The Antarctic sponge 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 , , and methicillin-resistant (MRSA) biofilm. In total, eleven natural products were isolated, including three new compounds designated dendrillins B-D (-). Chemical modification of abundant natural products led to three semisynthetic derivatives (-), which were also screened. Several compounds showed potency against the leishmaniasis parasite, with the natural products tetrahydroaplysulphurin-1 () and dendrillin B (), as well as the semisynthetic triol , displaying single-digit micromolar activity and low mammalian cytotoxicity. Triol displayed the best profile against the liver-stage malaria parasites, while membranolide () and dendrillin C () were strong hits against MRSA biofilm cultures.
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| http://dx.doi.org/10.3390/md18060327 | DOI Listing |
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