Unité Mixte de Service 2597, Centre National de la Recherche Scientifique (CNRS)-Pierre Fabre, Institut des Sciences et Technologies du Médicament de Toulouse (ISTMT), Toulouse, France.
Planta Med. 2011 Mar;77(5):461-6. doi: 10.1055/s-0030-1250407. Epub 2010 Oct 13.
Six protoflavonoids, including two new compounds, were isolated during a large scale screening of fern extracts for original interaction with mitosis. The new compounds isolated from PHEGOPTERIS decursive-pinnata and EQUISETUM fluviatile were 2',3'-dihydroprotogenkwanone (1) and 2',3'-dihydro-2'-hydroxyprotoapigenone (2). Known compounds were: protoapigenone, protogenkwanone, protoapigenin, and 4'- O- β-D-glucopyranosyl protoapigenin. They showed a cytotoxic activity against HeLa cells at a micromolar level. IC₅₀ values were 2 µM for compound 1 > 10 µM for compound 2, and respectively 2.4, 0.6, > 10 µM for the known compounds. Their cytotoxic effects were associated with phenotypic changes never observed before and characterized by the loss of centrosomal γ-tubulin labelling in both mitotic and interphasic cells.
在大规模筛选蕨类植物提取物以寻找与有丝分裂原初相互作用的物质时，分离得到了六种原黄酮类化合物，包括两种新化合物。从 PHEGOPTERIS decursive-pinnata 和 EQUISETUM fluviatile 中分离得到的新化合物为 2',3'-二氢原儿茶酮（1）和 2',3'-二氢-2'-羟基原芹菜素（2）。已知化合物为：原芹菜素、原儿茶酮、原芹菜苷和 4'-O-β-D-吡喃葡萄糖基原芹菜素。它们对 HeLa 细胞表现出微摩尔级别的细胞毒性。化合物 1 的 IC₅₀ 值为 2 µM>化合物 2 的 IC₅₀ 值为 10 µM，而已知化合物的 IC₅₀ 值分别为 2.4、0.6、>10 µM。它们的细胞毒性作用与以前从未观察到的表型变化相关，其特征是有丝分裂和间期中细胞中心体 γ-微管蛋白标记的丧失。
