Dvorak J A, Howe C L
Am J Trop Med Hyg. 1977 Jan;26(1):58-63. doi: 10.4269/ajtmh.1977.26.58.
The effects of 3-methyl-4-(5'-nitrofurfurylidene-amino)-tetrahydro-4H-1,4-thiazine-1,1-dioxide [Lampit, Bayer 2502] on the intracellular cycle of Trypanosoma cruzi were studied with an in vitro steady-state culture system that permitted the continuous analysis of individual host cell-parasite interactions. Lampit concentrations of 10(-4) and 10(-5) M significantly affected the ability of trypomastigotes to penetrate vertebrate cells. Lampit concentrations above 10(-4) M were toxic to the host cell population and Lampit concentrations below 10(-5) M did not affect the ability of trypomastigotes to penetrate vertebrate cells. Lampit concentrations of 10(-5) M or greater completely inhibited the intracellular cycle of T. cruzi whereas Lampit concentrations of 10(-7) M or less had no effect on the intracellular cycle. Continuous perfusion with 10(-6) M Lampit resulted in a linear increase in intracellular parasite reproduction time. A stable strain of T. cruzi was produced in vitro that was resistant to a 100-fold greater concentration of Lampit that the parent strain.
利用体外稳态培养系统研究了3-甲基-4-(5'-硝基糠叉氨基)-四氢-4H-1,4-噻嗪-1,1-二氧化物[拉米呋啶,拜耳2502]对克氏锥虫细胞内周期的影响,该系统可对单个宿主细胞与寄生虫的相互作用进行连续分析。10(-4)和10(-5)M的拉米呋啶浓度显著影响锥鞭毛体穿透脊椎动物细胞的能力。高于10(-4)M的拉米呋啶浓度对宿主细胞群体有毒性,而低于10(-5)M的拉米呋啶浓度不影响锥鞭毛体穿透脊椎动物细胞的能力。10(-5)M或更高浓度的拉米呋啶完全抑制克氏锥虫的细胞内周期,而10(-7)M或更低浓度的拉米呋啶对细胞内周期没有影响。用10(-6)M拉米呋啶连续灌注导致细胞内寄生虫繁殖时间呈线性增加。在体外产生了一种稳定的克氏锥虫菌株,其对拉米呋啶的耐受浓度比亲本菌株高100倍。