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Pharmacokinetic evidence on the contribution of intestinal bacterial conversion to beneficial effects of Astragaloside IV, a marker compound of Astragali Radix, in traditional oral use of the herb
Zhou R.-N.1; Song Y.-L.1; Ruan J.-Q.1; Wang Y.-T.1,2; Yan R.1
2012
Source PublicationDrug Metabolism and Pharmacokinetics
ISSN13474367
Volume27Issue:6Pages:586
Abstract

Astragaloside IV (AIV) is the most abundant saponin and a marker compound in Astragali Radix, a Chinese herb notable for its anti-aging and immune-enhancing effects. The present study investigated the role of intestinal bacterial conversion in the in vivo fate of AIV administered through a traditional oral route for the first time. When incubated anaerobically with rat intestinal bacteria, AIV generated five metabolites with three [monoglycosides brachyoside B and cyclogaleginoside B, the aglycone cycloastragenol (CA)] via stepwise deglycosylation and two from further epimerization (CA-iso) and dehydrogenation (CA-2H). Hydrolytic removal of C-6 glucose was a rate-limiting step for formations of CA and its derivatives. When AIV was orally administered to the rat, CA and CA-iso presented as the main components in plasma following AIV, and the AUC0-∞ were 88.60 ± 9.66 (CA), 179.06 ± 28.53 (CA-iso) and 452.28 ± 43.33 nM·h (AIV). CA-2H was the predominant form in feces but was not detected in urine or plasma. This agreed well with in vitro data including rapid hepatic metabolism of CA-2H to form CA and CA-iso and reversible conversions between CA-2H and CA/CA-iso by intestinal bacteria. These findings support a crucial role of gut bacterial conversion of AIV in the traditional application of Astragali herb and warrant further investigational emphasis on CA and CA-iso. © 2012 by the Japanese Society for the Study of Xenobiotics (JSSX).

Keyword3-epi-cycloastragenol Astragali Radix Astragaloside Iv Cycloastragenol Intestinal Bacteria Metabolism Oral Pharmacokinetics
DOIhttps://doi.org/10.2133/dmpk.DMPK-11-RG-160
URLView the original
Indexed BySCI
Language英语
WOS Research AreaPharmacology & Pharmacy
WOS SubjectPharmacology & Pharmacy
WOS IDWOS:000312616800004
The Source to ArticleScopus
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Cited Times [WOS]:35   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionInstitute of Chinese Medical Sciences
Affiliation1.State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau
2.School of Chinese Materia Medica, Beijing University of Chinese Medicine
First Author AffilicationInstitute of Chinese Medical Sciences
Recommended Citation
GB/T 7714
Zhou R.-N.,Song Y.-L.,Ruan J.-Q.,et al. Pharmacokinetic evidence on the contribution of intestinal bacterial conversion to beneficial effects of Astragaloside IV, a marker compound of Astragali Radix, in traditional oral use of the herb[J]. Drug Metabolism and Pharmacokinetics,2012,27(6):586.
APA Zhou R.-N.,Song Y.-L.,Ruan J.-Q.,Wang Y.-T.,&Yan R..(2012).Pharmacokinetic evidence on the contribution of intestinal bacterial conversion to beneficial effects of Astragaloside IV, a marker compound of Astragali Radix, in traditional oral use of the herb.Drug Metabolism and Pharmacokinetics,27(6),586.
MLA Zhou R.-N.,et al."Pharmacokinetic evidence on the contribution of intestinal bacterial conversion to beneficial effects of Astragaloside IV, a marker compound of Astragali Radix, in traditional oral use of the herb".Drug Metabolism and Pharmacokinetics 27.6(2012):586.
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