Abstract: To discover inhibitors of enoylpyruvate transferase with antibacterial activity a batch of 2490 extract or fraction samples from plants and animals belonging to 169 families, 560 genera and 916 species were tested on enoylpyruvate transferase bioassay in 96-well microtiterplates. Finally 309 samples, which belong to 80 families, 169 genera and 218 species, showed inhibitory activity at 96.15ug/ml, in which 14 samples showed IC50 at=<10.00ug/ml, 40 samples showed IC50 at 10.01-30.00ug/ml, 83 samples showed IC50 at 30.01-50.00ug/ml and 172 samples showed IC50 at 50.01-96.15ug/ml. It is indicated that this in-vitro bioassay is convenient, stable, rapid, sensitive and effective in searching for antibacterial activity samples from natural sources.

Key words: Antibacterial activity screening

摘要： 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169个科、560个属、916种动植物2490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96.15μg/ml浓度下发现了来源于80个科、169个属、218个种的309个样品有活性，其中14个样品的IC50小于10.00μg/ml，40个样品的IC50在10.01～30.00μg/ml范围，83个样品的IC50在30.01～50.00μg/ml范围，172个样品的IC50在50.01～96.15?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。

关键词: 抗细菌活性筛选, 烯醇式丙酮酸转移酶, 天然产物, 提取物, 分离部位