Wright C W, O'Neill M J, Phillipson J D, Warhurst D C
Department of Pharmacognosy, School of Pharmacy, University of London, United Kingdom.
Antimicrob Agents Chemother. 1988 Nov;32(11):1725-9. doi: 10.1128/AAC.32.11.1725.
A microdilution technique for the assessment of in vitro activity against Entamoeba histolytica was devised and validated with metronidazole. The test was used to detect the antiamoebic activities of plant extracts prepared from the traditional remedies Brucea javanica fruits and Simarouba amara stems. The activity was associated with quassinoid-containing fractions. The 50% inhibitory concentrations for some quassinoids against amoebae were determined by using the microdilution method. These concentrations ranged from 0.019 micrograms.ml-1 for bruceantin, the most active quassinoid, to greater than 5 micrograms.ml-1 for glaucarubol, the least active compound tested. These results are discussed with reference to the known activities of these compounds against Plasmodium falciparum. Overall, the activities of the quassinoids against both protozoa are similar. The microdilution technique will be useful in the search for novel antiamoebic drugs.
设计了一种用于评估体外抗溶组织内阿米巴活性的微量稀释技术，并用甲硝唑进行了验证。该试验用于检测从传统药物鸦胆子果实和苦木科植物茎中制备的植物提取物的抗阿米巴活性。该活性与含苦木素的组分有关。使用微量稀释法测定了一些苦木素对阿米巴的50%抑制浓度。这些浓度范围从活性最强的苦木苦素的0.019微克·毫升-1到所测试活性最低的化合物格劳卡鲁醇的大于5微克·毫升-1。参照这些化合物对恶性疟原虫的已知活性对这些结果进行了讨论。总体而言，苦木素对这两种原生动物的活性相似。微量稀释技术将有助于寻找新型抗阿米巴药物。
