mechanism of / CYP3A4 inhibition by Xenobiotics. / J. Biol. Chem., 277, 32453鈥?2458 (2002). CrossRef
  25. Thummel, K. E., Brimer, C., Yasuda, K., Thottassery, J., Senn, T., Lin, Y., Ishizuka, H., Kharasch, E., Schuetz, J., and Schuetz, E., Transcriptional control of intestinal cytochrome P-4503A by 1alpha,25-dihydroxy vitamin D3. / Mol. Pharmacol., 60, 1399鈥?406 (2001).
  26. Wu, C., Chromatin remodeling and the control of gene expression. / J. Biol. Chem., 272, 28171鈥?8174 (1997). CrossRef
  
• 作者单位：Ja Young Kim (1)
  Mee Ryung Ahn (1)
  Dae-Kee Kim (1)
  Yhun Yhong Sheen (1)
  
  1. College of Pharmacy, Ewha Womans University, 11-1 Daehyun-dong, Seodaemun-ku, 120-750, Seoul, Korea
  
• ISSN：1976-3786

文摘

The expression ofCYP3A4 gene is induced by a variety of structurally unrelated xenobiotics including the antibiotic rifampicin, pregnenolone 16-carbonitrile (PCN), and endogenous hormones, that might mediate through steroid and xenobiotic receptor (SXR) system. The molecular mechanisms underlying regulation ofCYP3A4 gene expression have not been understood. In order to gain the insight of the molecular mechanism ofCYP3A4 gene expression, study has been undertaken to investigate if the histone deacetylation is involved in the regulation ofCYP3A4 gene expression by proximal promoter in human hepatoma HepG2 cells. Also we have investigated to see if SXR is involved in the regulation of CYP3A4 proximal promoter activity in human hepatoma HepG2 cells. HepG2 cells were transfected with a plasmidpCYP3A4-Luc containing~1 kb of theCYP3A4 proximal promoter region (-863 to +64 bp) in front of a reporter gene, luciferase, in the presence or absence of pSAP-SXR. In HepG2 cells, CYP3A4 inducers, such as rifampicin, PCN and RU486 showed minimal stimulation ofCYP3A4 proximal promoter activity in the absence of SXR and histone deacetylase (HDAC) inhibitors. 4-Dimethylamino-N-[4-(2-hydroxycarbamoylvinyl)benzyl]benzamide (IN2001), a new class HDAC inhibitor significantly increasedCYP3A4 proximal promoter activity over untreated control cells and rifampicin concomitant treatment with IN2001 increased furtherCYP3A4 proximal promoter activity that was stimulated by IN2001. The results of this study demonstrated that both HDAC inhibitors and SXR are essential to increase ofCYP3A4 proximal promoter activity by CYP3A4 inducers such as PCN, rifampicin, and RU486. Especially SXR seems to be important for the dose dependent response of CYP3A4 inducing chemicals to stimulateCYP3A4 proximal promoter activity. Also this data suggested that HDAC inhibitors seemed to facilitate theCYP3A4 proximal promoter to be activated by chemicals.