Stermitz Frank R, Scriven Lacey N, Tegos George, Lewis Kim
Department of Chemistry, Colorado State University, Fort Collins, Colorado, USA.
Planta Med. 2002 Dec;68(12):1140-1. doi: 10.1055/s-2002-36347.
Bioassay-guided fractionation of an extract of Artemisia annua L. (Asteraceae) was conducted in order to assess the possible presence in the plant material of inhibitors of bacterial multidrug resistance pumps. Fractions were tested for Staphylococcus aureus growth inhibition in the presence of a subinhibitory dose of the weak antibacterial alkaloid berberine. Active fractions yielded the flavones chrysosplenol-D and chrysoplenetin, which themselves had very weak growth inhibitory action, but which made a potent combination with berberine. In comparison with work on other flavonols, it is likely that potentiation is due to the inhibition of an S. aureus multidrug resistance (MDR) pump. These same two flavonols were earlier reported to potentiate the activity of artemisinin against Plasmodium falciparum.
为了评估黄花蒿(菊科)提取物中是否可能存在细菌多药耐药泵抑制剂,进行了生物测定引导的分级分离。在存在亚抑制剂量的弱抗菌生物碱黄连素的情况下,测试各馏分对金黄色葡萄球菌生长的抑制作用。活性馏分产生了黄酮类化合物金缕梅醇-D和金缕梅黄素,它们本身具有非常弱的生长抑制作用,但与黄连素形成了有效的组合。与其他黄酮醇的研究相比,增强作用可能是由于抑制了金黄色葡萄球菌的多药耐药(MDR)泵。此前有报道称,这两种黄酮醇可增强青蒿素对恶性疟原虫的活性。