Effects of baicalin on oral pharmacokinetics of caffeine in rats

Biomolecules & Therapeutics
Keumhan NohTae Cheon Jeong

Abstract

Scutellaria baicalensis is one of the most widely used herbal medicines in East Asia. Because baicalein and baicalin are major components of this herb, it is important to understand the effects of these compounds on drug metabolizing enzymes, such as cytochrome P450 (CYP), for evaluating herb-drug interaction. The effects of baicalin and baicalein on activities of ethoxyresorufin O-deethylase (EROD), methoxyresorufin O-demethylase (MROD), benzyloxyresorufin O-debenzylase (BROD), p-nitrophenol hydroxylase and erythromycin N-demethylase were assessed in rat liver microsomes in the present study. In addition, the pharmacokinetics of caffeine and its three metabolites (i.e., paraxanthine, theobromine and theophylline) in baicalin-treated rats were compared with untreated control. As results, EROD, MROD and BROD activities were inhibited by both baicalin and baicalein. However, there were no significant differences in the pharmacokinetic parameters of oral caffeine and its three metabolites between control and baicalin-treated rats. When the plasma concentration of baicalin was determined, the maximum concentration of baicalin was below the estimated IC50 values observed in vitro. In conclusion, baicalin had no effects on the pharma...Continue Reading

References

Sep 1, 1995·Phytochemistry·K IshimaruK Shimomura
May 14, 2003·Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences·Heiko SchneiderHansruedi Glatt
Dec 11, 2008·European Journal of Clinical Pharmacology·Lan FanHong-Hao Zhou
Apr 7, 2011·Archives of Pharmacal Research·Keumhan NohTae Cheon Jeong
Jun 19, 2013·Archives of Pharmacal Research·Mi Jeong KangTae Cheon Jeong
Aug 27, 2014·Phytotherapy Research : PTR·Saud M AlsanadRachel L Howard

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Citations

Jan 16, 2016·Molecular and Cellular Neurosciences·Karim A Alkadhi, Ibrahim A Alhaider
Mar 16, 2016·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Keumhan NohTae Cheon Jeong
Apr 22, 2016·Biomolecules & Therapeutics·Keumhan NohTae Cheon Jeong
Oct 8, 2016·Experimental Dermatology·Seayoung JooWonku Kang
Sep 14, 2018·European Journal of Drug Metabolism and Pharmacokinetics·Ting HuangChengliang Zhang
Apr 11, 2019·Metabolites·Mahesh Raj NepalTae Cheon Jeong
Aug 4, 2019·Pharmaceutics·Robert AncuceanuVlad Negulescu
May 1, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Leonid KaluzhskiyAlexis Ivanov

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