ISSN:
0268-2605
Keywords:
Inflammation
;
amine carboxyboranes
;
metal complexes
;
HCT-8 toxicity
;
Chemistry
;
Organic Chemistry
Source:
Wiley InterScience Backfile Collection 1832-2000
Topics:
Chemistry and Pharmacology
Notes:
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 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 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.
Additional Material:
8 Tab.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1002/aoc.590080507
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