Bioactivity of spongian diterpenoid scaffolds from the antarctic sponge dendrilla antarctica

Academic Article

Abstract

  • © 2020 MDPI AG. All rights reserved. The Antarctic sponge Dendrilla antarctica is rich in defensive terpenoids with promising antimicrobial potential. Investigation of this demosponge has resulted in the generation of a small chemical library containing diterpenoid secondary metabolites with bioactivity in an infectious disease screening campaign focused on Leishmania donovani, Plasmodium falciparum, and methicillin-resistant Staphylococcus aureus (MRSA) biofilm. In total, eleven natural products were isolated, including three new compounds designated dendrillins B D (10 12). Chemical modification of abundant natural products led to three semisynthetic derivatives (13 15), which were also screened. Several compounds showed potency against the leishmaniasis parasite, with the natural products tetrahydroaplysulphurin-1 (4) and dendrillin B (10), as well as the semisynthetic triol 15, displaying single-digit micromolar activity and low mammalian cytotoxicity. Triol 15 displayed the best profile against the liver-stage malaria parasites, while membranolide (5) and dendrillin C (11) were strong hits against MRSA biofilm cultures.
  • Published In

  • Marine Drugs  Journal
  • Digital Object Identifier (doi)

    Author List

  • Bory A; Shilling AJ; Allen J; Azhari A; Roth A; Shaw LN; Kyle DE; Adams JH; Amsler CD; McClintock JB
  • Volume

  • 18
  • Issue

  • 6