A Dimeric Sesquiterpenoid from a Malaysian Meiogyne as a New Inhibitor of Bcl-xL/BakBH3 Domain Peptide Interaction

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. B...

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Veröffentlicht in:	Journal of natural products (Washington, D.C.) D.C.), 2009-03, Vol.72 (3), p.480-483
Hauptverfasser:	Litaudon, Marc, Bousserouel, Hadjira, Awang, Khalijah, Nosjean, Olivier, Martin, Marie-Thérèse, Dau, Marie Elise Tran Huu, Hadi, Hamid A, Boutin, Jean A, Sévenet, Thierry, Guéritte, Françoise
Format:	Artikel
Sprache:	eng
Schlagworte:	Annonaceae anticarcinogenic activity biochemical pathways Biological and medical sciences Cellular Biology chemical structure cytotoxicity General pharmacology Life Sciences Malaysia Medical sciences medicinal properties Meiogyne cylindrocarpa meiogynin Molecular Structure Pharmacognosy. Homeopathy. Health food Pharmacology. Drug treatments Plant Bark - chemistry Proto-Oncogene Proteins c-bcl-2 - antagonists & inhibitors Sesquiterpenes - chemistry Sesquiterpenes - isolation & purification Sesquiterpenes - pharmacology sesquiterpenoids spectral analysis stereochemistry Stereoisomerism
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Zusammenfassung:	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 μM.
ISSN:	0163-3864 1520-6025
DOI:	10.1021/np8006292