Laboratório de Farmacognosia, Universidade de Brasília, Brasília, Brazil.
J Ethnopharmacol. 2010 Aug 19;131(1):116-21. doi: 10.1016/j.jep.2010.06.011. Epub 2010 Jun 22.
To investigate the activities of the 217 plant extracts in traditional medicine of the Brazilian Cerrado against protozoans and yeasts.
Plant extracts were prepared by the method of maceration using solvents of different polarities. The growth inhibition of chloroquine-resistant Plasmodium falciparum strain (FcB1) was determined by measuring the radioactivity of the tritiated hypoxanthine incorporated. Activity against Leishmania (Leishmania) chagasi and Trypanosoma cruzi was measured by the MTT colorimetric assay. The antifungal tests were carried out by using the CLSI method. The active extracts were tested also by cytotoxicity assay using NIH-3T3 cells of mammalian fibroblasts.
Two hundred and seventeen extracts of plants were tested against Plasmodium falciparum. The eleven active extracts, belonging to eight plant species were evaluated against L. (L.) chagasi, Trypanosoma cruzi, yeasts and in NIH-3T3 cells. The results found in these biological models are consistent with the ethnopharmacological data of these plants. The ethyl acetate extract of Diospyros hispida root showed IC(50) values of 1 microg/mL against Plasmodium falciparum. This extract demonstrated no toxicity against mammalian cells, resulting in a significant selectivity index (SI) of 435.8. The dichloromethane extract of Calophyllum brasiliense root wood was active against Cryptococcus gattii LMGO 01 with MIC of 1.95 microg/mL; and Candida albicans ATCC 10231 and Candida krusei LMGO 174, both with MIC of 7.81 microg/mL. The same extract was also active against Plasmodium falciparum and L. (L.) chagasi with IC(50) of 6.7 and 27.6 microg/mL respectively. The ethyl acetate extract of Spiranthera odoratissima leaves was active against Cryptococcus gattii LMGO 01 with MIC of 31.25 microg/mL, and against Plasmodium falciparum with IC(50) of 9.2 microg/mL and Trypanosoma cruzi with IC(50) of 56.3 microg/mL.
The active extracts for protozoans and human pathogenic yeasts are considered promising to continue the search for the identification and development of leading compounds.
研究巴西塞拉多传统医学中的 217 种植物提取物对原生动物和酵母的活性。
采用不同极性溶剂的浸渍法制备植物提取物。通过测量放射性标记的次黄嘌呤掺入来测定氯喹耐药恶性疟原虫（FcB1）的生长抑制。使用 MTT 比色法测定对利什曼原虫（L.）查加斯和克氏锥虫的活性。使用 CLSI 方法进行抗真菌试验。还使用哺乳动物成纤维细胞 NIH-3T3 细胞进行细胞毒性试验测试活性提取物。
对 217 种植物提取物进行了抗疟原虫活性检测。11 种活性提取物，来自 8 种植物，针对 L.（L.）查加斯、克氏锥虫、酵母和 NIH-3T3 细胞进行了评估。这些生物模型中的结果与这些植物的民族药理学数据一致。Diospyros hispida 根的乙酸乙酯提取物对恶性疟原虫的 IC50 值为 1 μg/mL。该提取物对哺乳动物细胞无毒性，导致显著的选择性指数（SI）为 435.8。Calophyllum brasiliense 根木的二氯甲烷提取物对隐球菌属 gattii LMGO 01 的 MIC 为 1.95 μg/mL；白色念珠菌 ATCC 10231 和克柔念珠菌 LMGO 174 的 MIC 均为 7.81 μg/mL。相同的提取物也对恶性疟原虫和 L.（L.）查加斯具有活性，IC50 值分别为 6.7 和 27.6 μg/mL。Spiranthera odoratissima 叶的乙酸乙酯提取物对隐球菌属 gattii LMGO 01 的 MIC 为 31.25 μg/mL，对恶性疟原虫的 IC50 值为 9.2 μg/mL，对克氏锥虫的 IC50 值为 56.3 μg/mL。
针对原生动物和人类致病性酵母的活性提取物被认为有希望继续寻找鉴定和开发先导化合物。
