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青蒿琥酯及四种经典抗疟药对大鼠肝线粒体亚铁螯合酶活性的影响
引用本文:姚朗 石笑春. 青蒿琥酯及四种经典抗疟药对大鼠肝线粒体亚铁螯合酶活性的影响[J]. 中国药理学与毒理学杂志, 1996, 10(3): 239-240
作者姓名:姚朗 石笑春
作者单位:广州军区后勤部药物研究所
摘    要:

关 键 词:青蒿琥酯  抗疟药  亚铁螯合酶  线粒体  血红素
收稿时间:1995-06-09

Effects of artesunate and four classical antimalarials on mitochondrial ferrochelatase activity in isolated rat liver
YAO Lang, SHI Xiao-Chun, TENG Xi-He, XIONG Chun-Sheng. Effects of artesunate and four classical antimalarials on mitochondrial ferrochelatase activity in isolated rat liver[J]. Chinese Journal of Pharmacology and Toxicology, 1996, 10(3): 239-240
Authors:YAO Lang   SHI Xiao-Chun   TENG Xi-He   XIONG Chun-Sheng
Affiliation:(Institute of Microbiology and Epidemiology, Academy of Military Medical Sciences, Beijing 100071)
Abstract:The effects of artesunate(Art) and four classical antimalarials on the mitochondrial ferrochelatase(FC) activity in isolated rat liver were studied with pyridine hemochromogen method. It was shown that Art markedly inhibited the FC activity whether ferrous or ferric ion was used as substrate, but the heme biosynthesis from ferric ion was more susceptible to Art. The IC50 of Art on FC was 165 μmol·L-1 for Fe2+ and 30.2 μmol·L-1 for Fe3+ substrate, respectively. It meant that Art not only inhibited the FC activity directly, but also interfered with Fe3+ reduction and/or utilization by mitochondria. So that Art could produce stronger inhibitory effect on heme biosynthesis, and the effect might be one of the toxic mechanisms of Art on erythropoiesis. The inhibition of FC activity was not found with 1 mmol·L-1 chlo- roquine, quinine, cyclochloroguanide or primaquine treatment.
Keywords:artesunate  antimalarials  ferrochelatase  mitochondria  heme
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