del Rayo Camacho Maria, Phillipson J David, Croft Simon L, Rock Peter, Marshall Sarah J, Schiff Paul L
Centre for Pharmacognosy and Phytotherapy, The School of Pharmacy, University of London, 29-39 Brunswick Square, London WC 1N 1AX, UK.
Phytother Res. 2002 Aug;16(5):432-6. doi: 10.1002/ptr.929.
In the search for antiprotozoal compounds from natural sources, Triclisia patens displayed activity against L. donovani promastigotes (IC(50) = 1.5 microg/mL) and T. b. brucei blood stream trypomastigote forms (IC(50) = 31.25 microg/mL). In addition, a total of 20 bisbenzylisoquinoline alkaloids were screened for antileishmanial and antitrypanosomal activity in vitro. Fangchinoline (IC(50) = 0.39 microM) was found to be as active as the standard pentamidine against Leishmania donovani promastigotes. Phaeanthine was three-fold more active (IC(50) = 2.41 microM; 1.5 microg/mL) than the standard drug Pentostam against L. donovani amastigotes, but at this concentration was toxic to murine macrophages. In contrast, cocsoline (IC(50) = 12.3 microM; 6.76 microg/mL) was as active as Pentostam, and was not toxic to macrophages at this concentration. Thalisopidine showed the strongest activity (IC(50) = 1.14 microM) against Trypanosoma brucei brucei blood stream form trypomastigotes, but was less active than pentamidine.
在从天然来源寻找抗原生动物化合物的过程中，三叶崖爬藤对杜氏利什曼原虫前鞭毛体（IC(50)=1.5微克/毫升）和布氏锥虫血流型锥鞭毛体（IC(50)=31.25微克/毫升）显示出活性。此外，总共筛选了20种双苄基异喹啉生物碱的体外抗利什曼原虫和抗锥虫活性。发现粉防己碱（IC(50)=0.39微摩尔）对杜氏利什曼原虫前鞭毛体的活性与标准药物喷他脒相当。樟柳碱对杜氏利什曼原虫无鞭毛体的活性比标准药物喷他脒高三倍（IC(50)=2.41微摩尔；1.5微克/毫升），但在此浓度下对小鼠巨噬细胞有毒性。相比之下，考克索林（IC(50)=12.3微摩尔；6.76微克/毫升）的活性与喷他脒相当，且在此浓度下对巨噬细胞无毒。thalisopidine对布氏锥虫血流型锥鞭毛体显示出最强的活性（IC(50)=1.14微摩尔），但活性低于喷他脒。
