Laboratoire de Pharmacognosie, Faculté des Sciences Pharmaceutiques et Biologiques, Université Lille Nord de France, Lille, France.
Planta Med. 2010 Jan;76(1):86-7. doi: 10.1055/s-0029-1185972. Epub 2009 Jul 30.
Three methoxylated flavones isolated from Marrubium peregrinum - ladanein, scutellarein-5,7,4'-trimethyl ether, and scutellarein-5,6,7,4'-tetramethyl ether - were assayed for their cytotoxicity towards a recently developed dasatinib-resistant murine leukemia cell line (DA1-3b/M2 (BCR-ABL)), together with the structurally related non-methylated flavone scutellarein. The most active compound, ladanein, was looked for in 20 common Lamiaceae species by a quick HPLC screening. Among the possible positive results, the most interesting source was found to be Marrubium vulgare, which led to the isolation and identification of ladanein for the first time in this species. Ladanein also displayed moderate (20-40 microM) activities against K562, K562R (imatinib-resistant), and 697 human leukemia cell lines but was toxic neither to MOLM13 nor to human peripheral blood mononuclear cells. This work provides a common natural source for the hemi-synthesis of future ladanein-derived flavones and the study of their antileukemic activity.
从外来千里光（Marrubium peregrinum）中分离得到的三种甲氧基黄酮——拉坦内因、野黄芩素-5,7,4'-三甲醚和野黄芩素-5,6,7,4'-四甲醚——与结构相关的非甲基化黄酮野黄芩素一起，对最近开发的达沙替尼耐药的小鼠白血病细胞系（DA1-3b/M2（BCR-ABL））进行了细胞毒性测试。最具活性的化合物拉坦内因通过快速 HPLC 筛选在 20 种常见的唇形科植物中进行了检测。在可能的阳性结果中，最有趣的来源是普通百里香，这导致拉坦内因首次在该种植物中被分离和鉴定。拉坦内因对 K562、K562R（伊马替尼耐药）和 697 个人类白血病细胞系也具有中等（20-40 μM）的活性，但对 MOLM13 和人外周血单核细胞既没有毒性。这项工作为未来拉坦内因衍生黄酮类化合物的半合成提供了一种常见的天然来源，并研究了它们的抗白血病活性。
