Anti-Zika virus activity of several abietane-type ferruginol analogues

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Citações na Scopus
12
Tipo de produção
article
Data de publicação
2020
Título da Revista
ISSN da Revista
Título do Volume
Editora
INST MEDICINA TROPICAL SAO PAULO
Citação
REVISTA DO INSTITUTO DE MEDICINA TROPICAL DE SAO PAULO, v.62, article ID e97, 4p, 2020
Projetos de Pesquisa
Unidades Organizacionais
Fascículo
Resumo
Abietane diterpenoids are naturally occurring plant metabolites with a broad spectrum of biological effects including antibacterial. antileishmanial, antitumor, antioxidant, as well as antiinfiammatory activities. Recently, we found that some analogues of natural ferruginol (2) actively inhibited dengue virus 2 (DENV-2) replication. Due to the similarity with DENY, we envisaged that abietane diteipenoids would also be active against Zika virus (ZIKV). Six selected semi-synthetic abietane derivatives of (+)-dehydroabietylatnine (3) were tested. Cytotoxicity was determined by Mn' assay in Vero cells. In vitro anti-ZIKV (clinical isolate. imT17) activity was evaluated by plaque assay. Interestingly, these molecules showed potential as anti-ZIKV agents, with EC50 values ranging from 0.67 to 18.57 mu M. and cytotoxicity (CC50 values) from 256 to 35.09 mu M. The 18-Oxoferruginol (8) (EC50 = 2.60 mu M, SI = 13.51) and 12-nitro-N-benzoyldehydroabietylamine (9) (ECG 0.67 mu M, SI = 3.82) were the most active compounds, followed by 12-hydroxy-N-tosyldehydroabietylamine (7) (EC50 = 3.58 mu M, SI = 3.20) and 12-hydroxy-N,N-phthaloyldehydroabietylamine (5) (EC50 = 7.76 mu M, SI = 1.23). To the best of our knowledge, this is the first report on anti-Zika virus properties of abietanes.
Palavras-chave
Zika, Abietane, Ditelpenoid, Semi-synthesis, Anti-ZIKV activity
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