Document Detail


Biological disposition of boldine: in vitro and in vivo studies.
MedLine Citation:
PMID:  10861968     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Boldine is a natural compound with well-established free radical scavenger and hepatoprotective properties. The further exploration of its actual therapeutic potential as an antioxidant is, however, partially limited by the absence of knowledge on its pharmacokinetics. In the present studies, we provide information on the in vitro and in vivo biological disposition of boldine. The addition of 200 microM boldine to an isolated rat hepatocyte suspension was followed by a time-dependent (0-60 min) disappearance of boldine from the extracellular medium. This decline was associated with an early (first 2 min) and swift accumulation (1600 microM) of boldine within the cells. Although the intracellular concentration of boldine diminished, boldine was always found to occur within the cells at concentrations substantially higher than those initially added to the preparation. Boldine was also concentration-dependently removed from the extracellular medium by isolated rat livers portally perfused with the antioxidant. In vivo studies, conducted in rats, revealed that following either its oral or its intravenous administration, plasma boldine concentrations declined rapidly and according to an apparently first order type of kinetics. After its oral administration (50 or 75 mg/kg), boldine was rapidly (within 30 min) absorbed and preferentially concentrated in the liver, with substantially lower concentrations being found in the brain and heart. Maximal hepatic concentrations of boldine were found to be equal to or greater than those needed to afford antioxidant and hepatoprotective effects in vitro.
Authors:
I Jiménez; H Speisky
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Publication Detail:
Type:  In Vitro; Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Phytotherapy research : PTR     Volume:  14     ISSN:  0951-418X     ISO Abbreviation:  Phytother Res     Publication Date:  2000 Jun 
Date Detail:
Created Date:  2000-08-22     Completed Date:  2000-08-22     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  8904486     Medline TA:  Phytother Res     Country:  ENGLAND    
Other Details:
Languages:  eng     Pagination:  254-60     Citation Subset:  IM    
Copyright Information:
Copyright 2000 John Wiley & Sons, Ltd.
Affiliation:
Laboratory of Lipids and Antioxidants, Nutrition and Food Technology Institute, University of Chile, Santiago, Chile.
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MeSH Terms
Descriptor/Qualifier:
Animals
Aporphines / blood,  pharmacokinetics*
Liver / cytology,  metabolism
Male
Rats
Rats, Wistar
Chemical
Reg. No./Substance:
0/Aporphines; 476-70-0/boldine

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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