Coplan P M, Nolan L L
School of Public Health, University of Massachusetts, Amherst 01003.
Drug Chem Toxicol. 1991;14(3):257-64. doi: 10.3109/01480549109002188.
Eleven medications used in the treatment of the human immunodeficiency virus or subsequent opportunistic infections were tested to determine their toxicity to the growth of the CEM line of transformed CD4+ T-cells. A selectivity ratio (IC50/EC50) for each agent against its target pathogen was calculated as an in vitro indication of the therapeutic value of that agent. Among the anti-HIV agents tested in this study, 2',3'-dideoxyinosine (ddI) had the highest in vitro selectivity ratio, 2.5 times higher than that of 3'-azido-3'-deoxythymidine (AZT). Dapsone had the highest selectivity ratio of the four agents used in the treatment of Pneumocystis carinii pneumonia that were tested. Ketoconazole had a very low selectivity ratio for Candida spp. due to its very high toxicity to CD4+T-cells.
对用于治疗人类免疫缺陷病毒或后续机会性感染的11种药物进行了测试,以确定它们对转化的CD4+T细胞CEM系生长的毒性。计算每种药物针对其目标病原体的选择性比率(IC50/EC50),作为该药物治疗价值的体外指标。在本研究中测试的抗HIV药物中,2',3'-双脱氧肌苷(ddI)具有最高的体外选择性比率,比3'-叠氮-3'-脱氧胸苷(AZT)高2.5倍。在测试的用于治疗卡氏肺孢子虫肺炎的四种药物中,氨苯砜具有最高的选择性比率。酮康唑对念珠菌属的选择性比率非常低,因为它对CD4+T细胞毒性非常高。