The Relationship Between Cytokine Regulation and Anti-Inflammatory
Action of Amine-Carboxyborane in L929 Fibroblasts and IC-21
Macrophages
Margaret E. Murphy,1Robert P. Shrewsbury,1Anup Sood,3Bernard F. Spielvogel,3Amy L. Elkins,2and Iris Hall2
Received14 Jul 1995
Accepted23 Aug 1997
Abstract
The amine-carboxyboranes anti-inflammatory agents were shown to block
TNFα release at 90 min. and IL-1 release at 5 hr. from macrophages.
The agenst competed with L929 fibroblasts high affinity receptors for
endogenous cytokines which regulate the inflammation process. Blocking
the TNFα
receptor at 90 min. by the agents from 10 to 50 μΜ
, resulted in
lysosomal hydrolytic enzyme inhibition and lowering of prostaglandin
synthesis as well as reductions in calcitonin high affinity receptor
binding and calcium influx into the cells. IL-1 receptors when blocked
by the agents at 5 hr. resulted in a reduction of NAG activity and
leukotriene synthesis. An elevation of proline incorporation into
collagen occurred at 90 min. and 24 hr. in the presence of the agents.