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从红树林衍生的真菌中获得的具有潜在生物活性的多基化物

Huawei Lv¹, Haibo Su¹, Yaxin Xue²

¹College of Pharmaceutical Science & Key Laboratory of Marine Fishery Resources Exploitment & Utilization of Zhejiang Province, Zhejiang University of Technology, Hangzhou, 310014 China.

Marine life science & technology

|June 5, 2023

概括

微生物代谢物产生了新的depsidone和xanthone化合物,它们对Helicobacter pylori具有显著的抗微生物活性. 酸D还显示出强大的抗癌性质,突出了新药发现的潜力.

科学领域:

自然产品化学自然产品化学
微生物代谢学
药物发现药物发现药物发现

背景情况:

微生物代谢物是新药发现的丰富来源.
像Talaromyces物种一样,红树林衍生的真菌是已知的生物活性化合物的生产者.

研究的目的:

从Talaromyces物种WHUF0362.2.中分离和描述新的德西和桑衍生物.
评估分离化合物的抗微生物和细胞毒性活动.

主要方法:

使用乙酸乙烯提取的化合物的分离.
通过光谱数据分析和化学方法 (性水解,莫舍尔法) 阐明结构.
使用最小抑制度 (MIC) 试验对Helicobacter pylori进行抗菌活性测试.
使用IC50值对癌细胞系 (Bel-7402,HCT-116) 的细胞毒性评估.

主要成果:

分离了8种新的化合物 (五种depsidones:塔拉罗宁A-E,三种xanthones:塔拉罗宁F-H) 和16种已知的化合物.
化合物5,9,10和14对H. pylori表现出强烈的活性 (MICs为2.4236.04μmol/L).
酸D (19) 显示出显著的H. pylori抑制 (MICs 0.201.57 μmol/L) 和细胞毒性 (IC50 0.150.19 μmol/L).
结构-活性关系表明,乳环和C-10基对西抗菌活性至关重要.

结论:

塔拉罗米切斯物种 WHUF0362 是新型德普西和克桑衍生物的来源.
德普西衍生物显示出有前途的潜力,作为开发新抗生素对抗H.pylori的领导者.
红酸D显示出对抗微生物和抗癌应用的潜力.

关键词:

抗微生物药物抗微生物药物德普西多尼的使用方法来自红树林的真菌来源于红树林.塔拉罗米切斯 (Talaromyces) 种类.克桑 (Xanthone) 是一种有机化学物质.

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