Cimanga K, De Bruyne T, Pieters L, Vlietinck A J, Turger C A
Department of Pharmaceutical Sciences, University of Antwerp (U.I.A.), Belgium.
J Nat Prod. 1997 Jul;60(7):688-91. doi: 10.1021/np9605246.
Three different extracts and four alkaloids from the root bark of Cryptolepis sanguinolenta have been assessed in vitro against Plasmodium falciparum D-6 (chloroquine-sensitive strain), K-1, and W-2 (chloroquine-resistant strains). Cryptolepine (1) and its hydrochloride (2), 11-hydroxycryptolepine (3), and neocryptolepine (5) showed a strong antiplasmodial activity against P. falciparum chloroquine-resistant strains. Quindoline (4) was less active. The highest activity was obtained with compound 1. In vivo tests on infected mice showed that cryptolepine (1), when tested as its hydrochloride (2), exhibited a significant chemosuppressive effect against Plasmodium berghei yoelii and Plasmodium berghei, berghei, while 1 had the same effect against P. berghei yoelii only. Compounds 3 and 4 did not show activity in this in vivo test system.
对红根草（Cryptolepis sanguinolenta）根皮中的三种不同提取物和四种生物碱进行了体外抗恶性疟原虫D-6（氯喹敏感株）、K-1和W-2（氯喹耐药株）的评估。隐喹啉（1）及其盐酸盐（2）、11-羟基隐喹啉（3）和新隐喹啉（5）对恶性疟原虫氯喹耐药株表现出较强的抗疟活性。喹多啉（4）活性较低。化合物1的活性最高。对感染小鼠的体内试验表明，隐喹啉（1）以其盐酸盐（2）形式测试时，对约氏疟原虫伯氏疟原虫和伯氏疟原虫表现出显著的化学抑制作用，而1仅对约氏疟原虫有相同作用。化合物3和4在该体内试验系统中未表现出活性。
