Macrolides with promotive activity of monocyte to macrophage differentiation

Abstract

We have been interested in the immunomodulatory effect, to promote differentiation of the human monocytic cell line THP-1 to macrophages of EM-A. We chemically modified EM-A in order to obtain derivatives with stronger promoting activity of monocyte to macrophage differentiation and no antibacterial activity. Most of the EM701 derivatives produced, all 12-membred macrolides, were remarkably active and were free of antibacterial activity. Among them, the most potent derivative was EM703, which showed very weak gastrointestinal motor-stimulating activity. EM703 may be useful tool to study the mechanisms of action of macrophage differentiation, and may be lead candidate for the development of new therapeutic drugs for chronic airway disease. © Japan Antibiotics Research Association.