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氧化衍生物的前体导向生物合成与氧化生产抑制活性

Huiping Yu¹, Xuejing Hao¹, Yungeng Gao¹

¹State Key Laboratory of Applied Organic Chemistry, College of Chemistry and Chemical Engineering, Lanzhou University, 222 South Tianshui Road, Lanzhou, 730000, P. R. China.

Chembiochem : a European journal of chemical biology

|October 22, 2024

概括

研究人员开发了一种新的生物合成策略,从真菌中制造出新型的panepoxydone衍生物. 合成和测试了14种新化合物,其中一些显示出对氧化产生的显著抑制作用.

科学领域:

自然产品化学自然产品化学
生物合成生物合成
药用化学医学化学

背景情况:

帕涅波克西顿是一种天然的NF-κB抑制剂,来源于基菌种.
它的生物合成涉及通过氧化,环氧化和还原的prenylhydroquinone.
抑制NF-κB对于调节炎症反应至关重要.

研究的目的:

建立一个有效的前体导向生物合成策略,用于panepoxydone的结构扩张.
通过使用prenylhydroquinone类似物合成新的panepoxydone衍生物.
评估这些新化合物的抗炎潜力.

主要方法:

使用真菌Panus rudis的前体指导生物合成.
培养基的补充与前尼尔化类似物.
隔离和结构阐明十四种新的panepoxydone衍生物 (panepoxyquinoid A-N).
在RAW 264.7细胞中对脂聚糖 (LPS) 诱导的氧化 (NO) 生产的抑制活性进行体外评估.

主要成果:

已经成功合成了14种新的panepoxydone衍生物 (化合物2-14).
化合物1,5-6,10-11和14-15显示显著抑制了LPS诱导的NO生产.
这些活性化合物的IC50值在4.3至30.1μM之间.

结论:

开发的前体导向生物合成策略是有效的产生不同的panepoxydone类似物.
几种新的panepoxydone衍生物对氧化生产表现出强烈的抑制活性,这表明它们具有潜在的抗炎性质.
这些发现为开发针对炎症途径的新治疗剂开辟了道路.

关键词:

没有生产,没有生产.自然产品是一种自然产品.帕涅波克西多尼 (Panepoxydone) 是一种帕努斯·鲁迪斯 (Panus rudis) 是一种常见的食物.前体指导生物合成的前体.

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