Key Laboratory of Combinatorial Biosynthesis and Drug Discovery Ministry of Education, School of Pharmaceutical Sciences , Wuhan University , Wuhan , Hubei Province 430071 , People's Republic of China.
Department of Pathogen Biology , Nanjing Medical University , Nanjing , Jiangsu Province 210029 , People's Republic of China.
J Nat Prod. 2019 Feb 22;82(2):318-323. doi: 10.1021/acs.jnatprod.8b00753. Epub 2019 Feb 12.
Armeniaspirols (1-3) are potent antibiotics against Gram-positive pathogens. Through a biosynthetic investigation, we identified four enzymes involved in the structural modification of 1-3. Manipulation of their activity led to the generation of 4-6 and nine novel analogues, 7-15. Bioactivity assessments revealed that the pyrrole chloro group and the methyl group are important for the antimicrobial activities of armeniaspirols, which lays the foundation for future structure optimization and mechanism of action studies of armeniaspirols.
Armeniaspirols（1-3）是针对革兰氏阳性病原体的强效抗生素。通过生物合成研究，我们鉴定出了四个参与 1-3 结构修饰的酶。对它们的活性进行操作导致了 4-6 和 9 个新类似物 7-15 的产生。生物活性评估表明，吡咯氯基团和甲基是 Armeniaspirols 抗菌活性的重要因素，这为未来的 Armeniaspirols 结构优化和作用机制研究奠定了基础。
