Concentration-Dependent Inhibitory Effect of Baicalin on the Plasma Protein Binding and Metabolism of Chlorzoxazone, a CYP2E1 Probe Substrate, in Rats In Vitro and In Vivo

PLoS ONE

Volumn 8, Issue 1, 2013, Pages

  Gao, Na ^a   Zou, Dan ^a   Qiao, Hai Ling ^a  

^a ZHENGZHOU UNIVERSITY   (China)

Author keywords

[No Author keywords available]

Indexed keywords

6 HYDROXYCHLORZOXAZONE; BAICALIN; CHLORZOXAZONE; CYTOCHROME P450 2E1; PLASMA PROTEIN;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG CLEARANCE; DRUG HALF LIFE; DRUG METABOLISM; ENZYME ACTIVITY; ENZYME SUBSTRATE; FEMALE; IN VITRO STUDY; IN VIVO STUDY; LIVER MICROSOME; MAXIMUM PLASMA CONCENTRATION; METHODOLOGY; NONHUMAN; PROTEIN BINDING; RANDOMIZATION; RAT;

ANIMALS; AREA UNDER CURVE; CHLORZOXAZONE; CROSS-OVER STUDIES; CYTOCHROME P-450 CYP2E1; DOSE-RESPONSE RELATIONSHIP, DRUG; ENZYME INHIBITORS; FEMALE; FLAVONOIDS; MICROSOMES, LIVER; PLANT EXTRACTS; PROTEIN BINDING; RANDOM ALLOCATION; RATS; RATS, SPRAGUE-DAWLEY; TIME FACTORS; TREATMENT OUTCOME;

ANIMALIA; RATTUS;

EID: 84871791381     PISSN: None     EISSN: 19326203     Source Type: Journal    
DOI: 10.1371/journal.pone.0053038     Document Type: Article

References (22)

1. Li C, Lin G, Zuo Z, (2011) Pharmacological effects and pharmacokinetics properties of Radix Scutellariae and its bioactive flavones. Biopharm Drug Dispos 32: 427-445.
2. Lai MY, Hsiu SL, Tsai SY, Hou YC, Chao PD, (2003) Comparison of metabolic pharmacokinetics of baicalin and baicalein in rats. J Pharm Pharmacol 55: 205-209.
3. Srinivas NR, (2010) Baicalin, an emerging multi-therapeutic agent: pharmacodynamics, pharmacokinetics, and considerations from drug development perspectives. Xenobiotica 40: 357-367.
4. Fan L, Wang JC, Jiang F, Tan ZR, Chen Y, et al. (2009) Induction of cytochrome P450 2B6 activity by the herbal medicine baicalin as measured by bupropion hydroxylation. Eur J Clin Pharmacol 65: 403-409.
5. Lininger SW, Gaby AR, Austin S, Brown DJ, Wright JV, et al. (2000) The natural pharmacy. Random House, New York.
6. McGuffin M, Hobbs C, Upton R, Goldberg A (1997) American Herbal Products Association botanical safety handbook. CRC Press, Boca Raton.
7. Lee KS, Kim SK (2011) Direct and metabolism-dependent cytochrome P450 inhibition assays for evaluating drug-drug interactions. J Appl Toxicol: In press.
8. Lai MY, Hsiu SL, Hou YC, Tsai SY, Chao PD, (2004) Significant decrease of cyclosporine bioavailability in rats caused by a decoction of the roots of Scutellaria baicalensis. Planta Med 70: 132-137.
9. Hou YN, Zhu XY, Cheng GF (2000) Effects of baicalin on liver microsomal cytochrome P450 system. Acta Pharmaceutica Sinica 35, 890-892 (Chinese).
10. Jang SI, Kim HJ, Hwang KM, Jekal SJ, Pae HO, et al. (2003) Hepatoprotective Effect of Baicalin, a Major Flavone from Scutellaria radix, on Acetaminophen-Induced Liver Injury in Mice. Immunopharmacol Immunotoxicol 25: 585-594.
11. Li Y, Wang Q, Yao X, Li Y, (2010) 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. Eur J Pharmacol 640: 46-54.
12. Li J, Wei DQ, Wang JF, Yu ZT, Chou KC, (2012) Molecular dynamics simulations of CYP2E1. Med Chem 8: 208-221.
13. Shaik IH, Mehvar R, (2011) Effects of normothermic hepatic ischemia-reperfusion injury on the in vivo, isolated perfused liver, and microsomal disposition of chlorzoxazone, a cytochrome P450 2E1 probe, in rats. J Pharm Sci 100: 5281-5292.
14. Chittur SV, Tracy TS, (1997) Rapid and sensitive high-performance liquid chromatographic assay for 6-hydroxychlorzoxazone and chlorzoxazone in liver microsomes. J Chromatogr B Biomed Sci App l693: 479-483.
15. Rockich K, Blouin R, (1999) Effect of the acute-phase response on the pharmacokinetics of chlorzoxazone and cytochrome P-450 2E1 in vitro activity in rats. Drug Metab Dispos 27: 1074-1077.
16. Zeng MF, Pan LM, Zhu HX, Zhang QC, Guo LW, (2010) Comparative pharmacokinetics of baicalin in plasma after oral administration of Huang-Lian-Jie-Du-Tang or pure baicalin in MCAO and sham-operated rats. Fitoterapia 81: 490-496.
17. Gonzalez FJ, (1988) The molecular biology of cytochrome P450s. Pharmacol Rev 40: 243-288.
18. Waxman DJ, Dannan GA, Guengerich FP, (1985) Regulation of rat hepatic cytochrome P-450: Age-dependent Expression, Hormonal Imprinting, and Xenobiotic Inducibility of Sex-specific isoenzymes. Biochemistry 24: 4409-4417.
19. Tang Y, Zhu H, Zhang Y, Huang C, (2006) Determination of human plasma protein binding of baicalin by ultrafiltration and high-performance liquid chromatography. Biomed Chromatogr 20: 1116-1119.
20. Christensen H, Baker M, Tucker GT, Rostami-Hodjegan A, (2006) Prediction of plasma protein binding displacement and its implications for quantitative assessment of metabolic drug-drug interactions from in vitro data. J Pharm Sci 95: 2778-2787.
21. Tortorici MA, Kochanek PM, Bies RR, Poloyac SM, (2006) Therapeutic hypothermia-induced pharmacokinetic alterations on CYP2E1 chlorzoxazone-mediated metabolism in a cardiac arrest rat model. Crit Care Med 34: 785-791.
22. Baek HW, Bae SK, Lee MG, Sohn YT, (2006) Pharmacokinetics of Chlorzoxazone in Rats with Diabetes: Induction of CYP2E1 on 6-Hydroxychlorzoxazone Formation. J Pharm Sci 95: 2452-2462.