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Calcium ionophoretic activity of chemically synthesized oligomeric derivatives of prostaglandin B1.
- Source :
-
Biochimica et biophysica acta [Biochim Biophys Acta] 1987 Apr 16; Vol. 924 (1), pp. 87-98. - Publication Year :
- 1987
-
Abstract
- 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.
- Subjects :
- Animals
Intracellular Membranes drug effects
Intracellular Membranes physiology
Kinetics
Male
Membrane Potentials drug effects
Mitochondria, Liver drug effects
Potassium pharmacology
Prostaglandins B chemical synthesis
Rats
Rats, Inbred Strains
Sodium pharmacology
Structure-Activity Relationship
Calcium metabolism
Ionophores pharmacology
Mitochondria, Liver metabolism
Prostaglandins pharmacology
Prostaglandins B pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 0006-3002
- Volume :
- 924
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- Biochimica et biophysica acta
- Publication Type :
- Academic Journal
- Accession number :
- 3828398
- Full Text :
- https://doi.org/10.1016/0304-4165(87)90074-2