Ortiz Sergio, Dali-Yahia Kamel, Vasquez-Ocmin Pedro, Grougnet Raphaël, Grellier Philippe, Michel Sylvie, Maciuk Alexandre, Boutefnouchet Sabrina
Laboratoire de Pharmacognosie, UMR CNRS 8638 COMETE, Faculté de Pharmacie de Paris, Université Paris-Descartes, Sorbonne Paris Cité, 4, av. de l'Observatoire, 75006 Paris, France.
Département de Pharmacie, Faculté de Médecine, Université de Tlemcen, 13000 Tlemcen, Algérie.
Fitoterapia. 2017 Apr;118:1-5. doi: 10.1016/j.fitote.2017.01.012. Epub 2017 Feb 3.
A heme-binding assay based on mass spectrometry was performed on P. monodiana Maire (Asteraceae) extracts to identify metabolites able to form adducts with heminic part of haemoglobin, as potential antimalarial drugs. Main adducts were characterized and their stability was measured. Isolation of main constituents of P. monodiana Maire lead to identification of the two methoxyflavones 3'-O-methyleupatorin (7) and artemetin (8) involved in the adducts formation. Four seco-tanapartholides (1-4), a guaianolide (5), a germacranolide (6) and two other methoxyflavones (9, 10) were also characterized. Evaluation of isolated compounds on P. falciparum and T. brucei brucei showed a moderate antiprotozoal activity of the two methoxyflavones.
对单花佩兰(菊科)提取物进行了基于质谱的血红素结合测定,以鉴定能够与血红蛋白的血红素部分形成加合物的代谢物,作为潜在的抗疟药物。对主要加合物进行了表征并测定了它们的稳定性。对单花佩兰主要成分的分离导致鉴定出参与加合物形成的两种甲氧基黄酮3'-O-甲基泽兰素(7)和青蒿亭(8)。还对四种断-艾里莫芬内酯(1-4)、一种愈创木烷型倍半萜内酯(5)、一种吉马烷型倍半萜内酯(6)以及另外两种甲氧基黄酮(9,10)进行了表征。对分离出的化合物针对恶性疟原虫和布氏布氏锥虫的评估显示,这两种甲氧基黄酮具有中等程度的抗原虫活性。