Document Detail


Calcium ionophoretic activity of chemically synthesized oligomeric derivatives of prostaglandin B1.
MedLine Citation:
PMID:  3828398     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Chemically synthesized dimers, trimers and tetramers of 15-dehydroprostaglandin B1 and 16,16'-dimethyl-15-dehydroprostaglandin B1 facilitate the release of Ca2+ from isolated rat liver mitochondria. The parent monomeric prostaglandins had no significant activity. The rate of release was stimulated by exogenous K+ or Na+, suggesting an antiport exchange of monovalent cations for intra-mitochondrial Ca2+. The activity depended upon the presence of ruthenium red, which prevented recycling of Ca2+; comparison of the activity with A23187 and carbonyl cyanide p-trifluoromethoxyphenylhydrazone indicated that the prostaglandin B1 oligomers were functioning as ionophores and the release of Ca2+ was not caused by an uncoupling of oxidative phosphorylation. The oligomers caused a major decrease in the membrane potential but only when the mitochondria were preloaded with exogenous Ca2+, and even then, the Ca2+ efflux was completed before the membrane potential decreased to less than 90 mV. The oligomeric molecules were able to form supramolecular aggregates in the presence of Ca2+ as detected by light scattering. They extracted Ca2+ into an organic phase, and translocated Ca2+ from one aqueous domain to another across an organic barrier; K+ and Na+ modulated these processes. The prostaglandin B1 derivatives also translocated Rb+ from one aqueous phase to another across an organic barrier when Ca2+ was translocated.
Authors:
S Uribe; S T Ohnishi; C Israelite; T M Devlin
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, Non-P.H.S.    
Journal Detail:
Title:  Biochimica et biophysica acta     Volume:  924     ISSN:  0006-3002     ISO Abbreviation:  Biochim. Biophys. Acta     Publication Date:  1987 Apr 
Date Detail:
Created Date:  1987-05-21     Completed Date:  1987-05-21     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  0217513     Medline TA:  Biochim Biophys Acta     Country:  NETHERLANDS    
Other Details:
Languages:  eng     Pagination:  87-98     Citation Subset:  IM    
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MeSH Terms
Descriptor/Qualifier:
Animals
Calcium / metabolism*
Intracellular Membranes / drug effects,  physiology
Ionophores / pharmacology*
Kinetics
Male
Membrane Potentials / drug effects
Mitochondria, Liver / drug effects,  metabolism*
Potassium / pharmacology
Prostaglandins / pharmacology*
Prostaglandins B / chemical synthesis,  pharmacology*
Rats
Rats, Inbred Strains
Sodium / pharmacology
Structure-Activity Relationship
Chemical
Reg. No./Substance:
0/16,16-dimethyl-15-dehydroprostaglandin B1 trimer; 0/Ionophores; 0/Prostaglandins; 0/Prostaglandins B; 7440-09-7/Potassium; 7440-23-5/Sodium; 7440-70-2/Calcium

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


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