从天然提取物或分离部位中以烯醇式丙酮酸转移酶为靶点的抗细菌活性筛选(英文)

Searching for Antibacterial Activities of Extracts and Fractions Derived from Natural Sources Targeting Enoylpyruvate Transferase

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 。

To discover inhibitors of enoylpyruvate transferase with antibacterial activity a batch of 2490 extract or fraction samples prepared 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 15?μg/ml, in which 14 samples showed IC 50 at=<10 00?μg/ml, 40 samples showed IC 50 at 10 01-30 00?μg/ml, 83 samples showed IC 50 at 30 01-50 00?μg/ml and 172 samples showed IC 50 at 50 01-96 15?μg/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.