Design, synthesis and biological evaluation of Streptazolin analogs as anti-inflammatory agents

Abstract

A plant endophytic actinomycete Streptomyces sp. JS39–4 was isolated from the root of water spinach (Ipomoea aquatica Forsk.). Its main secondary metabolite streptazolin (1) was purified in a high yield under the optimized cultural condition. Sixteen analogs of streptazolin with modification at C-5 were synthesized. Among them, compound 2e exhibits the most potent anti-inflammatory activity in LPS-induced RAW 264.7 mouse macrophages. The current research provides the first report on the anti-inflammatory activity of streptazolin analogs.