Ramharter Michael, Burkhardt Dominik, Nemeth Johannes, Adegnika Ayola A, Kremsner Peter G
Medical Research Unit, Albert Schweitzer Hospital, Lambaréné, Gabon.
Am J Trop Med Hyg. 2006 Oct;75(4):637-9.
Artemisinins show the potential for neurotoxicity in preclinical studies. Artemisone is a leading candidate of second-generation semi-synthetic artemisinin derivatives for antimalarial therapy devoid of neurotoxicity. Artemisone showed 3-5-fold higher in vitro activity (50% effective concentration (EC50) = 0.14 nmol/L, EC90 = 2.55 nmol/L) than artesunate against fresh Plasmodium falciparum isolates from Gabon and a high-activity correlation indicates a shared drug target.
青蒿素类药物在临床前研究中显示出神经毒性的可能性。蒿甲醚是第二代半合成青蒿素衍生物中用于抗疟疾治疗且无神经毒性的主要候选药物。与青蒿琥酯相比,蒿甲醚对来自加蓬的新鲜恶性疟原虫分离株的体外活性高3至5倍(半数有效浓度(EC50)=0.14纳摩尔/升,EC90=2.55纳摩尔/升),且高活性相关性表明存在共同的药物靶点。