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Isolation, identification and antiviral activities of metabolites of calycosin-7-O-β-d-glucopyranoside.
MedLine Citation:
PMID:  21703796     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
In vivo and in vitro metabolites of calycosin-7-O-β-d-glucopyranoside in rats were identified using a specific and sensitive high performance liquid chromatography-tandem mass spectrometry (HPLC-MS(n)) method. The parent compound and twelve metabolites were found in rat urine after oral administration of calycosin-7-O-β-d-glucopyranoside. The parent compound and six metabolites were detected in rat plasma. In heart, liver, spleen, lung and kidney samples, respectively, six, eight, seven, nine and nine metabolites were identified, in addition to the parent compound. Three metabolites, but no trace of parent drug, were found in the rat intestinal flora incubation mixture and feces, which demonstrated cleavage of the glycosidic bond of the parent compound in intestines. The main phase I metabolic pathways of calycosin-7-O-β-d-glucopyranoside in rats were deglycosylation, dehydroxylation and demethylation reactions; phase II metabolism included sulfation, methylation, glucuronidation and glycosylation (probably). Furthermore, two metabolites commonly found in rat urine, plasma and tissues were isolated from feces and characterized by NMR. The antiviral activities of the metabolite calycosin against coxsackie virus B(3) (CVB(3)) and human immunodeficiency virus (HIV) were remarkably stronger than those of calycosin-7-O-β-d-glucopyranoside.
Authors:
Luying Chen; Zhixiong Li; Yihong Tang; Xiaolan Cui; Ronghua Luo; Shanshan Guo; Yongtang Zheng; Chenggang Huang
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2011-6-1
Journal Detail:
Title:  Journal of pharmaceutical and biomedical analysis     Volume:  -     ISSN:  1873-264X     ISO Abbreviation:  -     Publication Date:  2011 Jun 
Date Detail:
Created Date:  2011-6-27     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  8309336     Medline TA:  J Pharm Biomed Anal     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Copyright Information:
Copyright © 2011 Elsevier B.V. All rights reserved.
Affiliation:
Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 501 Haike Rd., Pudong, 201203 Shanghai, China.
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