Anti-inflammatory activity of (polyphenolic)-sulfonates and their sodium 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 muM inhibited TNFalpha 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.
Hall
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IH
Division of Medicinal Chemistry and Natural Products School of Pharrnacy University of North Carolina Chapel Hill Chapel Hill North Carolina 27559-7360 USA.
Murphy
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Elkins
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