Marley S E, Eberhard M L, Steurer F J, Ellis W L, McGreevy P B, Ruebush T K
Division of Parasitic Diseases, Centers for Disease Control and prevention, Department of Health and Human Services, Atlanta, Georgia 30341, USA.
Antimicrob Agents Chemother. 1997 Jan;41(1):91-4. doi: 10.1128/AAC.41.1.91.
The presently used therapy for Babesia microti infections, a combination of quinine and clindamycin, does not always result in parasitologic cures. To identify possible alternative chemotherapeutic agents for such infections, we screened, in the hamster-B. microti system, 12 antiprotozoal drugs that have either recently been released for human use or were in experimental stages of development at the Walter Reed Army Institute of Research for the treatment of malaria and leishmaniasis. Several well-recognized antimalarial drugs, such as mefloquine, halofantrine, artesunate, and artelenic acid, exhibited little or no effect on parasitemia. Two 8-aminoquinolines, WR006026 [8-(6-diethylaminohexylamino)-6-methoxy-4-methylquinoline dihydrochloride] and WR238605 [8-[(4-amino-1-methylbutyl)amino]-2,6-dimethoxy-4-methyl-5 -(3-trifluoromethylphenoxy-7) quinoline succinate], produced clearance of patent parasitemia. Furthermore, blood from infected hamsters treated with WR238605 via an intramuscular injection failed to infect naive hamsters on subpassage, thus producing a parasitologic cure. These two compounds merit further screening in other systems and may prove useful in treating human babesiosis.
目前用于治疗微小巴贝斯虫感染的疗法，即奎宁和克林霉素联合使用，并不总能实现寄生虫学治愈。为了确定针对此类感染可能的替代化疗药物，我们在仓鼠 - 微小巴贝斯虫系统中筛选了12种抗原生动物药物，这些药物要么最近已获批用于人类，要么正处于沃尔特·里德陆军研究所治疗疟疾和利什曼病的实验开发阶段。几种公认的抗疟药物，如甲氟喹、卤泛群、青蒿琥酯和蒿甲醚，对寄生虫血症几乎没有影响。两种8 - 氨基喹啉，WR006026 [8 - (6 - 二乙氨基己基氨基)-6 - 甲氧基 - 4 - 甲基喹啉二盐酸盐] 和WR238605 [8 - [(4 - 氨基 - 1 - 甲基丁基)氨基]-2,6 - 二甲氧基 - 4 - 甲基 - 5 - (3 - 三氟甲基苯氧基 - 7)喹啉琥珀酸盐]，使显性寄生虫血症得以清除。此外，经肌肉注射WR238605治疗的感染仓鼠的血液在传代时未能感染未感染的仓鼠，从而实现了寄生虫学治愈。这两种化合物值得在其他系统中进一步筛选，可能对治疗人类巴贝斯虫病有用。
