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.
journal_name
Mar Drugsjournal_title
Marine drugsauthors
Bory A,Shilling AJ,Allen J,Azhari A,Roth A,Shaw LN,Kyle DE,Adams JH,Amsler CD,McClintock JB,Baker BJdoi
10.3390/md18060327subject
Has Abstractpub_date
2020-06-23 00:00:00issue
6issn
1660-3397pii
md18060327journal_volume
18pub_type
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