Phenolic compounds as antiangiogenic CMG2 inhibitors from costa rican endophytic fungi

Shugeng Cao, Lorna Cryan, Kaiane A. Habeshian, Catalina Murillo, Giselle Tamayo-Castillo, Michael S. Rogers, Jon Clardy

Research output: Contribution to journalArticlepeer-review

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.

Original languageEnglish (US)
Pages (from-to)5885-5888
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume22
Issue number18
DOIs
StatePublished - Sep 15 2012

Keywords

  • Aurapex penicillata
  • CMG2
  • Coccomyces proteae
  • Fungus
  • Phenolic

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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