Induction of CYP3A4 and MDR1 gene expression by baicalin, baicalein, chlorogenic acid, and ginsenoside Rf through constitutive androstane receptor- and pregnane X receptor-mediated pathways

European Journal of Pharmacology

Volumn 640, Issue 1-3, 2010, Pages 46-54

  Li, Yue ^a   Wang, Qi ^b,c   Yao, Xiaomin ^a   Li, Yan ^a  

^a INSTITUTE OF MATERIA MEDICA   (China)

^b CAPITAL MEDICAL UNIVERSITY   (China)

^c CAPITAL MEDICAL UNIVERSITY   (China)

Author keywords

Constitutive androstane receptor; CYP3A4; Herbal product; MDR1; Pregnane X receptor

Indexed keywords

BAICALEIN; BAICALIN; CHLOROGENIC ACID; CONSTITUTIVE ANDROSTANE RECEPTOR; CYTOCHROME P450 3A4; GINSENOSIDE RF; LUCIFERASE; MESSENGER RNA; MULTIDRUG RESISTANCE PROTEIN 1; PREGNANE X RECEPTOR; RIFAMPICIN; CELL RECEPTOR; CYP3A4 PROTEIN, HUMAN; CYTOCHROME P450 3A; FLAVANONE DERIVATIVE; FLAVONOID; GINSENOSIDE; MULTIDRUG RESISTANCE PROTEIN; PLANT EXTRACT; RETINOID X RECEPTOR; STEROID RECEPTOR;

ARTICLE; CELL STRAIN HEPG2; CONTROLLED STUDY; ENZYME ACTIVATION; ENZYME ACTIVITY; GEL MOBILITY SHIFT ASSAY; GENE; GENE EXPRESSION; GENETIC TRANSFECTION; HUMAN; HUMAN CELL; LUMINESCENCE; NUCLEOTIDE SEQUENCE; PRIORITY JOURNAL; PROMOTER REGION; PROTEIN INTERACTION; REAL TIME POLYMERASE CHAIN REACTION; TRANSCRIPTION REGULATION; UPREGULATION; WESTERN BLOTTING; CELL LINE; CELL SURVIVAL; CHEMISTRY; DNA RESPONSIVE ELEMENT; DRUG EFFECTS; GENETICS; METABOLISM; PROTEIN MULTIMERIZATION; PROTEIN QUATERNARY STRUCTURE; TRANSCRIPTION INITIATION;

CELL LINE; CELL SURVIVAL; CHLOROGENIC ACID; CYTOCHROME P-450 CYP3A; FLAVANONES; FLAVONOIDS; GINSENOSIDES; HUMANS; P-GLYCOPROTEIN; PLANT EXTRACTS; PROTEIN MULTIMERIZATION; PROTEIN STRUCTURE, QUATERNARY; RECEPTORS, CYTOPLASMIC AND NUCLEAR; RECEPTORS, STEROID; RESPONSE ELEMENTS; RETINOID X RECEPTORS; RNA, MESSENGER; TRANSCRIPTIONAL ACTIVATION;

EID: 77953812705     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejphar.2010.05.017     Document Type: Article

References (44)

1. Ahmed S.M., Banner N.R., Dubrey S.W. Low cyclosporin-A level due to Saint-John's-wort in heart transplant patients. J. Heart Lung Transplant. 2001, 20:795.
2. Attele A.S., Wu J.A., Yuan C.S. Ginseng pharmacology: multiple constituents and multiple actions. Biochem. Pharmacol. 1999, 58:1685-1693.
3. Bae E.A., Han M.J., Shin Y.W., Kim D.H. Inhibitory effects of Korean red ginseng and its genuine constituents ginsenosides Rg3, Rf, and Rh2 in mouse passive cutaneous anaphylaxis reaction and contact dermatitis models. Biol. Pharm. Bull. 2006, 29:1862-1867.
4. Baer-Dubowska W., Szaefer H., Krajka-Kuzniak V. Inhibition of murine hepatic cytochrome P450 activities by natural and synthetic phenolic compounds. Xenobiotica 1998, 28:735-743.
5. Burk O., Arnold K.A., Geick A., Tegude H., Eichelbaum M. A role for constitutive androstane receptor in the regulation of human intestinal MDR1 expression. Biol. Chem. 2005, 386:503-513.
6. Cerveny L., Svecova L., Anzenbacherova E., Vrzal R., Staud F., Dvorak Z., Ulrichova J., Anzenbacher P., Pavek P. Valproic acid induces CYP3A4 and MDR1 gene expression by activation of constitutive androstane receptor and pregnane X receptor pathways. Drug Metab. Dispos. 2007, 35:1032-1041.
7. Chen C.H., Huang T.S., Wong C.H., Hong C.L., Tsai Y.H., Liang C.C., Lu F.J., Chang W.H. Synergistic anti-cancer effect of baicalein and silymarin on human hepatoma HepG2 cells. Food Chem. Toxicol. 2009, 47:638-644.
8. Chou T.C., Chang L.P., Li C.Y., Wong C.S., Yang S.P. The antiinflammatory and analgesic effects of baicalin in carrageenan-evoked thermal hyperalgesia. Anesth. Analg. 2003, 97:1724-1729.
9. Dos Santos M.D., Almeida M.C., Lopes N.P., De Souza G.E. Evaluation of the anti-inflammatory, analgesic and antipyretic activities of the natural polyphenol chlorogenic acid. Biol. Pharm. Bull. 2006, 29:2236-2240.
10. Duniec-Dmuchowski Z., Fang H.L., Strom S.C., Ellis E., Runge-Morris M., Kocarek T.A. Human pregnane X receptor activation and CYP3A4/CYP2B6 induction by 2, 3-oxidosqualene: lanosterol cyclase inhibition. Drug Metab. Dispos. 2009, 37:900-908.
11. Evers D.L., Chao C.F., Wang X., Zhang Z., Huong S.M., Huang E.S. Human cytomegalovirus-inhibitory flavonoids: studies on antiviral activity and mechanism of action. Antivir. Res. 2005, 68:124-134.
12. Fan L., Wang J.C., Jiang F., Tan Z.R., Chen Y., Li Q., Zhang W., Wang G., Lei H.P., Hu D.L., Wang D., Zhou H.H. Induction of cytochrome P450 2B6 activity by the herbal medicine baicalin as measured by bupropion hydroxylation. Eur. J. Clin. Pharmacol. 2009, 65:403-409.
13. Faucette S.R., Sueyoshi T., Smith C.M., Negishi M., Lecluyse E.L., Wang H. Differential regulation of hepatic CYP2B6 and CYP3A4 genes by constitutive androstane receptor but not pregnane X receptor. J. Pharmacol. Exp. Ther. 2006, 317:1200-1209.
14. Geick A., Eichelbaum M., Burk O. Nuclear receptor response elements mediate induction of intestinal MDR1 by rifampin. J. Biol. Chem. 2001, 276:14581-14587.
15. Gillis C.N. Panax ginseng pharmacology: a nitric oxide link?. Biochem. Pharmacol. 1997, 54:1-8.
16. Goodwin B., Hodgson E., Liddle C. The orphan human pregnane X receptor mediates the transcriptional activation of CYP3A4 by rifampicin through a distal enhancer module. Mol. Pharmacol. 1999, 56:1329-1339.
17. Hall S.D., Wang Z., Huang S.M., Hamman M.A., Vasavada N., Adigun A.Q., Hilligoss J.K., Miller M., Gorski J.C. The interaction between St. John's wort and an oral contraceptive. Clin. Pharmacol. Ther. 2003, 74:525-535.
18. Henderson G.L., Harkey M.R., Gershwin M.E., Hackman R.M., Stern J.S., Stresser D.M. Effects of ginseng components on c-DNA-expressed cytochrome P450 enzyme catalytic activity. Life Sci. 1999, 65:PL209-PL214.
19. Hou Y.N., Zhu X.Y., Cheng G.F. Effects of baicalin on liver microsomal cytochrome P450 system. Yao Xue Xue Bao 2000, 35:890-892.
20. Huynh H.T., Teel R.W. Effects of plant-derived phenols on rat liver cytochrome P450 2B1 activity. Anticancer Res. 2002, 22:1699-1703.
21. Iwahori T., Matsuura T., Maehashi H., Sugo K., Saito M., Hosokawa M., Chiba K., Masaki T., Aizaki H., Ohkawa K., Suzuki T. CYP3A4 inducible model for in vitro analysis of human drug metabolism using a bioartificial liver. Hepatology 2003, 37:665-673.
22. Jodoin J., Demeule M., Beliveau R. Inhibition of the multidrug resistance P-glycoprotein activity by green tea polyphonols. Biochim. Biophys. Acta 2002, 1542:149-159.
23. Kessler R.C., Davis R.B., Foster D.F., Van Rompay M.I., Walters E.E., Wilkey S.A., Kaptchuk T.J., Eisenberg D.M. Long-term trends in the use of complementary and alternative medical therapies in the United States. Ann. Intern. Med. 2001, 135:262-268.
24. Kim J.Y., Lee S., Kim D.H., Kim B.R., Park R., Lee B.M. Effects of flavonoids isolated from Scutellariae radix on cytochrome P-450 activities in human liver microsomes. J. Toxicol. Environ. Health A 2002, 65:373-381.
25. Lai M.Y., Hsiu S.L., Hou Y.C., Tsai S.Y., Chao P.D. Significant decrease of cyclosporine bioavailability in rats caused by a decoction of the roots of Scutellaria baicalensis. Planta Med. 2004, 70:132-137.
26. Lemaire G., de Sousa G., Rahmani R. A PXR reporter gene assay in a stable cell culture system: CYP3A4 and CYP2B6 induction by pesticides. Biochem. Pharmacol. 2004, 68:2347-2358.
27. Li C.Y., Chiu C.H., Huang H.S., Lin C.H., Wu T.S. High-performance liquid chromatographic method for simultaneous quantification of eight major biologically active ingredients in 'Da-Chai-Hu-Tang' preparation. Biomed. Chromatogr. 2006, 20:305-308.
28. Li L., Stanton J.D., Tolson A.H., Luo Y., Wang H. Bioactive terpenoids and flavonoids from ginkgo biloba extract induce the expression of hepatic drug-metabolizing enzymes through pregnane X receptor, constitutive androstane receptor, and aryl hydrocarbon receptor-mediated pathways. Pharm. Res. 2009, 26:872-882.
29. Liu C.T., Wu C.Y., Weng Y.M., Tseng C.Y. Ultrasound-assisted extraction methodology as a tool to improve the antioxidant properties of herbal drug Xiao-chia-hu-tang. J. Ethnopharmacol. 2005, 99:293-300.
30. Maglich J.M., Parks D.J., Moore L.B., Collins J.L., Goodwin B., Billin A.N., Stoltz C.A., Kliewer S.A., Lambert M.H., Willson T.M., Moore J.T. Identification of a novel human constitutive androstane receptor (CAR) agonist and its use in the identification of CAR target genes. J. Biol. Chem. 2003, 278:17277-17283.
31. Markowitz J.S., Donovan J.L., DeVane C.L., Taylor R.M., Ruan Y., Wang J.S., Chavin K.D. Effect of St. John's wort on drug metabolism by induction of cytochrome P450 3A4 enzyme. JAMA. 2003, 290:1500-1504.
32. Moore L.B., Parks D.J., Jones S.A., Bledsoe R.K., Consler T.G., Stimmel J.B., Goodwin B., Liddle C., Blanchard S.G., Willson T.M., Collins J.L., Kliewer S.A. Orphan nuclear receptors constitutive androstane receptor and pregnane X receptor share xenobiotic and steroid ligands. J. Biol. Chem. 2000, 275:15122-15127.
33. Pascussi J.M., Gerbal-Chaloin S., Drocourt L., Maurel P., Vilarem M.J. The expression of CYP2B6, CYP2C9 and CYP3A4 genes: a tangle of networks of nuclear and steroid receptors. Biochim. Biophys. Acta 2003, 1619:243-253.
34. Pavek P., Dvorak Z. Xenobiotic-induced transcriptional regulation of xenobiotic metabolizing enzymes of the cytochrome P450 superfamily in human extrahepatic tissues. Curr. Drug Metab. 2008, 9:129-143.
35. Piscitelli S.C., Burstein A.H., Chaitt D., Alfaro R.M., Falloon J. Indinavir concentrations and St. John's wort. Lancet 2000, 355:547-548.
36. Rencurel F., Stenhouse A., Hawley S.A., Friedberg T., Hardie D.G., Sutherland C., Wolf C.R. AMP-activated protein kinase mediates phenobarbital induction of CYP2B gene expression in hepatocytes and a newly derived human hepatoma cell line. J. Biol. Chem. 2005, 280:4367-4373.
37. Shao Z.H., Vanden Hoek T.L., Qin Y., Becker L.B., Schumacker P.T., Li C.Q., Dey L., Barth E., Halpern H., Rosen G.M., Yuan C.S. Baicalein attenuates oxidant stress in cardiomyocytes. Am. J. Physiol. Heart Circ. Physiol. 2002, 282:H999-H1006.
38. Si D., Wang Y., Zhou Y.H., Guo Y., Wang J., Zhou H., Li Z.S., Fawcett J.P. Mechanism of CYP2C9 inhibition by flavones and flavonols. Drug Metab. Dispos. 2009, 37:629-634.
39. Timsit Y.E., Negishi M. CAR and PXR: the xenobiotic-sensing receptors. Steroid. 2007, 72:231-246.
40. Tolson A.H., Li H.S., Eddington N.D., Wang H.B. Methadone induces the expression of hepatic drug-metabolizing enzymes through the activation of pregnane X receptor and constitutive androstane receptor. Drug Metab. Dispos. 2009, 37:1887-1894.
41. Vignati L.A., Bogni A., Grossi P., Monshouwer M. A human and mouse pregnane X receptor reporter gene assay in combination with cytotoxicity measurements as a tool to evaluate species-specific CYP3A induction. Toxicology 2004, 199:23-33.
42. Wang H., LeCluyse E.L. Role of orphan nuclear receptors in the regulation of drug-metabolising enzymes. Clin. Pharmacokinet. 2003, 42:1331-1357.
43. Wang G.F., Shi L.P., Ren Y.D., Liu Q.F., Liu H.F., Zhang R.J., Li Z., Zhu F.H., He P.L., Tang W., Tao P.Z., Li C., Zhao W.M., Zuo J.P. Anti-hepatitis B virus activity of chlorogenic acid, quinic acid and caffeic acid in vivo and in vitro. Antivir. Res. 2009, 83:186-190.
44. Yu C., Ye S., Sun H., Liu Y., Gao L., Shen C., Chen S., Zeng S. PXR-mediated transcriptional activation of CYP3A4 by cryptotanshinone and tanshinone IIA. Chem. Biol. Interact. 2009, 177:58-64.