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The anti‐inflammatory activity of metal complexes and salts of amine carboxyboranes
Author(s) -
Hall Iris H.,
Rajendran K. G.,
Chen S. Y.,
Norwood V. N.,
Morse K. W.,
Sood A.,
Spielvogel B. F.
Publication year - 1994
Publication title -
applied organometallic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.53
H-Index - 71
eISSN - 1099-0739
pISSN - 0268-2605
DOI - 10.1002/aoc.590080507
Subject(s) - chemistry , inflammation , pharmacology , carrageenan , leukotriene b4 , enzyme , macrophage , pleurisy , biochemistry , in vitro , immunology , medicine , biology , pleural effusion
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 effective in blocking induced edema, pleurisy and endotoxic shock while blocking both local and central pain processes. The ability of the agents to function as anti‐inflammatory agents is multi‐fold. First, lysosomal enzymes of specific cells, e.g. macrophages, were inhibited with IC 50 values in the range of 10 −6 M . Collagenase I and II activities were inhibited with IC 50 values approximately equal to 10 −4 M . The anti‐inflammatory activity of these agents at the molecular levels appears to be due to inhibition of the release of TNFα and Il‐1 from macrophages which indirectly control chemotaxic migration of white blood cells as indicated by the suppression of PMN and macrophage invasion into sponges implanted subcutaneously (SC) in mice. Furthermore, in these invading cells, the agents' blockage of TNFα and Il‐1 or Il‐2 release down‐regulates prostaglandin and leukotriene enzymatic synthetic rates and, consequently, their release, resulting in a reduction of the inflammation process.