Jullian Valérie, Bonduelle Colin, Valentin Alexis, Acebey Lucia, Duigou Anne-Gaëlle, Prévost Marie-Francoise, Sauvain Michel
UMR 152 (IRD-UPS) Institut de Recherche pour le Développement-Université Paul Sabatier, Faculté de Pharmacie, 35 chemin des Maraîchers, 31062 Toulouse cedex 04, France.
Bioorg Med Chem Lett. 2005 Nov 15;15(22):5065-70. doi: 10.1016/j.bmcl.2005.07.090.
Extracts of Laetia procera (Flacourtiaceae) displayed significant in vitro activity against Plasmodium falciparum. P. falciparum bioassay guided fractionation of a trunk bark extract of this plant led to the isolation of six clerodane diterpenoids (1-6) and a butanolide (7). Five of these compounds are new and called Laetiaprocerine A-D (3-6) and Laetianolide A (7). Their structures were established on the basis of 1D and 2D NMR experiments. Absolute configurations of 1 and 2 were determined by a modified Mosher's method and the absolute configuration of 5 by chemical correlation. The clerodane diterpenoids displayed activities against P. falciparum with an IC50 down to 0.5 microM on FCb1 and F32 strains, and also cytotoxicity toward human tumor cell line MCF7. The most active compound showed a selectivity index of 6.8. Some of these compounds also displayed activities against Leishmania amazonensis amastigote axenic stages and promastigote.
长叶拉蒂木（大风子科）提取物对恶性疟原虫显示出显著的体外活性。通过恶性疟原虫生物测定法对该植物树干树皮提取物进行分级分离，得到了六种克罗烷二萜（1 - 6）和一种丁内酯（7）。其中五种化合物是新的，分别称为长叶拉蒂木素A - D（3 - 6）和拉蒂内酯A（7）。它们的结构是基于一维和二维核磁共振实验确定的。1和2的绝对构型通过改良的莫舍尔方法确定，5的绝对构型通过化学关联确定。克罗烷二萜对恶性疟原虫具有活性，在FCb1和F32菌株上的IC50低至0.5微摩尔，并且对人肿瘤细胞系MCF7也具有细胞毒性。活性最强的化合物的选择性指数为6.8。其中一些化合物对亚马逊利什曼原虫无鞭毛体体外阶段和前鞭毛体也具有活性。
