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四醇A-G:来自Aspergillus quadrilineata的七种未经描述的欧醇

Mengsha Wei¹, Xiaoxin Li¹, Hong Liao¹

¹Hubei Key Laboratory of Natural Medicinal Chemistry and Resource Evaluation, School of Pharmacy, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, 430030, People's Republic of China.

|July 2, 2023

概括

从Aspergillus quadrilineata中分离出了七种新的厄戈斯特醇,四斯特醇A-G. 四醇B,C,D和E表现出显著的免疫抑制活性,抑制T和B淋巴细胞的增殖.

科学领域:

自然产品化学化学
免疫学免疫学免疫学
菌类学菌类学是指菌类学.

背景情况:

欧戈斯特醇是具有多种生物活动的重要真菌固醇.
阿斯珀吉卢斯物种是已知的生物活性二次代谢产物的来源.
了解新型埃尔戈斯特的结构-活性关系对于药物发现至关重要.

研究的目的:

为了隔离和描述来自Aspergillus quadrilineata的新型ergosterols.
阐明新化合物的结构和绝对配置.
评估分离的欧戈斯特醇的免疫抑制潜力.

主要方法:

使用色谱技术分离化合物.
通过高分辨率电子喷射电离质谱法 (HRESIMS),核磁共振 (NMR) 光谱法和单晶X射线衍射来阐明结构.
量子化学计算用于绝对配置的确定.
使用T和B淋巴细胞增殖模型进行体外免疫抑制活性测定.

主要成果:

发现了七种新的厄戈斯特醇,被指定为四斯特醇AG.
四醇A-C是二同位素,在C-6处有一个2-基-基基组.
四斯特醇D-G是具有2,3-butanediol组在C-6.的epimers,在C-6.的位置上具有2,3-butanediol组.
四醇B和C显示T淋巴细胞增殖的强烈抑制 (IC50值为7.43和3.95微米).
四醇 D 和 E 强烈抑制了 B 淋巴细胞增殖 (IC50 值为 10.96 和 7.47 μM).

结论:

阿斯珀吉勒斯四线虫产生结构多样化的爱尔戈斯特醇,具有显著的免疫抑制性质.
四醇B,C,D和E代表了开发新型免疫调节剂的有希望的化合物.
这项研究扩大了已知的埃尔戈斯特的化学多样性及其生物活性.

关键词:

阿斯珀吉勒斯四行线性植物埃尔戈斯醇是一种固醇.具有免疫抑制活性的药物.这种植物属于Trichocomaceae.

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