Table of Contents
Metal-Based Drugs
Volume 2 (1995), Issue 5, Pages 257-269
http://dx.doi.org/10.1155/MBD.1995.257

The Relationship Between Cytokine Regulation and Anti-Inflammatory Action of Amine-Carboxyborane in L929 Fibroblasts and IC-21 Macrophages

1Division of Pharmaceutics, School of Pharmacy, University of North Carolina, Chapel Hill 27559-7360, North Carolina , USA
2Division of Medicinal Chemistry & Natural Products, School of Pharmacy, University of North Carolina, Chapel Hill 27559-7360, North Carolina , USA
3Boron Biologicals, Inc., 620 Hutton St., Raleigh 27606, N.C., USA

Received 14 July 1995; Accepted 23 August 1997

Copyright © 1995 Hindawi Publishing Corporation. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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.