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):53-9. doi: 10.1007/s00508-007-0870-8.
The blood schizontocidal activity of monodesbutyl-benflumetol (DBB), retinol (RET) and combinations (DBB-RET) at retinol concentrations corresponding to the 50th, 65th and 80th percentile of physiological retinol concentrations in healthy adults has been investigated in Plasmodium falciparum. Parallel in vitro tests with DBB, RET and the 3 DBB-RET combinations were carried out with 26 fresh parasite isolates from northwestern Thailand, following the WHO standard protocol Mark II for determining the inhibition of schizont maturation. The EC(50) values for DBB, RET and for DBB in DBB-RET low, medium and high were 5.72 nM, 561.83 nM, 1.68 nM, 0.60 nM and 0.07 nM, respectively, the EC(90) values 44.14 nM, 9338.60 nM, 49.00 nM, 28.48 nM and 8.94 nM. The geometric mean cut-off concentrations of schizont maturation for DBB alone and for DBB in DBB-RET low, medium and high were 153.20 nM, 62.93nM, 34.00 nM and 13.74 nM, respectively, indicating significant synergistic interaction between DBB and retinol. The degree of synergism increases with the retinol concentration in the combination and is highest at the EC(99) level for DBB.
已在恶性疟原虫中研究了单去丁基苯氟隆（DBB）、视黄醇（RET）及其组合（DBB-RET）在对应于健康成年人生理视黄醇浓度第 50、65 和 80 百分位数的血裂殖体杀伤活性。采用 26 株来自泰国西北部的新鲜寄生虫分离株，根据世界卫生组织确定裂殖体成熟抑制的标准协议 Mark II 进行了平行的 DBB、RET 和 3 种 DBB-RET 组合的体外试验。DBB、RET 和 DBB-RET 低、中、高的 EC（50）值分别为 5.72 nM、561.83 nM、1.68 nM、0.60 nM 和 0.07 nM，EC（90）值分别为 44.14 nM、9338.60 nM、49.00 nM、28.48 nM 和 8.94 nM。DBB 单独和 DBB-RET 低、中、高的裂殖体成熟几何平均截止浓度分别为 153.20 nM、62.93 nM、34.00 nM 和 13.74 nM，表明 DBB 和视黄醇之间存在显著的协同相互作用。协同作用的程度随组合中视黄醇浓度的增加而增加，在 DBB 的 EC（99）水平最高。
