自由基调节青蒿素类药物的抗血吸虫作用.PDF

2003 3 3 　CHINA TROPICAL MEDICINE Vol.3 No.3 May 2003 　　　　　　　　　　　　　　　　　　　　　　3　9 1　 [] 1 2 翟自立 　王振果 1 2 Free radicals medi ate the schistosomicidal activity of artemi sinin-based drugs.ZHAI Zi-li , Wang Zhenguo .1 Institute of Parasitic Diseases, Chinese Center for Disease Control and Prevention, Shanghai 200025, P.R.China, 2 Shanghai Center for Dis- ease Control and Prevention, Shanghai 200336, P.R.China. Summary　Artemisinin-typed endopero ides are a promising novel class of antischistosomal agents.Their antischistosomal ac- tivity is associated with high levels of intraceca to ic heme, which catalyzes the cleavage of the endopero ide bridge to generate free radicals followed by such membrane damages as lipid pero idation and protein denaturation.The interaction of the endopero ides with heme also enhances heme-induced membrane to icity by way of stimulating the redo activity of heme and preventing its polymeriza- tion to chemically inert pigment.Moreover, the drug-derivative radicals may disturb the parasites proo idant-antio idant balance, thereby sensitizing them to subsequent lethal damages of endogenous and e ogenous o idants increase.The free radicals-mediated mode of action of the endopero ides may be used to e plain such phenomena as se difference and developmental stage difference in susceptibility to the endopero ides as well as their slow schistosome killing. Key words　Artemisinin-typed compounds, Free radicals, Heme, Schistosome, Membrane damage, Antio idant system. + 中图分类号:R383.2 4　　文献标识码:B　　文章编号:1009-9727(2003)03-0391-04 　　, , , ,