【摘要】 目的检测棉子酚、吡喹酮、蒿甲醚对重组日本血吸虫乳酸脱氢酶(rSjLDH)活性的影响。方法在已建立的rSjLDH标准酶活性测定体系中分别加入不同浓度的棉子酚(0～0.10mmol/L)、吡喹酮(0～0.20mmol/L)及蒿甲醚(0～0.10mmol/L),以相应药物溶剂作对照,分光光度法测定药物对rSjLDH活性的影响。用SPSS13.0软件统计结果,计算药物对酶活性的相对抑制率。结果与对照组比较,0.04mmol/L棉子酚对rSjLDH催化丙酮酸还原为乳酸及乳酸氧化为丙酮酸的相对抑制率分别为59.1%和34.4%(P<0.01),0.10mmol/L棉子酚分别为91.3%和89.1%(P<0.01);0.06mmol/L吡喹酮分别为5.77%和41.4%(P<0.05),0.20mmol/L吡喹酮分别为83.8%和72.2%(P<0.01)。0.10mmol/L蒿甲醚对rSjLDH则无抑制作用(P>0.05)。结论棉子酚及吡喹酮对rSjLDH活性均有显著的抑制作用,SjLDH可能是吡喹酮的分子靶标之一。更多还原

【Abstract】 Objective To detect the effect of gossypol,praziquantel and artemether on activity of the recombinant lactate dehydrogenase of Schistosoma japonicum(rSjLDH).Methods Effect of gossypol(0-0.10 mmol/L),praziquantel(0-0.20 mmol/L)and artemether(0-0.10 mmol/L)on the enzymatic activity of rSjLDH was detected by spectrophotometric method in standard reaction system established before,same solvent of each reagent was used as control.Results were analyzed by SPSS13.0 software.Results Compared with the control,considerable inhibition for both reduction and ox-idation reactions catalyzed by rSjLDH was observed at 0.04 mmol/L of gossypol(P<0.01).The enzyme activities of rSjLDH for reduction and oxidation reactions were inhibited by 91.3% and 89.1% respectively at 0.1 mmol/L of gossypol,com-pared with the control(P<0.01).To praziquantel,enzymatic activity inhibition was observed at 0.02 mmol/L for oxidation reaction and at 0.06 mmol/L for reduction reaction(P<0.05).At 0.2 mmol/L of praziquantel,enzymatic activities were inhibited by 83.8% for reduction reaction and 72.2% for oxidation reaction respectively,than that of the control(P<0.01).No inhibition for both reduction and oxidation reactions was observed at 0.1 mmol/L of artemether,compared with that of the control(P>0.05).Conclusion Gossypol and praziquantel show a high inhibition on rSjLDH.SjLDH may be one of the molecular targets of praziquantel.更多还原