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

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 P388 D1 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.