Document Detail


Selective inhibition of group II phospholipase A2 by quercetin.
MedLine Citation:
PMID:  8225564     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The influence of quercetin, chlorpromazine, aristolochic acid, and indomethacin on group I phospholipase A2 (PLA2) from porcine pancreas and on group II PLA2 from Vipera russelli was compared. Quercetin and chlorpromazine were found to inhibit PLA2 activity in lower concentrations (< 100 microM), while aristolochic acid and indomethacin were inhibitory only in higher concentrations (> 100 microM). The order of potency against Vipera PLA2 was: quercetin > chlorpromazine > aristolochic acid > indomethacin, while the order of potency against pancreatic PLA2 was: chlorpromazine > aristolochic acid > indomethacin >> quercetin. Thus, quercetin was a potent inhibitor towards group II PLA2 (IC50 = 2 microM), but a very weak inhibitor against group I PLA2, with maximum 30% inhibition. Aristolochic acid and indomethacin were three to four times more potent towards group II PLA2 than towards group I PLA2, while chlorpromazine was equally potent towards the two PLA2 types. Quercetin and chlorpromazine were also tested against two PLA2 fractions purified from the plasma of septic shock patients; chlorpromazine was then equally potent towards the two PLA2 fractions, whereas quercetin was a potent inhibitor of only one of the two PLA2 fractions (IC50 = 4 microM). Together, these results indicate that (1) different PLA2 inhibitors have different potency depending on which type of PLA2 they are used against, (2) quercetin selectively inhibits group II PLA2 and may therefore be used to discriminate between different PLA2 forms in biological materials, and (3) both PLA2 of group I and group II are present in septic shock plasma.
Authors:
M Lindahl; C Tagesson
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Publication Detail:
Type:  Comparative Study; Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Inflammation     Volume:  17     ISSN:  0360-3997     ISO Abbreviation:  Inflammation     Publication Date:  1993 Oct 
Date Detail:
Created Date:  1993-12-13     Completed Date:  1993-12-13     Revised Date:  2007-11-15    
Medline Journal Info:
Nlm Unique ID:  7600105     Medline TA:  Inflammation     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  573-82     Citation Subset:  IM    
Affiliation:
Department of Clinical Chemistry, University of Linköping, Sweden.
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MeSH Terms
Descriptor/Qualifier:
Animals
Aristolochic Acids*
Chlorpromazine / pharmacology
Humans
Indomethacin / pharmacology
Pancreas / enzymology
Phenanthrenes / pharmacology
Phospholipases A / antagonists & inhibitors*,  blood
Phospholipases A2
Quercetin / pharmacology*
Shock, Septic / enzymology
Substrate Specificity
Swine
Viper Venoms / enzymology
Chemical
Reg. No./Substance:
0/Aristolochic Acids; 0/Phenanthrenes; 0/Viper Venoms; 117-39-5/Quercetin; 313-67-7/aristolochic acid I; 50-53-3/Chlorpromazine; 53-86-1/Indomethacin; EC 3.1.1.-/Phospholipases A; EC 3.1.1.4/Phospholipases A2

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