Ih. Hall et al., THE ANTIINFLAMMATORY ACTIVITY OF METAL-COMPLEXES AND SALTS OF AMINE CARBOXYBORANES, Applied organometallic chemistry, 8(5), 1994, pp. 473-480
The metal complexes and salts of amine carboxyboranes were shown to be
potent anti-inflammatory agents in rodents at 8 mg kg-1. They were ef
fective in blocking induced edema, pleurisy and endotoxic shock while
blocking both local and central pain processes. The ability of the age
nts to function as anti-inflammatory agents is multi-fold. First, lyso
somal enzymes of specific cells, e.g. macrophages, were inhibited with
IC50 values in the range of 10(-6) M. Collagenase I and II activities
were inhibited with IC50 values approximately equal to 10(-4) M. The
anti-inflammatory activity of these agents at the molecular levels app
ears to be due to inhibition of the release of TNFalpha and Il-1 from
macrophages which indirectly control chemotaxic migration of white blo
od cells as indicated by the suppression of PMN and macrophage invasio
n into sponges implanted subcutaneously (SC) in mice. Furthermore, in
these invading cells, the agents' blockage of TNFalpha and Il-1 or Il-
2 release down-regulates prostaglandin and leukotriene enzymatic synth
etic rates and, consequently, their release, resulting in a reduction
of the inflammation process.