Activity of ladanein on leukemia cell lines and its occurrence in Marrubium vulgare.

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.
AuthorsRacha Alkhatib, Sami Joha, Meyling Cheok, Vincent Roumy, Thierry Idziorek, Claude Preudhomme, Bruno Quesnel, Sevser Sahpaz, François Bailleul, Thierry Hennebelle
JournalPlanta medica (Planta Med) Vol. 76 Issue 1 Pg. 86-7 (Jan 2010) ISSN: 1439-0221 [Electronic] Germany
PMID19644796 (Publication Type: Letter)
CopyrightCopyright Georg Thieme Verlag KG Stuttgart . New York.
Chemical References
  • Antineoplastic Agents, Phytogenic
  • Flavones
  • Plant Extracts
  • ladanein
  • Animals
  • Antineoplastic Agents, Phytogenic (isolation & purification, pharmacology, therapeutic use)
  • Cell Line, Tumor
  • Flavones (isolation & purification, pharmacology, therapeutic use)
  • Humans
  • Leukemia (drug therapy)
  • Marrubium (chemistry)
  • Mice
  • Phytotherapy
  • Plant Extracts (chemistry, pharmacology, therapeutic use)

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