Bioactivity of Spongian Diterpenoid Scaffolds from the Antarctic Sponge Dendrilla antarctica.
Mar Drugs
; 18(6)2020 Jun 23.
Article
en En
| MEDLINE
| ID: mdl-32586020
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.
Palabras clave
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Poríferos
/
Diterpenos
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Leishmania
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Antiinfecciosos
Límite:
Animals
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Humans
Idioma:
En
Año:
2020
Tipo del documento:
Article