van Baren Catalina, Anao Ivie, Leo Di Lira Paola, Debenedetti Silvia, Houghton Peter, Croft Simon, Martino Virginia
Cátedra de Farmacognosia, Instituto de Química y Metabolismo del Fármaco IQUIMEFA (UBA-CONICET), Facultad de Farmacia y Bioquímica, Universidad de Buenos Aires, República Argentina.
Z Naturforsch C J Biosci. 2006 Mar-Apr;61(3-4):189-92. doi: 10.1515/znc-2006-3-406.
Bioassay-guided fractionation of a Satureja parvifolia MeOH extract led to the isolation of eriodictyol, luteolin and ursolic and oleanolic acids as its active components against Plasmodium falciparum K1. This is the first time these compounds are reported as constituents of S. parvifolia. Ursolic acid showed an IC50 of 4.9 microg/ml, luteolin 6.4 microg/ml, oleanolic acid 9.3 microg/ml and eriodictyol 17.2 microg/ml. Antiplasmodial activity of eriodictyol and luteolin is reported here for the first time. Besides, the four compounds showed activity against P. falciparum 3D7 strain and Trypanosoma brucei rhodesiense. Eriodictyol showed moderate activity on all the parasites but was the most selective compound as a result of its rather low cytotoxicity (IC50 174.2 microg/ml) on the mammalian KB cell line.
对矮小香薷甲醇提取物进行生物测定导向的分级分离,得到了圣草酚、木犀草素、熊果酸和齐墩果酸,它们是该提取物抗恶性疟原虫K1的活性成分。这是首次报道这些化合物为矮小香薷的成分。熊果酸的半数抑制浓度(IC50)为4.9微克/毫升,木犀草素为6.4微克/毫升,齐墩果酸为9.3微克/毫升,圣草酚为17.2微克/毫升。本文首次报道了圣草酚和木犀草素的抗疟活性。此外,这四种化合物对恶性疟原虫3D7株和布氏罗得西亚锥虫均有活性。圣草酚对所有寄生虫均表现出中等活性,但由于其对哺乳动物KB细胞系的细胞毒性相当低(IC50为174.2微克/毫升),所以它是最具选择性的化合物。