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Bioactivity of Spongian Diterpenoid Scaffolds from the Antarctic Sponge Dendrilla antarctica.


ABSTRACT: 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.

SUBMITTER: Bory A 

PROVIDER: S-EPMC7344659 | biostudies-literature | 2020 Jun

REPOSITORIES: biostudies-literature

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Bioactivity of Spongian Diterpenoid Scaffolds from the Antarctic Sponge <i>Dendrilla antarctica</i>.

Bory Alexandre A   Shilling Andrew J AJ   Allen Jessie J   Azhari Ala A   Roth Alison A   Shaw Lindsey N LN   Kyle Dennis E DE   Adams John H JH   Amsler Charles D CD   McClintock James B JB   Baker Bill J BJ  

Marine drugs 20200623 6


The Antarctic sponge <i>Dendrilla antarctica</i> 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 <i>Leishmania donovani</i>, <i>Plasmodium falciparum</i>, and methicillin-resistant <i>Staphylococcus aureus</i> (MRSA) biofilm. In total, eleven natural products were is  ...[more]

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