Exploitation of Mangrove Endophytic Fungi for Infectious Disease Drug Discovery.
Danielle H DemersMatthew A KnestrickRenee FleemanRahmy TawfikAla AzhariAshley SouzaBrian VeselyMandy NethertonRashmi GuptaBeatrice L ColonChristopher A RiceMario A Rodríguez-PérezKyle H RohdeDennis E KyleLindsey N ShawBill J BakerPublished in: Marine drugs (2018)
There is an acute need for new and effective agents to treat infectious diseases. We conducted a screening program to assess the potential of mangrove-derived endophytic fungi as a source of new antibiotics. Fungi cultured in the presence and absence of small molecule epigenetic modulators were screened against Mycobacterium tuberculosis and the ESKAPE panel of bacterial pathogens, as well as two eukaryotic infective agents, Leishmania donovani and Naegleria fowleri. By comparison of bioactivity data among treatments and targets, trends became evident, such as the result that more than 60% of active extracts were revealed to be selective to a single target. Validating the technique of using small molecules to dysregulate secondary metabolite production pathways, nearly half (44%) of those fungi producing active extracts only did so following histone deacetylase inhibitory (HDACi) or DNA methyltransferase inhibitory (DNMTi) treatment.
Keyphrases
- infectious diseases
- small molecule
- drug discovery
- histone deacetylase
- mycobacterium tuberculosis
- gene expression
- dna methylation
- protein protein
- electronic health record
- circulating tumor
- quality improvement
- endothelial cells
- single cell
- pulmonary tuberculosis
- respiratory failure
- cell free
- combination therapy
- antimicrobial resistance
- deep learning
- replacement therapy
- acute respiratory distress syndrome