Effect of oligomeric derivatives of prostaglandin B1 on oxidative phosphorylation and their Ca2+ ionophoretic activity.

Dimers, trimers and tetramers of 15-dehydro-PGB1 and of 16,16'-dimethyl-15-dehydro-PGB1 have been synthesized and their effect on mitochondrial function evaluated. The trimers and tetramers, and to a lesser extent the dimers, of both series, protected isolated mitochondria from the loss of phosphorylating capacity during in vitro incubation. The monomers were inactive. The trimers and tetramers inhibited between 40 and 50% the F1F0-ATPase of submitochondrial particles. All of the oligomers, but not the monomers, had Ca2+ ionophoretic activity with isolated mitochondria. These activities are qualitatively similar to that reported for the oligomeric mixture of 15-dehydro-PGB1, termed PGBX.