Institute of Specific Prophylaxis and Tropical Medicine, Center for Physiology and Pathophysiology, Medical University of Vienna, Vienna, Austria.
Wien Klin Wochenschr. 2007;119(19-20 Suppl 3):60-6. doi: 10.1007/s00508-007-0861-9.
The blood schizontocidal activity of lumefantrine, monodesbutyl-benflumetol (DBB) and a 999:1 combination of both compounds has been investigated in 26 fresh isolates of Plasmodium falciparum from northwestern Thailand, using the WHO standard protocol Mark II for determining the inhibition of schizont maturation. The geometric mean cut-off concentrations of schizont maturation (GMCOC) were 943.2 nM for lumefantrine, 146.3 nM for DBB and 182.2 nM for the 999:1 combination of lumefantrine and DBB. The EC(50) values were 27.3 nM for lumefantrine, 5.7 nM for DBB, and 16.5 nM for the combination, and the EC(90) values 163.1 nM for lumefantrine, 44.1 nM for DBB, and 78.3 nM for the combination. Despite the very low concentration in the combination, DBB exerted significant synergistic activity with lumefantrine that was strongest at the EC(90) and EC(99) levels. Correlation analysis indicates that DBB is the leading determinant for the activity of the combination.
在泰国西北部，26 株新鲜分离的恶性疟原虫（Plasmodium falciparum）采用世界卫生组织（WHO）标准方案 II 检测了咯萘啶、单去乙基-苯芴醇（DBB）及其 999:1 联合物的血裂殖体杀伤活性。用 WHO 标准方案 II 检测咯萘啶、DBB 及其 999:1 联合物对裂殖体成熟的半数最大抑制浓度（GMCOC）分别为 943.2、146.3 和 182.2 nM；半数有效浓度（EC50）分别为 27.3、5.7 和 16.5 nM；90%有效浓度（EC90）分别为 163.1、44.1 和 78.3 nM。尽管联合物中的 DBB 浓度很低，但它与咯萘啶表现出显著的协同作用，在 EC90 和 EC99 水平上作用最强。相关分析表明，DBB 是联合物活性的主要决定因素。
