Cardona-G Wilson, Robledo Sara, Alzate Fernando, Yepes Andrés F, Hernandez Cristian, Velez Ivan Dario, Calderon Juan Carlos, Tabares Isabel Vásquez
Chemistry of Colombian Plants, Institute of Chemistry, Natural and Exact Sciences Faculty, Universidad de Antioquia, Colombia.
Group of Botanical Studies, Institute of Biology, Natural and Exact Sciences Faculty, Universidad de Antioquia, Colombia.
Vet World. 2020 Oct;13(10):2178-2182. doi: 10.14202/vetworld.2020.2178-2182. Epub 2020 Oct 19.
(L.S) Cuatrec., (P.F) Kunth, (O.F), and (P.B) belong to the families Chrysobalanaceae, Lauraceae, Araliaceae, and Rubiaceae, respectively, which have been used as medicines by communities in the Andes. This study evaluated the leishmanicidal and cytotoxic activities of alcohol and non-alcohol extracts from four Andean plant extracts (L.S, O.F, P.F, and P.B).
Extracts were obtained by percolation with solvents of different polarities - hexane, dichloromethane, ethyl acetate, and ethanol. Phytochemical screening was conducted based on reported methods. All products were evaluated to determine the leishmanicidal activity against amastigotes of and cytotoxicity against U937 cells.
Flavonoids, triterpenes, and tannins were the main secondary metabolites found. From the results, dichloromethane extracts from O.F and P.B, ethanol extract from P.B, and ethyl acetate extracts of all plants were active, with EC <30 μg/mL. Ethyl acetate was the most active extract, which showed EC values of 9.8, 14.1, 23.7, and 25.5 μg/mL, for L.S, P.B, O.F, and P.F, respectively. Hexane extracts from P.B and O.F exhibited moderate activity with EC values of 84.8 and 87.4 μg/mL, respectively. Hexane and ethanol extracts from O.F, ethyl acetate, and ethanol extracts from L.S, and all extracts from P.F were not toxic. Alternatively, hexane and dichloromethane extracts from L.S and P.B as well as dichloromethane and ethyl acetate extracts from O.F displayed high toxicity.
Based on the activity we observed, ethyl acetate extract can continue in its usage in the search for new antileishmanial drugs, mainly ethyl acetate extract from L.S showed activity comparable to meglumine antimoniate and was not cytotoxic.
(L.S)Cuatrec.、(P.F)Kunth、(O.F)和(P.B)分别属于金虎尾科、樟科、五加科和茜草科,安第斯地区的社区一直将这些植物用作药物。本研究评估了四种安第斯植物提取物(L.S、O.F、P.F和P.B)的乙醇提取物和非乙醇提取物的杀利什曼原虫活性和细胞毒性。
通过用不同极性的溶剂——己烷、二氯甲烷、乙酸乙酯和乙醇进行渗漉来获得提取物。根据报道的方法进行植物化学筛选。评估所有产品以确定其对利什曼原虫无鞭毛体的杀利什曼原虫活性以及对U937细胞的细胞毒性。
发现主要的次生代谢产物为黄酮类、三萜类和单宁类。结果显示,O.F和P.B的二氯甲烷提取物、P.B的乙醇提取物以及所有植物的乙酸乙酯提取物具有活性,其半数有效浓度(EC)<30μg/mL。乙酸乙酯是活性最高的提取物,L.S、P.B、O.F和P.F的EC值分别为9.8、14.1、23.7和25.5μg/mL。P.B和O.F的己烷提取物表现出中等活性,EC值分别为84.8和87.4μg/mL。O.F的己烷和乙醇提取物、L.S的乙酸乙酯和乙醇提取物以及P.F的所有提取物均无毒性。另外,L.S和P.B的己烷和二氯甲烷提取物以及O.F的二氯甲烷和乙酸乙酯提取物显示出高毒性。
基于我们观察到的活性,乙酸乙酯提取物可继续用于寻找新的抗利什曼原虫药物,主要是L.S的乙酸乙酯提取物显示出与葡甲胺锑酸盐相当的活性且无细胞毒性。