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Oral pharmacokinetics of baicalin, wogonoside, oroxylin A 7-O-β-D-glucuronide and their aglycones from an aqueous extract of Scutellariae Radix in the rat
Cai Y.; Li S.; Li T.; Zhou R.; Yan R.; Wai A.T.-S.
2015
Source PublicationJournal of Chromatography B: Analytical Technologies in the Biomedical and Life Sciences
ISSN15700232
Volume1026Pages:124
Abstract

Scutellariae Radix (SR) has been extensively prescribed in folk medicines due to its notable beneficial activities. The flavonoid glucuronides baicalin (BG), wogonoside (WG), oroxylin A 7-O-β-D-glucuronide (OG) and their aglycones baicalein, wogonin and oroxylin A, are the main components of the herb. So far, majority of previous studies failed to report the pharmacokinetics and none offered an explanation for the systemic exposures of these six flavonoids when the herbal extract was orally administered. In this study, when a SR extract was orally dosed to rats (800 mg/kg, equivalent to BG 324.80, WG 124.00, OG 43.04, baicalein 25.36, wogonin 24.40, and oroxylin A 5.79 mg/kg), all six flavonoids were detectable throughout the experimental period (48 h) using an LC–MS/MS method with the Cmax and AUC0–48 h of the glucuronides 10–130 times that of respective aglycones. As the lowest among the three glucuronides in the herb, OG was the most abundant in vivo, while the systemic exposure of wogonin was the highest amongst the three aglycones. The dose-normalized AUC0–48 h descended in orders of OG/oroxylin A, WG/wogonin and BG/baicalein. Two di-conjugates of baicalein (BG glucuronide and BG glucoside), two BG isomers (minor BM1 and major BM2), and one WG isomer (wogonin 5-O-glucuronide) were detected in rat plasma. Semi-quantitation of the isomers with peak area data revealed that the AUPs (area under peak area ratio-time curves) of BG isomers were ∼3 times that of BG, yet the AUP of wogonin 5-O-glucuronide was only one seventh of WG. BM2, tentatively assigned as baicalein 6-O-glucuronide, was formed from both microbial isomerization of BG and hepatic glucuronidation of baicalein. Wogonin 5-O-glucuronide was only formed in hepatic glucuronidation of wogonin. Demethylated wogonin was observed in gut bacteria, offering an optional origin of BM1 apart from baicalein glucuronidation. Microbial isomerization of BG and extensive hepatic glucuronidation of baicalein to form BM2 as well as a poorer intestinal permeability of baicalein (Papp × 10−6 cm/s) should account for the lower systemic exposures of BG and baicalein. Faster microbial hydrolysis of WG, high intestinal permeability (Papp × 10−5 cm/s) and less hepatic glucuronidation of wogonin explain the relatively high systemic exposure of wogonin. Sole microbial deglycosylation of OG, high intestinal permeability (Papp × 10−5 cm/s) and extensive hepatic glucuronidation of oroxylin A supported the highest systemic exposure of OG. Taken together, the oral kinetics of six flavonoid glucuronides and aglycones in the SR extract were simultaneously obtained. Microbial conversion, intestinal epithelial permeability and hepatic glucuronidation are determinant factors for their systemic exposures. © 2015 Elsevier B.V.

KeywordHepatic Glucuronidation Intestinal Permeability Isomerization Microbial Metabolism Scutellaria Radix Systemic Exposure
DOIhttp://doi.org/10.1016/j.jchromb.2015.11.049
URLView the original
Indexed BySCI
Language英语
WOS Research AreaBiochemistry & Molecular Biology ; Chemistry
WOS SubjectBiochemical Research Methods ; Chemistry, Analytical
WOS IDWOS:000379636800014
The Source to ArticleScopus
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Cited Times [WOS]:15   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionInstitute of Chinese Medical Sciences
Corresponding AuthorYan R.
AffiliationState Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Taipa, Macao, China
First Author AffilicationInstitute of Chinese Medical Sciences
Corresponding Author AffilicationInstitute of Chinese Medical Sciences
Recommended Citation
GB/T 7714
Cai Y.,Li S.,Li T.,et al. Oral pharmacokinetics of baicalin, wogonoside, oroxylin A 7-O-β-D-glucuronide and their aglycones from an aqueous extract of Scutellariae Radix in the rat[J]. Journal of Chromatography B: Analytical Technologies in the Biomedical and Life Sciences,2015,1026:124.
APA Cai Y.,Li S.,Li T.,Zhou R.,Yan R.,&Wai A.T.-S..(2015).Oral pharmacokinetics of baicalin, wogonoside, oroxylin A 7-O-β-D-glucuronide and their aglycones from an aqueous extract of Scutellariae Radix in the rat.Journal of Chromatography B: Analytical Technologies in the Biomedical and Life Sciences,1026,124.
MLA Cai Y.,et al."Oral pharmacokinetics of baicalin, wogonoside, oroxylin A 7-O-β-D-glucuronide and their aglycones from an aqueous extract of Scutellariae Radix in the rat".Journal of Chromatography B: Analytical Technologies in the Biomedical and Life Sciences 1026(2015):124.
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