Phenolic compounds as antiangiogenic CMG2 inhibitors from costa rican endophytic fungi
Fecha
2012
Tipo
artículo original
Autores
Cao, Shugeng
Cryan, Lorna
Habeshian, Kaiane A.
Murillo Cruz, Catalina
Tamayo Castillo, Giselle
Rogers, Michael S.
Clardy, Jon
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Resumen
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.
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Palabras clave
MUSHROOM, Coccomyces proteae, Aurapex penicillata, CMG2, Phenolic, COSTA RICA