Monzote Lianet, Piñón Abel, Setzer William N
Parasitology Department, Institute of Tropical Medicine "Pedro Kouri", 10400 Havana, Cuba.
Department of Chemistry, University of Alabama in Huntsville, Huntsville, AL 35899, USA.
Medicines (Basel). 2014 Nov 19;1(1):32-55. doi: 10.3390/medicines1010032.
A total of 115 different plant extracts from our collection, representing 96 plant species, have been evaluated for antileishmanial activity against promastigotes. In addition, the extracts were screened for cytotoxic activity against BALB/c mouse macrophages in order to assess a selectivity index. Crude extracts that showed a selectivity index ( for macrophage / for promastigotes) ³ 5 or with < 12.5 μg/mL against promastigotes, a total of 28 extracts, were further screened for anti-amastigote activity. A total of 25 extracts showed promising activity against promastigotes with low cytotoxic activity. Ten of these extracts showed selectivity indices, ( for macrophages / for amastigotes) greater than 10 and are considered "hits", worthy candidates for further phytochemical exploration: methanol bark extract, bark extract, acetone bark extract, sp. "fine leaf" acetone bark extract, chloroform bark extract, ethanol bark extract, ethanol extract, ethanol bark extract, dichloromethane bark extract, and acetone bark extract.
我们从收集的植物提取物中选取了总共115种不同的提取物,它们代表了96种植物,已针对前鞭毛体进行了抗利什曼原虫活性评估。此外,还对这些提取物进行了针对BALB/c小鼠巨噬细胞的细胞毒性活性筛选,以评估选择性指数。对于显示选择性指数(巨噬细胞IC50/前鞭毛体IC50)≥5或前鞭毛体IC50<12.5μg/mL的粗提物,总共28种提取物,进一步筛选其抗无鞭毛体活性。共有25种提取物对前鞭毛体显示出有前景的活性且细胞毒性活性较低。其中10种提取物的选择性指数(巨噬细胞IC50/无鞭毛体IC50)大于10,被认为是“命中物”,是进一步进行植物化学探索的有价值候选物:甲醇树皮提取物、树皮提取物、丙酮树皮提取物、“细叶”种丙酮树皮提取物、氯仿树皮提取物、乙醇树皮提取物、乙醇提取物、乙醇树皮提取物、二氯甲烷树皮提取物和丙酮树皮提取物。