Buchanan Malcolm S, Davis Rohan A, Duffy Sandra, Avery Vicky M, Quinn Ronald J
Eskitis Institute, Griffith University, Nathan, Queensland 4111, Australia.
J Nat Prod. 2009 Aug;72(8):1541-3. doi: 10.1021/np9002564.
Mass-directed isolation of the CH(2)Cl(2)/MeOH extract of Doryphora sassafras resulted in the purification of a new benzylisoquinoline alkaloid, 1-(4-hydroxybenzyl)-6,7-methylenedioxy-2-methylisoquinolinium trifluoroacetate (1), and the known aporphine alkaloid (S)-isocorydine (2). The structures of 1 and 2 were determined by 1D and 2D NMR and MS data analyses. The compounds were isolated during a drug discovery program aimed at identifying new antimalarial leads from a prefractionated natural product library. When tested against two different strains of the parasite Plasmodium falciparum (3D7 and Dd2), 1 displayed IC(50) values of 3.0 and 4.4 microM, respectively. Compound 1 was tested for cytotoxicity toward a human embryonic kidney cell line (HEK293) and displayed no activity at 120 microM.
对澳洲番荔枝的二氯甲烷/甲醇提取物进行大量定向分离，得到了一种新的苄基异喹啉生物碱，即1-(4-羟基苄基)-6,7-亚甲二氧基-2-甲基异喹啉三氟乙酸盐(1)，以及已知的阿朴啡生物碱(S)-异紫堇定(2)。通过一维和二维核磁共振以及质谱数据分析确定了1和2的结构。这些化合物是在一个药物发现项目中分离得到的，该项目旨在从预分级的天然产物库中鉴定新的抗疟先导化合物。当针对两种不同的恶性疟原虫菌株(3D7和Dd2)进行测试时，1的半数抑制浓度(IC50)值分别为3.0和4.4微摩尔。对化合物1针对人胚肾细胞系(HEK293)进行细胞毒性测试，在120微摩尔浓度下未显示活性。
