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In vitro pharmacokinetic characterization of mulberroside A, the main polyhydroxylated stilbene in mulberry (Morus alba L.), and its bacterial metabolite oxyresveratrol in traditional oral use
Mei M.1; Ruan J.-Q.1; Wu W.-J.1; Zhou R.-N.1; Lei P.-C.3; Zhao H.-Y.1; Yan R.1; Wang Y.-T.1,2
2012
Source PublicationJournal of Agricultural and Food Chemistry
ISSN218561
Volume60Issue:9Pages:2299
Abstract

Mulberroside A (MulA) is one of the main bioactive constituents in mulberry (Morus alba L.). This study examined the determining factors for previously reported oral pharmacokinetic profiles of MulA and its bacterial metabolite oxyresveratrol (OXY) on in vitro models. When incubated anaerobically with intestinal bacteria, MulA underwent rapid deglycosylation and generated two monoglucosides and its aglycone OXY sequentially. MulA exhibited a poor permeability and predominantly traversed Caco-2 cells via passive diffusion; yet, the permeation of OXY across Caco-2 cells was much more rapid and involved efflux (both p-glycoprotein and MRPs)-mediated mechanisms. Moreover, OXY underwent extensive hepatic glucuronidation; yet, the parent MulA was kept intact in liver subcellular preparations. There was insignificant species difference in intestinal bacterial conversion of MulA and the extent of OXY hepatic glucuronidation between humans and rats, while OXY exhibited a distinct positional preference of glucuronidation in the two species. Overall, these findings revealed a key role of intestinal bacterial conversion in absorption and systemic exposure of MulA and its resultant bacterial metabolite OXY in oral route in humans and rats and warranted further investigational emphasis on OXY and its hepatic metabolites for understanding the benefits of mulberry. © 2011 American Chemical Society.

KeywordDeglycosylation Glucuronidation Hydroxystilbenes Intestinal Bacteria Morus AL.a L. Mulberroside a Oxyresveratrol Permeability
DOIhttp://doi.org/10.1021/jf204495t
URLView the original
Indexed BySCI
Language英语
WOS Research AreaAgriculture ; Chemistry ; Food Science & Technology
WOS SubjectAgriculture, Multidisciplinary ; Chemistry, Applied ; Food Science & Technology
WOS IDWOS:000301098900031
The Source to ArticleScopus
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Cited Times [WOS]:29   [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, Taipa, Macao, China
2.School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing, China
3.Clinical Laboratory, Kiang Wu Hospital, Estrada do Repouso, Macau, China
First Author AffilicationInstitute of Chinese Medical Sciences
Recommended Citation
GB/T 7714
Mei M.,Ruan J.-Q.,Wu W.-J.,et al. In vitro pharmacokinetic characterization of mulberroside A, the main polyhydroxylated stilbene in mulberry (Morus alba L.), and its bacterial metabolite oxyresveratrol in traditional oral use[J]. Journal of Agricultural and Food Chemistry,2012,60(9):2299.
APA Mei M..,Ruan J.-Q..,Wu W.-J..,Zhou R.-N..,Lei P.-C..,...&Wang Y.-T..(2012).In vitro pharmacokinetic characterization of mulberroside A, the main polyhydroxylated stilbene in mulberry (Morus alba L.), and its bacterial metabolite oxyresveratrol in traditional oral use.Journal of Agricultural and Food Chemistry,60(9),2299.
MLA Mei M.,et al."In vitro pharmacokinetic characterization of mulberroside A, the main polyhydroxylated stilbene in mulberry (Morus alba L.), and its bacterial metabolite oxyresveratrol in traditional oral use".Journal of Agricultural and Food Chemistry 60.9(2012):2299.
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