A Dimeric sesquiterpenoid from a Malaysian Meiogyne as a new inhibitor of Bcl-xL/BakBH3 domain peptide interaction.

Autor: Litaudon M; Institut de Chimie des Substances Naturelles, 1 Avenue de la Terrasse, UPR2301, CNRS, 91198 Gif-sur-Yvette, France. litaudon@icsn.cnrs-gif.fr, Bousserouel H, Awang K, Nosjean O, Martin MT, Dau ME, Hadi HA, Boutin JA, Sévenet T, Guéritte F
Jazyk: angličtina
Zdroj: Journal of natural products [J Nat Prod] 2009 Mar 27; Vol. 72 (3), pp. 480-3.
DOI: 10.1021/np8006292
Abstrakt: In an effort to find potent inhibitors of the antiapoptotic protein Bcl-xL, a systematic in vitro evaluation was undertaken on 1470 Malaysian plant extracts. The ethyl acetate extract obtained from the bark of Meiogyne cylindrocarpa was selected for its interaction with the Bcl-xL/Bak association. Bioassay-guided purification of this species led to the isolation of two new dimeric sesquiterpenoids (1 and 2) possessing an unprecedented substituted cis-decalin carbon skeleton. Meiogynin A (1) showed the strongest activity with a K(i) of 10.8 +/- 3.1 microM.
Databáze: MEDLINE