An Effective Strategy for Identification of Highly Unstable Bacillaenes
An Effective Strategy for Identification of Highly Unstable Bacillaenes
复制标题
鉴定高度不稳定杆菌烯的有效策略
DOI：
10.1021/acs.jnatprod.9b00609
复制
发表时间：
2019-12-01
影响因子：
5.1
通讯作者：
Li, Wenli
中科院分区：
文献类型：
--
作者：
Li, Huayue;Han, Xiao;Li, Wenli
对不稳定化合物的探索是天然产物研究中很少探索的领域。我们将基因组学和代谢组学分析与生物测定指导的化合物挖掘相结合，以有效地探索不稳定的杆菌烯。采用DANS-SVI（二维核磁共振谱变强度单谱差异分析）方法从化合物混合物中鉴定出新的硅酸菌烯结构（2、4和5），并在严格控制的条件下进行了分离纯化。化合物1对多重耐药菌株具有抗菌活性，而糖基化降低了杆菌烯支架的活性。
Exploration of unstable compounds is a rarely explored area of natural product research. We describe the integration of genomic and metabolomic analyses with bioassay-guided compound mining to effectively explore unstable bacillaenes. New bacillaene structures (2, 4, and 5) were identified from compound mixtures using the DANS-SVI (differential analysis of 2D NMR spectrum single spectrum with variable intensities) method, which were further verified by the isolation of the pure compounds under strictly controlled conditions. Compound 1 exhibited antibacterial activity against multi-drug-resistant bacterial strains, while glycosylation decreased the activity of the bacillaene scaffold.