Shan Lu , Zhuang Li , Peng Jiang , Bo Jiang , Shanqin Huang , Xinhang Su , Ke Ma , Ying Xu , Lingling Ding , Di Mao
{"title":"Design, synthesis and biological evaluation of Streptazolin analogs as anti-inflammatory agents","authors":"Shan Lu , Zhuang Li , Peng Jiang , Bo Jiang , Shanqin Huang , Xinhang Su , Ke Ma , Ying Xu , Lingling Ding , Di Mao","doi":"10.1016/j.bmcl.2025.130139","DOIUrl":null,"url":null,"abstract":"<div><div>A plant endophytic actinomycete <em>Streptomyces</em> sp. JS39–4 was isolated from the root of water spinach (<em>Ipomoea aquatica</em> Forsk.). Its main secondary metabolite streptazolin (<strong>1</strong>) 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 <strong>2e</strong> 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.</div></div>","PeriodicalId":256,"journal":{"name":"Bioorganic & Medicinal Chemistry Letters","volume":"120 ","pages":"Article 130139"},"PeriodicalIF":2.5000,"publicationDate":"2025-02-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Bioorganic & Medicinal Chemistry Letters","FirstCategoryId":"3","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S0960894X25000484","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
引用次数: 0
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.
期刊介绍：
Bioorganic & Medicinal Chemistry Letters presents preliminary experimental or theoretical research results of outstanding significance and timeliness on all aspects of science at the interface of chemistry and biology and on major advances in drug design and development. The journal publishes articles in the form of communications reporting experimental or theoretical results of special interest, and strives to provide maximum dissemination to a large, international audience.
京公网安备 11010802042870号
京ICP备2023020795号-1
分享
求助内容：
应助结果提醒方式：
扫码关注我们
