利兰E-I,五度二元多基基化物,具有来自阿斯伯吉卢斯种类的潜在抗炎活性. 在AWG 1-15中,AWG 1-15是最常见的
Qun-Yan Jiang1, Guo-Ping Yin1, Ran He1
1State Key Laboratory of Natural Medicines, Jiangsu Key Laboratory of Bioactive Natural Product Research, School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing, P. R. China.
Chemistry & biodiversity
|April 7, 2025
概括
五种新的真菌化合物 - - 素E-I - - 显示出抗炎作用的潜力. 这些罕见的阿扎菲隆-富拉异构体抑制了免疫细胞中氧化的产生,表明了治疗的前景.
科学领域:
- 自然产品化学 自然产品化学
- 药用化学 医学化学
- 菌类学 菌类学是指菌类学.
背景情况:
- 的二次代谢产物,特别是多基,是新生物活性化合物的丰富来源.
- 阿斯伯吉勒斯种类是众所周知的多样化和复杂化学结构的生产者.
- 菌类多基菌的结构多样性为发现新的治疗剂提供了机会.
研究的目的:
- 从真菌Aspergillus sp.中分离和表征新的二维多基基菌. 在AWG 1-15.
- 为了研究分离的化合物的抗炎性质.
- 为了阐明这些独特的真菌代谢物的结构-活性关系.
主要方法:
- 使用色谱技术分离和净化化合物.
- 使用高分辨率电喷射电离质谱法 (HR-ESI-MS) 和广泛核磁共振 (NMR) 谱法进行结构阐明.
- 通过电子循环二元化 (ECD) 计算和化学衍生来确定绝对配置.
- 在体外抗炎试验测量氧化物 (NO) 在脂多糖 (LPS) 刺激的RAW 264.7巨细胞中的产量.
主要成果:
- 成功分离了五种新的二维多基基,被指定为化E-I (化合物1-5).
- 这些化合物代表了阿扎菲隆和 furanone 支架的罕见异构体.
- 化合物1-4通过抑制氧化的产生表现出适度的抗炎活性,IC50值在12.6至37.3μM之间,优于阳性对照.
结论:
- 这种真菌是Aspergillus sp. AWG 1-15产生独特的二维多基基,具有显著的抗炎功能.
- 酸E-I是一种新型的天然产品类别,具有作为抗炎药物的发展潜力.
- 需要对这些化合物的作用机制和优化进行进一步的研究.
相关概念视频
01:13Five-Membered Heterocyclic Aromatic Compounds: Overview
4.4K
Heterocyclic aromatic compounds are cyclic compounds that are aromatic and have one or more heteroatoms—atoms other than carbon, in the ring. Depending upon the number of atoms present in the ring, they can be either five or six-membered. Examples of five-membered heterocyclic aromatic compounds include pyrrole, furan, thiophene, and imidazole. Pyrrole consists of one nitrogen atom having one lone pair of electrons. Furan and thiophene have one oxygen and one sulfur heteroatom,...
4.4K
01:29Drugs for Treatment of Ulcerative Colitis in IBD
705
Ulcerative colitis is a chronic inflammatory condition primarily affecting the colon and rectum. The primary drugs used in the treatment of ulcerative colitis are aminosalicylates. They exhibit anti-inflammatory and immunosuppressive properties. They modulate inflammatory mediators and inhibit the activity of nuclear factor κB (NF-κB). Aminosalicylates also reduce inflammation by inhibiting prostaglandin and leukotriene production and decreasing neutrophil chemotaxis and superoxide...
705
01:28Fungal Phylum Ascomycota
2.4K
Phylum Ascomycota, a major division within the subkingdom Dikarya, comprises a diverse range of fungal species, including both unicellular yeasts and filamentous molds such as Aspergillus and Penicillium. These fungi thrive in a variety of habitats, from aquatic ecosystems to terrestrial environments, playing crucial ecological and economic roles.Morphology and ReproductionThe defining characteristic of Ascomycetes, commonly referred to as sac fungi, is the ascus—a sac-like structure that...
2.4K
01:15Antifungal Agents
119
Amphotericin B is a broad-spectrum antifungal agent that exploits structural differences between fungal and mammalian cell membranes. Its amphipathic structure—featuring a hydrophobic polyene-lactone ring and a hydrophilic region containing mycosamine and carboxylic acid groups—enables selective binding to ergosterol, a sterol predominantly found in fungal plasma membranes. This selective interaction underlies the drug’s antifungal activity, although weak binding to...
119