Anti-inflammatory activity of amine cyanoboranes, amine carboxyboranes, and related compounds.

Amine cyanoboranes and amine carboxyboranes (boron analogs of alpha-amino acids) were shown to inhibit inflammation. The analogs effectively blocked general inflammation, induced arthritis, and the writhing reflex associated with inflammation pain, while the inflammation associated with pleurisy was marginally inhibited. The boron analogs were shown in vitro to inhibit the release of lysosomal enzymes from liver and polymorphonuclear neutrophils. Furthermore, prostaglandin synthesis was blocked by these agents at a low concentration, i.e., 10(-6) M. Liver oxidative phosphorylation processes also were uncoupled by these agents, but the migration of polymorphonuclear neutrophils was unaltered at 10(-4) M. The elevation of cyclic adenosine monophosphate levels in polymorphonuclear neutrophils correlated positively with in vivo antiarthritic activity. Initial studies in rodents demonstrated that these boron analogs can be used at safe therapeutic doses.