Mouriès Christine, Rakotondramasy Vokatsoa C, Libot Francine, Koch Michel, Tillequin François, Deguin Brigitte
Laboratoire de Pharmacognosie de l'Université René Descartes, U.M.R./C.N.R.S. no8638, Faculté des Sciences Pharmaceutiques et Biologiques, 4, Avenue de l'Observatoire, F-75006 Paris.
Chem Biodivers. 2005 May;2(5):695-703. doi: 10.1002/cbdv.200590046.
The novel iridoid glycoside 2 was prepared in six steps (15% overall yield) from natural aucubin (1) and fully characterized. Compound 2, which comprises the same conjugated cyclopentenone pharmacophore as known antitumor oxylipins and prostaglandins, displayed significant antiproliferative in vitro activity towards leukemia L1210 cells. The Michael addition of nucleophilic thiols to compound 2 occurred on a different position compared to classical delta7-prostaglandin A1 methyl ester. The resulting adducts 7a and 7b were fully characterized, and their MS fragmentation patterns were elucidated.
新型环烯醚萜苷2由天然桃叶珊瑚苷（1）经六步反应制备而成（总产率15%），并对其进行了全面表征。化合物2含有与已知抗肿瘤氧化脂质和前列腺素相同的共轭环戊烯酮药效基团，对白血病L1210细胞显示出显著的体外抗增殖活性。与经典的δ7-前列腺素A1甲酯相比，亲核硫醇对化合物2的迈克尔加成发生在不同位置。对所得加合物7a和7b进行了全面表征，并阐明了它们的质谱裂解模式。
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