Han Wen-Bo, Zhai Yi-Jie, Zhang Rong, Gong Xu-Shun, Li Jia-Qian, Xu Gong, Lei Xinxiang, Du Liangcheng, Gao Jin-Ming
Shaanxi Key Laboratory of Natural Products & Chemical Biology, College of Chemistry and Pharmacy, Northwest A&F University, Xian Yang Shi, Yangling, 712100, China.
College of Plant Protection, Northwest A&F University, Xian Yang Shi, Yangling, 712100, China.
Angew Chem Int Ed Engl. 2023 Apr 3;62(15):e202300773. doi: 10.1002/anie.202300773. Epub 2023 Mar 6.
Tricrilactones A-H (1-8), a new family of oligomeric 10-membered macrolides featuring collectively five unique ring skeletons, were isolated from a hitherto unexplored fungus, Trichocladium crispatum. Compounds 1 and 7 contain two unconventional bridged (aza)tricyclic core skeletons, 2, 3, 5, and 6 share an undescribed tetracyclic 9/5/6/6 ring system, 4 bears an uncommon 9/5/6/10/3-fused pentacyclic architecture, and 8 is a dimer bridged by an unexpected C-C linkage. Their structures, including absolute configurations, were elucidated by spectroscopic analysis, quantum chemical calculations, and X-ray diffraction analysis. Importantly, the absolute configuration of the highly flexible side chain of 1 was resolved by the asymmetric synthesis of its four stereoisomers. The intermediate-trapping and isotope labeling experiments facilitated the proposal of the biosynthetic pathway for these macrolides. In addition, their antiosteoporosis effects were evaluated in vivo (zebrafish).
从一种此前未被研究过的真菌——皱卷毛霉(Trichocladium crispatum)中分离得到了三聚内酯A - H(1 - 8),这是一类新型的低聚十元大环内酯类化合物,共有五个独特的环骨架。化合物1和7含有两个非常规的桥连(氮杂)三环核心骨架,2、3、5和6具有一种未描述过的四环9/5/6/6环系,4具有一种罕见的9/5/6/10/3稠合五环结构,而8是通过一个意外的C - C键连接的二聚体。通过光谱分析、量子化学计算和X射线衍射分析阐明了它们的结构,包括绝对构型。重要的是,通过1的四种立体异构体的不对称合成确定了其高度灵活侧链的绝对构型。中间体捕获和同位素标记实验有助于提出这些大环内酯类化合物的生物合成途径。此外,还在体内(斑马鱼)评估了它们的抗骨质疏松作用。