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目的是以烯醇式丙酮酸转移酶 (EPT)为靶点筛选其抑制剂 ,以期寻找抗细菌活性样品。实验是在 96孔酶标板上对来源于 16 9个科、 5 6 0个属、 916种动植物 2 4 90个提取物或分离部位样品在EPT模型上进行了批量筛选。结果表明在 96 15 μg/ml浓度下发现了来源于 80个科、 16 9个属、 2 18个种的 30 9个样品有活性 ,其中 14个样品的IC50 小于 10 0 0 μg/ml,4 0个样品的IC50 在 10 0 1～ 30 0 0 μg/ml范围 ,83个样品的IC50 在 30 0 1～ 5 0 0 0 μg/ml范围 ,172个样品的IC50 在 5 0 0 1～ 96 15 μg/ml范围。通过以上工作我们认为以烯醇式丙酮酸转移酶为分子靶点的体外筛选方法稳定、方便、快速、微量、有效 ,特别适用于天然产物的抗细菌活性筛选
The purpose was to screen inhibitors with enolpyruvate transferase (EPT) as a target to search for antibacterial activity samples. The experiment was conducted on a 96-well microtiter plate for mass screening of samples from 16 families, 560 genus, 916 plant and animal 24, 90 extracts or isolates on the EPT model. The results showed that 30 9 samples derived from 80 families, 16 9 genera, and 2 18 species were found to be active at the concentration of 96 15 μg/ml, and IC50 of 14 samples was less than 100 μg/ml, 4 The IC50 of 0 samples ranged from 1 0 to 1 0 0 μg/ml, the IC50 of 83 samples ranged from 301 to 500 μg/ml, and the IC50 of 172 samples ranged from 500 to 9615. Μg/ml range. Through the above work, we believe that the in vitro screening method using enolpyruvate transferase as a molecular target is stable, convenient, rapid, trace, and effective, and is particularly suitable for the screening of antibacterial activity of natural products.