Benzoquinones and Terphenyl Compounds As Phosphodiesterase-4B Inhibitors from a Fungus of the Order Chaetothyriales (MSX 47445)
- UNCG Author/Contributor (non-UNCG co-authors, if there are any, appear on document)
- Mario Figueroa Saldivar, Adjunct Faculty (Creator)
- Tyler Graf, Research Scientist (Creator)
- Nicholas Oberlies, Patricia A. Sullivan Distinguished Professor of Chemistry (Creator)
- Cedric J Pearce, Adjunct Professor (Creator)
- Huzefa A. Raja, Research Scientist (Creator)
- Institution
- The University of North Carolina at Greensboro (UNCG )
- Web Site: http://library.uncg.edu/
Abstract: Three bioactive compounds were isolated from an organic extract of an ascomycete fungus of the order Chaetothyriales (MSX 47445) using bioactivity-directed fractionation as part of a search for anticancer leads from filamentous fungi. Of these, two were benzoquinones [betulinan A (1) and betulinan C (3)], and the third was a terphenyl compound, BTH-II0204-207:A (2). The structures were elucidated using a set of spectroscopic and spectrometric techniques; the structure of the new compound (3) was confirmed via single-crystal X-ray diffraction. Compounds 1–3 were evaluated for cytotoxicity against a human cancer cell panel, for antimicrobial activity against Staphylococcus aureus and Candida albicans, and for phosphodiesterase (PDE4B2) inhibitory activities. The putative binding mode of 1–3 with PDE4B2 was examined using a validated docking protocol, and the binding and enzyme inhibitory activities were correlated.
Benzoquinones and Terphenyl Compounds As Phosphodiesterase-4B Inhibitors from a Fungus of the Order Chaetothyriales (MSX 47445)
PDF (Portable Document Format)
447 KB
Created on 12/10/2015
Views: 1991
Additional Information
- Publication
- Journal of Natural Products
- Language: English
- Date: 2013
- Keywords
- fungi, cancer, betulinan A (1), betulinan C (3), BTH-II0204-207:A (2)