Phenolic compounds as antiangiogenic CMG2 inhibitors from Costa Rican endophytic fungi.
Bioorg Med Chem Lett
; 22(18): 5885-8, 2012 Sep 15.
Article
em En
| MEDLINE
| ID: mdl-22910038
ABSTRACT
Targeting and inhibiting CMG2 (Capillary Morphogenesis Gene protein 2) represents a new strategy for therapeutic agents for cancer and retinal diseases due to CMG2's role in blood vessel growth (angiogenesis). A high throughput FRET (Förster Resonance Energy Transfer) assay was developed for the identification of CMG2 inhibitors as anti-angiogenetic agents. Bioassay-guided separation led to the isolation and identification of two new compounds (1 and 2) from CR252M, an endophytic fungus Coccomyces proteae collected from a Costa Rican rainforest, and one known compound (3) from CR1207B (Aurapex penicillata). Secondary in vitro assays indicated anti-angiogenic activity. Compound 3 inhibited the endothelial cell migration at 52 µM, but did not show any endothelial cell antiproliferative effect at 156 µM. The structure of the two new compounds, A (1) and B (2), were elucidated on the basis of extensive spectroscopic analysis, including 1D and 2D NMR experiments.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Fenóis
/
Ascomicetos
/
Proteínas de Membrana
Limite:
Humans
País como assunto:
America central
/
Costa rica
Idioma:
En
Ano de publicação:
2012
Tipo de documento:
Article