Biomol Ther.  2015 Mar;23(2):201-206. 10.4062/biomolther.2014.134.

Effects of Baicalin on Oral Pharmacokinetics of Caffeine in Rats

• Noh K
• Nepal MR
• Jeong KS
• Kim SA
• Um YJ
• Seo CS
• Kang MJ
• Park PH
• Kang W
• Jeong HG
• Jeong TC

• KMID: 2380355
• DOI: http://doi.org/10.4062/biomolther.2014.134

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.

Keyword

Baicalin; Baicalein; Caffeine; Drug interaction; Pharmacokinetics

MeSH Terms

Administration, Oral
Animals
Caffeine*
Cytochrome P-450 CYP1A1
Cytochrome P-450 CYP2B1
Cytochrome P-450 CYP3A
Cytochrome P-450 Enzyme System
Drug Interactions
Far East
Herb-Drug Interactions
Inhibitory Concentration 50
Microsomes, Liver
Pharmacokinetics*
Plasma
Rats*
Scutellaria baicalensis
Theobromine
Caffeine
Cytochrome P-450 CYP1A1
Cytochrome P-450 CYP2B1
Cytochrome P-450 CYP3A
Cytochrome P-450 Enzyme System
Theobromine