Document Detail


Hydrolysis and hepatotoxicity of retronecine diesters.
MedLine Citation:
PMID:  6818720     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Rates of alkaline hydrolysis of 18 natural or semisynthetic pyrrolizidine alkaloids, all retronecine diesters, have been compared. Steric hindrance around the ester groups was the major factor inhibiting hydrolysis. Relative rates of hydrolysis by esterases in a rat liver homogenate were also dependent on steric hindrance. However, in a series of less hindered esters with unbranched acids, hydrolysis rates increased with chain length to a maximum for the valeryl diester. Enzymic hydrolysis of retronecine di-isovalerate occurred primarily at the allylic 9-ester group. The results supported the view that a factor contributing to the lower hepatoxicity of semisynthetic retronecine diesters compared with some natural pyrrolizidine alkaloids, is their greater susceptibility to detoxication by hydrolysis.
Authors:
A R Mattocks
Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Toxicology letters     Volume:  14     ISSN:  0378-4274     ISO Abbreviation:  Toxicol. Lett.     Publication Date:  1982 Nov 
Date Detail:
Created Date:  1983-03-11     Completed Date:  1983-03-11     Revised Date:  2009-11-19    
Medline Journal Info:
Nlm Unique ID:  7709027     Medline TA:  Toxicol Lett     Country:  NETHERLANDS    
Other Details:
Languages:  eng     Pagination:  111-6     Citation Subset:  IM    
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MeSH Terms
Descriptor/Qualifier:
Animals
Drug-Induced Liver Injury / etiology*
Hydrolysis
Kinetics
Male
Monocrotaline
Pyrrolizidine Alkaloids / metabolism,  toxicity*
Rats
Rats, Inbred Strains
Chemical
Reg. No./Substance:
0/Pyrrolizidine Alkaloids; 315-22-0/Monocrotaline; 480-85-3/retronecine

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


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