Abstract:Objective To optimizehigh throughput screening model of ascaris suum NADH-fumarate reductase and mammal NADH oxidase, and to evaluate the activity and the selectivity of wortmannilactone F using the two models.
Method Ascaris suum and pig heart mitochondria were extracted, and then the parameters of the model, such as, temperature, pH, NADH concentration, mitochondrial concentration were optimized. The inhibititory activities of wortmannilactone F against ascaris suum NADH-fumarate reductase and pig heart NADH oxidase were also investigated under these optimum conditions.
Results These optimum conditions in ascaris suum NADH-fumarate reductase, such as, reaction temperature, pH, the NADH and mitochondrial concentration were 37 ℃, pH 6.5, 0.180 mmol/L and 0.025 g/L, respectively. The IC50 of wortmannilactone F against ascaris suum NADH-fumarate reductase was 5.0 nmol/L, while the IC50 against pig heart NADH oxidase was over 6.2 mmol/L.
Conclusion Wortmannilactone F shows selective inhibitory effect against ascaris suum NADH-fumarate reductase with IC50 at nmol level and could be expected as a potential anti-helmintic compound.
李原, 刘文财, 孙文龙, 董悦生, 阎浩林. 蠕虫NADH-延胡索酸还原酶模型优化及沃特曼内酯F的活性评价[J]. 《中国医药生物技术》杂志, 2012, 7(4): 276-280.
LI Yuan, LIU Wen-Cai, SUN Wen-Long, DONG Yue-Sheng, YAN Hao-Lin. The optimization of helminth NADH-fumarate reductase model and the activity evaluation of wortmannilactone F. , 2012, 7(4): 276-280.