Ramos H, Brajtburg J, Marquez V, Cohen B E
Centre for Cell Biology, Faculty of Sciences, Central University of Venezuela, Caracas.
Drugs Exp Clin Res. 1995;21(6):211-6.
We compared leishmanicidal activity of five formulations of amphotericin B (AmB). AmB used as Fungizone immediately caused cell lysis, at lower concentrations partial, and at higher concentrations total; the non-lysed cells reassuming growth. AmB formulated with egg-lecithin and bile salt at doses equivalent to those of Fungizone was not active, whereas at higher doses it resulted in a delayed but complete inhibition of cell growth. The activity of liposomal AmB was comparable to that of Fungizone. The time of initial leishmanicidal activity of the five formulations tested can be ascribed to the rate of free, monomeric AmB delivered. Features that are characteristic of the anticellular effect of AmB formulated with egg lecithin and bile salts, a delay in activity, a requirement for higher concentration and total inhibition of cell growth, were also noted.
我们比较了五种两性霉素B（AmB）制剂的杀利什曼原虫活性。用作Fungizone的AmB立即引起细胞裂解，较低浓度时部分裂解，较高浓度时完全裂解；未裂解的细胞恢复生长。与Fungizone剂量相当的用卵磷脂和胆盐配制的AmB无活性，而较高剂量时会导致细胞生长延迟但完全抑制。脂质体AmB的活性与Fungizone相当。所测试的五种制剂的初始杀利什曼原虫活性时间可归因于游离单体AmB的释放速率。用卵磷脂和胆盐配制的AmB的抗细胞效应所具有的特征，即活性延迟、需要更高浓度以及对细胞生长的完全抑制，也被观察到。
