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氮杂蒽醌抑制刚果锥虫细长型血流形式的呼吸及体外生长。

Azaanthraquinone inhibits respiration and in vitro growth of long slender bloodstream forms of Trypanosoma congolense.

作者信息

Nok Andrew Jonathan

机构信息

Department of Biochemistry, Ahmadu Bello University, Zaria, Nigeria.

出版信息

Cell Biochem Funct. 2002 Sep;20(3):205-12. doi: 10.1002/cbf.948.

Abstract

An ethanolic extract of Mitracarpus scaber was found to possess in vitro and in vivo trypanocidal activity against Trypanosoma congolense. At a dosage of 50 mg kg(-1) day(-1) in normal saline for 5 days, the extract cured Balbc mice infected with T. congolense without any relapse. The isolated active component benz(g)isoquinoline 5,10 dione (Azaanthraquinone) (AQ) purified from the extract was found to inhibit glucose-dependent cellular respiration and glycerol-3-phosphate-dependent mitochondrial O(2) assimilation of the long bloodstream forms of Trypanosoma congolense. On account of the pattern of inhibition, the target could be the mitochondrial electron transport system composed of glyceraldehyde 3-phosphate dehydrogenase (G3PDH). The azaanthraquinone specifically inhibited the reduced coenzyme Q(1)-dependent O(2) uptake of the mitochondria with respect to ubiquinone. The susceptible site could be due to ubiquinone redox system which links the two enzyme activities.

摘要

已发现糙叶米特草的乙醇提取物对刚果锥虫具有体外和体内杀锥虫活性。在以50 mg kg⁻¹ 天⁻¹ 的剂量溶于生理盐水给药5天的情况下,该提取物治愈了感染刚果锥虫的Balbc小鼠,且无任何复发。从提取物中纯化得到的分离活性成分苯并(g)异喹啉5,10 - 二酮(氮杂蒽醌)(AQ)被发现可抑制刚果锥虫长血流形式的葡萄糖依赖性细胞呼吸和甘油-3-磷酸依赖性线粒体O₂ 同化作用。基于抑制模式,靶点可能是由甘油醛-3-磷酸脱氢酶(G3PDH)组成的线粒体电子传递系统。氮杂蒽醌相对于泛醌特异性抑制线粒体中依赖于还原型辅酶Q₁ 的O₂ 摄取。易感位点可能归因于连接两种酶活性的泛醌氧化还原系统。

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