Yang D M, Liew F Y
Wellcome Research Laboratories, Beckenham, Kent, U.K.
Parasitology. 1993 Jan;106 ( Pt 1):7-11. doi: 10.1017/s0031182000074758.
We have investigated the effect of qinghaosu (QHS, artemisinin) and its derivatives on Leishmania major replication in vitro and on the disease development in mice infected with L. major. Artemisinin is effective against promastigotes in vitro, with an ED50 (50% effective dose) at 7.5 x 10(-7) M. Both artemisinin and artemether are leishmanicidal for amastigotes in infected murine macrophages in vitro, with ED50 at 3 x 10(-5) M and 3 x 10(-6) M respectively. These compounds have no effect on the viability of macrophages or on the phytohaemaglutinin-induced proliferation of normal spleen cells, even at 10(-4) M. BALB/c mice infected in the footpad with L. major developed significantly smaller lesions and parasite loads when treated with the compounds. Intra-lesion injection of the compounds was the most effective route. The intramuscular and oral routes were also effective; however, intravenous injection with artesunate was not effective.
我们研究了青蒿素（QHS，青蒿琥酯）及其衍生物对杜氏利什曼原虫体外增殖以及对感染杜氏利什曼原虫小鼠疾病发展的影响。青蒿素在体外对前鞭毛体有效，其半数有效剂量（ED50）为7.5×10⁻⁷M。青蒿素和蒿甲醚在体外对感染小鼠巨噬细胞内的无鞭毛体均有杀利什曼原虫作用，其ED50分别为3×10⁻⁵M和3×10⁻⁶M。这些化合物即使在浓度为10⁻⁴M时，对巨噬细胞活力或对植物血凝素诱导的正常脾细胞增殖也无影响。用这些化合物治疗后，足垫感染杜氏利什曼原虫的BALB/c小鼠的病变和寄生虫负荷显著减小。病灶内注射这些化合物是最有效的给药途径。肌肉注射和口服途径也有效；然而，青蒿琥酯静脉注射无效。
