来自内菌 Letendraea helminthicola A820 的二次代谢物具有抗炎活性
Jianpeng Zhang1,2, Ziling Tan2, Yuchan Chen2
1School of Traditional Chinese Medicine, Guangdong Pharmaceutical University, Guangzhou, 510006, China.
Chemistry & biodiversity
|September 28, 2024
概括
从Letendraea helminthicola真菌中分离出了两种新型的激进烯衍生物,即letendrones A-B. 这些天然产品显示出治疗抑郁症和心血管疾病的潜力.
科学领域:
- 自然产品化学 自然产品化学
- 菌类学 菌类学是指菌类学.
- 药用化学 医学化学
背景情况:
- 从 Aquilaria 分离出来的内生菌 Letendraea helminthicola A820 是生物活性二次代谢产物的来源.
- 烯衍生物是一种具有多种生物活性的自然产品.
研究的目的:
- 从Letendraea helminthicola A820.中分离和描述新的化合物.
- 评估分离化合物的生物活性和潜在的治疗应用.
主要方法:
- 使用色谱技术分离和净化真菌代谢物.
- 使用光谱方法 (1D/2D NMR,IR,UV,HRESIMS) 和X射线晶体学阐明结构.
- 在体外生物活性测定 (抑制NO生产) 和在分子对接研究.
主要成果:
- 确定了两种新的烯衍生物,莱特龙A-B (1-2),以及三种已知的化合物 (3-5).
- 化合物3-5在巨细胞中表现出对脂聚糖诱导的氧化生产的抑制活性.
- 化合物1对5-HT2c受体具有很高的结合亲和力,这表明它可能具有抗抑郁作用.
- 化合物2对二酶3A表现出显著的结合,表明潜在的心血管应用.
结论:
- 这项研究报告了首次分离具有激素形式的天然烯化合物.
- 列特伦A-B及其相关的生物活性为进一步研究列特伦海尔明提科拉代谢物的基础.
- 这些已识别的化合物对开发新型治疗抑郁症和心血管疾病的新疗法充满希望.
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