Effects of Baicalin on Oral Pharmacokinetics of Caffeine in Rats

Title
Effects of Baicalin on Oral Pharmacokinetics of Caffeine in Rats
Author(s)
정태천노금한네팔마헤시정기선김선아엄연지서채신강미정박필훈강원구[강원구]정혜광[정혜광]
Keywords
TANDEM MASS-SPECTROMETRY; SCUTELLARIA-BAICALENSIS; P-GLYCOPROTEIN; METABOLITES; INHIBITION; EXTRACT; WOGONIN; PLASMA; RADIX
Issue Date
201503
Publisher
KOREAN SOC APPLIED PHARMACOLOGY
Citation
BIOMOLECULES & THERAPEUTICS, v.23, no.2, pp.201 - 206
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 pharmacokinetics of caffeine and its metabolites in vivo, following single oral administration in rats.
URI
http://hdl.handle.net/YU.REPOSITORY/33218http://dx.doi.org/10.4062/biomolther.2014.134
ISSN
1976-9148
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약학대학 > 약학부 > Articles
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