A new cytotoxic ent-kaurane-type diterpene named xylopioxyde (16,17-epoxy-15-oxo-ent-kauran-19-oic acid) has been isolated from the fruits of Xylopia aethiopica Dunal (Annonaceae) together with three known compounds, namely 15α-acetoxy-ent-kaur-16-en-19 oic acid (xylopic acid), 15-oxo-ent-kaur-16-en-19-oic acid and ent-kaur-16-en-19-oic acid. Xylopic acid, obtained in a good amount, has been successively converted in moderate to good yields into 15-hydroxy-ent-kaur-16-en-19-oic acid, 15-oxo-ent-kaur-16-en-19-oic acid and two new selective trypanocidal stereoisomers of 15-acetoxy-16,17-ent-epoxy-kauran-19-oic acid, respectively. All the compounds except the synthetic epoxides displayed cytotoxic effects on the mammalian fibroblast cell line MRC-5 as well as inhibitory effects on the growth of the bloodstream forms of Trypanosoma brucei brucei cells (strain 241).
Désiré SOH, Ernestine NKWENGOUA, Igor NGANTCHOU, Barthélemy NYASSE, Colette DENIER, Véronique HANNAERT, Kamel H. SHAKER and Bernd SCHNEIDER Xylopioxyde and other bioactive kaurane-diterpenes from Xylopia aethiopica Dunal (Annonaceae). J App Pharm Sci, 2013; 3 (12): 013-019.
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