Study of marine natural products including resorcyclic acid lactones from Humicola fuscoatra that reactivate latent HIV-1 expression in an in vitro model of central memory CD4+ T cells.
J Nat Prod
; 77(3): 618-24, 2014 Mar 28.
Article
em En
| MEDLINE
| ID: mdl-24495105
ABSTRACT
An extract of Humicola fuscoatra (UCSC strain no. 108111A) was shown to reactivate latent HIV-1 expression in an in vitro model of central memory CD4+ T cells. We report the bioassay-guided isolation and structure determination of several resorcyclic acid lactones, including four known compounds, radicicol (1, aka. monorden) and pochonins B (2), C (3), and N (4), and three new analogues, radicicols B-D (5-7). Compounds 1-3 and 5 showed moderate activities in the memory T cell model of HIV-1 latency. Radicicol (1) displayed lower potency in reactivating latent HIV-1 (EC50 = 9.1 µM) relative to the HDAC inhibitors apicidin (EC50 = 0.3 µM), romidepsin (EC50 = 0.003 µM), and SAHA (EC50 = 0.6 µM); however, it achieved equivalent maximum efficacy relative to the positive control compounds (98% of SAHA and romidepsin).
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Ascomicetos
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Produtos Biológicos
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Linfócitos T CD4-Positivos
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HIV-1
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Macrolídeos
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Inibidores de Histona Desacetilases
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Lactonas
Limite:
Humans
Idioma:
En
Revista:
J Nat Prod
Ano de publicação:
2014
Tipo de documento:
Article
País de afiliação:
Estados Unidos