链他唑啉类似物抗炎作用的设计、合成及生物学评价

IF 2.5 4区医学 Q3 CHEMISTRY, MEDICINAL

Bioorganic & Medicinal Chemistry Letters Pub Date : 2025-02-14 DOI:10.1016/j.bmcl.2025.130139

Shan Lu , Zhuang Li , Peng Jiang , Bo Jiang , Shanqin Huang , Xinhang Su , Ke Ma , Ying Xu , Lingling Ding , Di Mao

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引用次数: 0

摘要

从水菠菜（Ipomoea aquatica Forsk.）根中分离到一株植物内生放线菌Streptomyces sp. JS39-4。在优化的培养条件下，其主要次级代谢产物链唑啉(1)得到了高纯度的纯化。合成了16个C-5修饰的链他唑啉类似物。其中化合物2e对lps诱导的RAW 264.7小鼠巨噬细胞的抗炎活性最强。本研究首次报道了链唑啉类似物的抗炎活性。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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

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

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.

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来源期刊

Bioorganic & Medicinal Chemistry Letters 医学-医药化学

CiteScore

5.70

自引率

3.70%

发文量

463

审稿时长

27 days

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.