Eskitis Institute, Griffith University, Brisbane, QLD 4111, Australia.
Bioorg Med Chem Lett. 2011 Jan 15;21(2):846-8. doi: 10.1016/j.bmcl.2010.11.081. Epub 2010 Nov 21.
Mass-directed isolation of the CH(2)Cl(2)/CH(3)OH extract from a marine sponge of the genus Pseudoceratina resulted in the purification of a new antimalarial bromotyrosine alkaloid, psammaplysin H (1), along with the previously isolated analogs psammaplysins G (2) and F (3). The structure of 1 was elucidated following 1D and 2D NMR, and MS data analysis. All compounds were tested in vitro against the 3D7 line of Plasmodium falciparum and mammalian cell lines (HEK293 and HepG2), with 1 having the most potent (IC(50) 0.41μM) and selective (>97-fold) antimalarial activity.
从属于 Pseudoceratina 属的一种海洋海绵的 CH(2)Cl(2)/CH(3)OH 提取物经定向分离,得到了一种新的抗疟溴代酪氨酸生物碱 psammaplysin H(1),同时还分离得到了先前分离得到的类似物 psammaplysins G(2)和 F(3)。通过 1D 和 2D NMR 以及 MS 数据分析阐明了 1 的结构。所有化合物均在体外针对 3D7 株疟原虫和哺乳动物细胞系(HEK293 和 HepG2)进行了测试,其中 1 的抗疟活性最强(IC(50)为 0.41μM)且选择性最高(>97 倍)。