Characterization of the Biosynthetic Gene Cluster for the Antibiotic Armeniaspirols in Streptomyces armeniacus

  • J Nat Prod. 2019 Feb 22;82(2):318-323. doi: 10.1021/acs.jnatprod.8b00753.
Yongjian Qiao  1 ,  Jiayan Yan  1 ,  Jia Jia  2 ,  Jiao Xue  1 ,  Xudong Qu  1 ,  Yunfeng Hu  3 ,  Zixin Deng  1 ,  Hongkai Bi  2 ,  Dongqing Zhu  1
Affiliations
  • 1. 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.
  • 2. Department of Pathogen Biology , Nanjing Medical University , Nanjing , Jiangsu Province 210029 , People's Republic of China.
  • 3. CAS Key Laboratory of Tropical Marine Bio-resources and Ecology, Guangdong Key Laboratory of Marine Materia Medica, South China Sea Institute of Oceanology , Chinese Academy of Sciences , Guangzhou , Guangdong Province 510301 , People's Republic of China.
PMID: 30747534 DOI: 10.1021/acs.jnatprod.8b00753
Abstract

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.

Products