Shaohong Lu, Kumagai Takashi, Qinghua Ai, Xiaolan Yan, Ohmae Hiroshi, Yabu Yoshisada, Siwen Li, Liyong Wen, Maruyama Haruhiko, Ohta Nobuo
Institute of Parasitic Diseases, Zhejiang Academy of Medical Sciences, Hangzhou 310013, China; Department of Molecular Parasitology, Nagoya City University Graduate School of Medical Sciences, Nagoya 467-8601, Japan.
Parasitol Int. 2006 Mar;55(1):63-8. doi: 10.1016/j.parint.2005.10.001. Epub 2005 Nov 11.
The therapeutic effects of artesunate against experimental Schistosoma mansoni infection in mice were analyzed. Previous studies showed that artesunate is highly effective against S. japonicum infection, but the action of this drug against S. mansoni remained uncovered. The present study examines the optical conditions for artesunate against S. mansoni and evaluates the effects of inhibiting the sexual maturation of adult worms. Mice infected with S. mansoni were orally administered with artesunate according to different schedules. Four consecutive administrations of 300 mg/kg of artesunate at 2-week intervals conferred almost total protection without the development of pathological lesions in the liver. The significant reduction in the number of eggs produced by surviving worms and the status of egg maturation suggested that artesunate inhibits sexual maturation. Electron microscopy revealed that artesunate caused morphological damage, especially on the worm tegument. Artesunate was also very effective in iron-deficient mice. Furthermore, the efficacy of artesunate was equal to or better than that of artemether against S. japonicum infection. Considering that artemether is more toxic, artesunate is currently one of the most efficient drugs against immature S. mansoni.
分析了青蒿琥酯对小鼠实验性曼氏血吸虫感染的治疗效果。先前的研究表明，青蒿琥酯对日本血吸虫感染非常有效，但该药物对曼氏血吸虫的作用仍未明确。本研究考察了青蒿琥酯针对曼氏血吸虫的最佳条件，并评估了其对成虫性成熟的抑制作用。感染曼氏血吸虫的小鼠按照不同的给药方案口服青蒿琥酯。以2周的间隔连续4次给予300mg/kg的青蒿琥酯，几乎提供了完全的保护，且肝脏未出现病理损伤。存活虫体产卵数量的显著减少以及虫卵成熟状态表明青蒿琥酯抑制了性成熟。电子显微镜显示，青蒿琥酯造成了形态学损伤，尤其是对虫体表皮。青蒿琥酯对缺铁小鼠也非常有效。此外，青蒿琥酯对日本血吸虫感染的疗效等同于或优于蒿甲醚。鉴于蒿甲醚毒性更强，青蒿琥酯目前是针对未成熟曼氏血吸虫最有效的药物之一。
