2. Academic Validation
  3. 3-Oxo-γ-costic acid fungal-transformation generates eudesmane sesquiterpenes with in vitro tumor-inhibitory activity

3-Oxo-γ-costic acid fungal-transformation generates eudesmane sesquiterpenes with in vitro tumor-inhibitory activity

  • Bioorg Med Chem Lett. 2017 Aug 15;27(16):3825-3828. doi: 10.1016/j.bmcl.2017.06.057.
Mohamed-Elamir F Hegazy 1,  Ahmed A El-Beih 2,  Ahmed R Hamed 3,  Abeer A Abd El Aty 2,  Naglaa S Mohamed 4,  Paul W Paré 5
Affiliations

Affiliations

  • 1 Phytochemistry Department, National Research Centre, El-Tahrir Street, Dokki, Giza 12622, Egypt.
  • 2 Chemistry of Natural & Microbial Products, National Research Centre, El-Tahrir Street, Dokki, Giza 12622, Egypt.
  • 3 Phytochemistry Department, National Research Centre, El-Tahrir Street, Dokki, Giza 12622, Egypt; Biology Unit, Central Laboratory for Pharmaceutical and Drug Industries Research Division, Egypt.
  • 4 Chemistry Department, Faculty of Science, Aswan University, Aswan, Egypt.
  • 5 Department of Chemistry, Texas Tech University, Lubbock, TX 79409, USA. Electronic address: Paul.Pare@ttu.edu.
PMID: 28676273 DOI: 10.1016/j.bmcl.2017.06.057
Abstract

While select eudesmane Sesquiterpenes exhibit anti-neoplastic activity, tumor-inhibition for costic-acids has not been established. Here biological activity of 3-oxo-γ-costic acid (1), previously isolated from Chiliadenus montanus, as well as new Sesquiterpenes (2-5) and the known derivative, 3-oxoeudesma-1,4,11(13)-trien-7-1061αH-l2-oic acid (6), all produced from 1 by the fungus Athelia rolfsii, are reported. Structures were elucidated using MS and NMR spectroscopy with activity-screening utilizing human colon- and lung-tumor lines, Caco-2 and A549 respectively. Compound 1 exhibited anti-proliferative activity against Caco-2 (IC50 39µM) and 2 was active against A549 (IC50 74µM) suggesting therapeutic potential for the original substrate and a bio-transformed product.

Keywords

3-Oxo-γ-costic acid; Athelia rolfsii; Chiliadenus montanus; Fungal transformation; Tumor inhibition activity.

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