植物源内生真菌中的生物活性 PKS-NRPS 生物碱

School of Life Science and Engineering, Lanhzou University of Technology, Lanzhou 730050, China.

Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing 100010, China.

Molecules. 2021 Dec 27;27(1):136. doi: 10.3390/molecules27010136.

A novel hybrid PKS-NRPS alkaloid, xylarialoid A (), containing a 13-membered macrocyclic moiety and [5,5,6] fused tricarbocyclic rings, together with ten known cytochalasins (-), was isolated from a plant-derived endophytic fungus, . The chemical structures of all compounds were elucidated using 1D and 2D NMR, HR ESIMS spectroscopic analyses, and electronic circular dichroism (ECD) calculation. Compounds - and exhibited significant antitumor activities against A549 and Hep G2 cell lines, with IC values of 3.6-19.6 μM. In addition, compound showed potent anti-inflammatory activity against LPS-induced nitric oxide (NO) production in macrophage RAW 264.7 cells (IC, 6.6 μM).

一种新型杂合 PKS-NRPS 生物碱，木霉素 A（），含有一个 13 元的大环部分和 [5,5,6] 稠合的三环碳环，以及十个已知的细胞色素（-），从植物来源的内生真菌中分离得到。所有化合物的化学结构均通过 1D 和 2D NMR、高分辨率 ESIMS 光谱分析和电子圆二色性（ECD）计算确定。化合物 - 和对 A549 和 Hep G2 细胞系表现出显著的抗肿瘤活性，IC 值为 3.6-19.6 μM。此外，化合物对 LPS 诱导的巨噬细胞 RAW 264.7 细胞中一氧化氮（NO）的产生具有很强的抗炎活性（IC，6.6 μM）。