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

  • Bioorg Med Chem Lett. 2025 Feb 14:120:130139. doi: 10.1016/j.bmcl.2025.130139.
Shan Lu  1 ,  Zhuang Li  1 ,  Peng Jiang  2 ,  Bo Jiang  3 ,  Shanqin Huang  1 ,  Xinhang Su  1 ,  Ke Ma  1 ,  Ying Xu  1 ,  Lingling Ding  4 ,  Di Mao  5
Affiliations
  • 1. School of Pharmacy, Jiangsu University, Zhenjiang 212013, China.
  • 2. Department of Physiology, School of Medicine, Jiangsu University, Zhenjiang 212013, China.
  • 3. Shanghai Changning Mental Health Center, Affiliated Mental Health Center of East China Normal University, Shanghai, 200335, China.
  • 4. Department of Physiology, School of Medicine, Jiangsu University, Zhenjiang 212013, China. Electronic address: [email protected].
  • 5. School of Pharmacy, Jiangsu University, Zhenjiang 212013, China. Electronic address: [email protected].
PMID: 39956275 DOI: 10.1016/j.bmcl.2025.130139
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.

Keywords
Anti-inflammatory activity; Streptazolin; Structure-activity relationship; Synthesis.
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