Anti‐Inflammatory Activity of (Polyphenolic)‐Sulfonates and TheirSodium Salts in Rodents

Abstract

A series of polyphenolic-sulfonated compounds were observed to have potent anti-inflammatory activity and were protective against induced endotoxic shock in mice at 8 and 16 mg/kg, I.P. These agents proved to be potent elastase inhibitors in human leukocytes and J774-AI and IC-21 mouse macrophages as well as prostaglandin cyclo-oxygenase inhibitors in J774-AI macrophages. The compounds from 5 to 50 μM inhibited TNFα release from IC-21 macrophages and IL-1 release from mouse P388D1 macrophages induced by LPS. The binding of these cytokines to high affinity receptors on target cells, e.g. L929 fibroblasts and IL-2 in HuT78 T lymphoma cells, were also suppressed by the agents. These compounds blocked the adhesion of leukocytes and macrophages to the plasma membranes of L929 fibroblasts.

Cytotoxicity of Poly(Phenolic)Sulfonates and Their Sodium Salts in L1210 Lymphoid Leukemia Cells

“…Related to suramin is a class of sulfonic acid azo dyes, for example, Evans blue, which has been shown to be active against replication of the AIDS virus [6]. Recently a series of poly(phenolic)sulfonated compounds were shown to have potent anti-inflammatory activity and protection against induced endotoxic shock in mice at 8 and 16 mg/kg, I.P [8]. These agents prove to be potent elastase and prostaglandin cyclooxygenase inhibitors, blocking the release of TNFt and IL-1 release.…”