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Effect of Scutellariae Radix Extract on Human CYP450 Mediated-Drug Metabolism

  • Received : 2011.03.24
  • Accepted : 2011.04.24
  • Published : 2011.06.20

Abstract

Scutellariae Radix is widely used in the traditional herbal medicine for the treatment of fever, cough, dysentery, hepatitis and hypertension in Korea, China and Japan. In this study, we investigated the effects of 70% ethanolic extract of Scutellariae Radix (SRE) on CYP450-mediated drug metabolism in the in vitro systems using human liver microsomes and hepatocytes. The microsomal incubation assay showed that SRE inhibited the drug metabolism reactions catalyzed by CYP1A2, CYP2C8 and CYP2C9 in a dose-dependent manner. In particular, SRE was shown to strongly inhibit the metabolic activity of CYP1A2 with an $IC_{50}$ value of 4.6 ${\mu}g/mL$. When SRE was evaluated for its effect on the induction of CYP450 enzyme activities in cryopreserved human hepatocytes, SRE did not exhibit any effect.

Keywords

References

  1. 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., 2009. Induction of cytochrome P450 2B6 activity by the herbal medicine baicalin as measured by bupropion hydroxylation. Eur. J. Clin. Pharmacol. 65, 403-409. https://doi.org/10.1007/s00228-008-0594-3
  2. Kim, B.R., Kim, D.H., Park, R., Kwon, K.B., Ryu, D.G., Kim, Y.C., Kim, N.Y., Jeong, S., Kang, B.K., Kim, K.S., 2001. Effect of an extract of the root of Scutellaria baicalensis and its flavonoids on aflatoxin B1 oxidizing cytochrome P450 enzymes. Planta Med. 67, 396-399. https://doi.org/10.1055/s-2001-15810
  3. Kim, J.Y., Lee, S., Kim, D.H., Kim, B.R., Park, R., Lee, B.M., 2002. Effects of flavonoids isolated from Scutellariae radix on cytochrome P-450 activities in human liver microsomes. J. Toxicol. Environ. Health A. 65, 373-381. https://doi.org/10.1080/15287390252808046
  4. 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. https://doi.org/10.1016/j.ejphar.2010.05.017
  5. Li-Weber, M., 2009. New therapeutic aspects of flavones: the anticancer properties of Scutellaria and its main active constituents wogonin, baicalein and baicalin. Cancer Treat Rev. 35, 57-68. https://doi.org/10.1016/j.ctrv.2008.09.005
  6. Lin, C.C., Shieh D.E., 1996. The anti-inflammatory activity of Scutellaria rivularis extracts and its active components, baicalin, baicalein and wogonin. Am. J. Chin. Med. 24, 31-36. https://doi.org/10.1142/S0192415X96000050
  7. Ortiz de Montellano, P.R., 1995. Cytochrome P450: structure, mechanism, and biochemistry. Plenum Press, New York, NY, pp. 3-48.