2. Academic Validation
  3. Antibiotic Potential of the Ambigol Cyanobacterial Natural Product Class and Simplified Synthetic Analogs

Antibiotic Potential of the Ambigol Cyanobacterial Natural Product Class and Simplified Synthetic Analogs

  • ACS Infect Dis. 2023 Oct 13;9(10):1941-1948. doi: 10.1021/acsinfecdis.3c00232.
Tobias M Milzarek 1,  Milena Stevanovic 2,  Dusan Milivojevic 2,  Sandra Vojnovic 2,  Denis Iliasov 3,  Diana Wolf 3,  Thorsten Mascher 3,  Jasmina Nikodinovic-Runic 2,  Tobias A M Gulder 1 4 5
Affiliations

Affiliations

  • 1 Chair of Technical Biochemistry, Technische Universität Dresden, Bergstraße 66, 01069 Dresden, Germany.
  • 2 Institute of Molecular Genetics and Genetic Engineering, University of Belgrade, Vojvode Stepe 444a, 11000 Belgrade, Serbia.
  • 3 Chair of General Microbiology, Technische Universität Dresden, Zellescher Weg 20b, 01217 Dresden, Germany.
  • 4 Helmholtz Institute for Pharmaceutical Research Saarland (HIPS), Department of Natural Product Biotechnology, Helmholtz Centre for Infection Research (HZI), Saarland University, 66123 Saarbrücken, Germany.
  • 5 Department of Pharmacy, Saarland University, 66123 Saarbrücken, Germany.
PMID: 37655776 DOI: 10.1021/acsinfecdis.3c00232
Abstract

The ambigols are cyanobacterial natural products characterized by three polychlorinated aromatic building blocks connected by biaryl and biaryl ether bridges. All ambigols known to date possess promising biological activities. Most significantly, ambigol A was reported to have Antibacterial activity against Gram-positive bacteria, such as Bacillus megaterium and B. subtilis. We established a diverse compound library for in-depth biological evaluation building on our previous bio- and total synthetic research on this natural product family. To explore the antimicrobial potential in detail and to determine initial structure-activity relationships of this product class, a large set of dimeric and trimeric compounds were screened against selected Bacterial and Candida target strains. Our results reveal exceptional Antibiotic activity of the ambigols, especially against challenging clinical isolates.

Keywords

ambigols; antibiotic screening; cell membrane integrity; drug-resistant Staphylococcus aureus.

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