Anderson M M, O'Neill M J, Phillipson J D, Warhurst D C
Department of Pharmacognosy, School of Pharmacy, University of London, U.K.
Planta Med. 1991 Feb;57(1):62-4. doi: 10.1055/s-2006-960020.
A microdilution technique was developed for the assessment of in vitro cytotoxicity against KB cells derived from a human epidermoid carcinoma of the nasopharynx. The test was used to determine the cytotoxicity of a series of quassinoids, isolated from Brucea javanica, and which have previously been shown to demonstrate activity against Plasmodium falciparum. The 50% effective dose (ED50) for 7 quassinoids tested against KB ranged from 0.008 microgram/ml for bruceantin, the most cytotoxic of the compounds tested to greater than 5 micrograms/ml for bruceolide, the least toxic tested. The activities of the quassinoids against KB did not parallel the known activities of the quassinoids against Plasmodium falciparum suggesting that the quassinoid mode of antimalarial action is not a simple cytotoxic effect and lends support to further investigation of the structure activity relationships within this group of compounds.
开发了一种微量稀释技术，用于评估对源自人鼻咽表皮样癌的KB细胞的体外细胞毒性。该试验用于确定从鸦胆子中分离出的一系列苦木素类化合物的细胞毒性，这些苦木素类化合物先前已显示出对恶性疟原虫有活性。针对KB测试的7种苦木素类化合物的50%有效剂量（ED50）范围为：细胞毒性最强的鸦胆丁为0.008微克/毫升，毒性最低的鸦胆灵大于5微克/毫升。苦木素类化合物对KB的活性与已知的对恶性疟原虫的活性不平行，这表明苦木素类化合物的抗疟作用模式不是简单的细胞毒性作用，这为进一步研究该类化合物的构效关系提供了支持。
