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螺旋A-E,五个螺旋来自于生产性盐水土壤,来源于Penicillium raistrickii

Desheng Liu¹, Liying Ma¹, Xianguo Rong¹

¹Laboratory of Natural Drug Discovery and Research, College of Pharmacy, Binzhou Medical University, Yantai, China.

Frontiers in microbiology

|December 9, 2024

概括

研究人员从Penicillium raistrickii中分离了五种新的真菌[6,6]-螺旋,螺旋A-E,从Penicillium raistrickii. 化合物4表现出抗菌活性,而化合物5表现出对癌细胞系的细胞毒性,这表明有可能开发新的药物.

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:

螺旋体以螺旋原子连接的两个环为特征,被认为具有多样化的生物活动.
真菌是独特化学结构的重要来源,但很少报告来自真菌来源的[6,6]-螺旋.
这项研究侧重于来自盐水土壤真菌,Penicillium raistrickii.的阿扎菲隆基[6,6]-螺旋.

研究的目的:

从Penicillium raistrickii的新型[6,6]-spiroketals中分离和描述其特征.
评估分离化合物的抗菌和细胞毒性活动.
修改已知类型的绝对配置,如佩斯塔福利德A.

主要方法:

使用二极管阵列检测 (HPLC-DAD) 的高性能液体染色学用于化合物隔离和紫外线检测.
频谱技术包括UV,IR,HRESIMS和1D/2DNMR用于结构阐明.
通过X射线单晶衍射和修改的莫舍尔法来确定绝对配置.

主要成果:

分离了五种新的以阿扎菲隆为基础的[6,6]-螺旋 (spirolones A-E) 和一种已知的类似物 (pestafolide A).
化合物4显示对 Pseudomonas aeruginosa 和 Escherichia coli 的抗菌活性.
化合物5对HepG2和Hep3B细胞系表现出细胞毒性,IC50值分别为3.40μM和8.14μM.

结论:

经过X射线结晶学分析,确定了Pestafolide A的修订绝对配置.
化合物4和5显示出开发新抗菌或抗瘤剂的潜力.
这项研究扩大了真菌[6,6]-spiroketals的化学多样性及其潜在的治疗应用.

关键词:

青素的种族主义者.它具有抗菌作用,具有抗菌作用.基于阿扎菲龙的螺旋基.细胞毒性细胞毒性盐土壤衍生的真菌菌.

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