从天然提取物或分离部位中以碳酸酐酶II为靶点的抗骨质疏松活性筛选(英文)

Searching for Antiosteoporotic Activities of Extracts and Fractions Derived from Natural Sources Targeting Carbonic Anhydrase II

目的是以碳酸酐酶II (CAII)为靶点筛选其抑制剂 ,以期寻找抗骨质疏松活性样品。实验是在 96孔酶标板上对来源于 1 78个科、 60 8个属、 1 0 2 0种动植物 2 91 9个提取物或分离部位样品在CA II模型上进行了批量筛选。结果表明在 1 0 μg ml浓度下发现了来源于 40个科、61个属、72个种的 1 0 0个样品有活性 ,其中 5个样品的IC50 小于 2 50 μg ml,2 2个样品的IC50 在 2 51～ 5 0 0 μg ml范围 ,73个样品的IC50 在 5 0 1～1 0 0 0 μg ml范围。通过以上工作我们认为以碳酸酐酶II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骨质疏松活性筛选。

To discover inhibitors of carbonic anhydrase II (CA II) with antiosteoporotic activity a batch of 2919 extract or fraction samples prepared from plants and animals belonging to 178 families,608 genera and 1020 species were tested on carbonic anhydrase II bioassay (CA-II) in 96-well microtiterplates.Finally 100 samples, which belong to 40 families, 61 genera and 72 species, showed inhibitory activity at 10μg/ml, in which 5 samples showed IC_(50) at =<2.50μg/ml,22 samples showed IC_(50) at 2.51-5.00μg/ml and 73 samples showed IC_(50) at 5.01-10.00μg/ml.It is indicated that this in-vitro bioassay is convenient,stable,rapid,sensitive and effective in searching for antiosteoporotic activity samples from natural sources.