Cordeiro Thuany de Moura, Borghetti Fabian, Caldas Oliveira Sarah C, Bastos Izabela Marques Dourado, de Santana Jaime Martins, Grellier Philippe, Charneau Sébastien
Department of Cell Biology, Laboratory of Biochemistry and Protein Chemistry, Institute of Biology, University of Brasilia, Darcy Ribeiro Campus, 70910-900, Brasilia, DF, Brazil.
Department of Botany, Laboratory of Thermobiology, Institute of Biology, University of Brasilia, Darcy Ribeiro Campus, 70910-900, Brasilia, DF, Brazil.
Pharmacogn Mag. 2017 Oct-Dec;13(52):668-672. doi: 10.4103/pm.pm_100_17. Epub 2017 Nov 13.
The rapid spread of drug-resistant strains of protozoan parasites required the urgent need for new effective drugs. Natural products offer a variety of chemical structures, which make them a valuable source of lead compounds for the development of such new drugs. Cerrado is the second largest biome in Brazil and has the richest flora of all the world savannahs. We selected , a plant species known for its proprieties in folk medicine and its antibacterial activity.
However, its antiprotozoal activity was not yet explored.
We investigated the activities of fractions from the ethyl acetate extract of leaves against human life forms of , , and , and for its cytotoxicity upon the rat L6-myoblast cell line. Ten fractions were produced by ethyl acetate:hexane chromatography.
The fractions showed no cytotoxicity against L-6 cells (IC > 100 μg/mL) and no hemolysis propriety. Three fractions had a moderate activity against , anyone was active against but four fractions demonstrated a high activity against bloodstream forms of (8.0< IC <15 μg/mL). Identification and characterization of the active compounds are currently under investigation.
is an endemic tree of the Brazilian Cerrado, which presents medicinal propertiesTen fractions of the ethyl acetate extract of leaves were assessed against , , and No fraction showed relevant cytotoxicity and hemolysis activityAll the fractions presented antiplasmodial and trypanocidal activitiesThree fractions with moderate antiplasmodial activity (49< IC <56 μg/mL)Four fractions with high activity against bloodstream forms of (8.0< IC <15 μg/mL). CQ: Chloroquine, DMSO: Dimethyl sulfoxide, HEPES: 4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid, HMI: Modified Iscove's medium, IC: Concentration inhibiting 50% of parasite growth, IC: Concentration inhibiting 90% of parasite growth, MTT: 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide, RPMI: Roswell Park Memorial Institute, SD: Standard deviation, SI: Ratio of cytotoxicity to biological activity - TC/IC, TC: Concentration causing 50% of cell growth inhibition, TC: Concentration causing 90% of cell growth inhibition, TLC: Thin-layer chromatography.
原生动物寄生虫耐药菌株的迅速传播迫切需要新的有效药物。天然产物具有多种化学结构,这使其成为开发此类新药的有价值的先导化合物来源。塞拉多是巴西第二大生物群落,拥有世界所有稀树草原中最丰富的植物群。我们选择了一种在民间医学中因其特性和抗菌活性而闻名的植物物种。
然而,其抗原生动物活性尚未得到探索。
我们研究了该植物叶子乙酸乙酯提取物的各馏分对恶性疟原虫、杜氏利什曼原虫和布氏锥虫人体形态的活性,以及对大鼠L6 - 成肌细胞系的细胞毒性。通过乙酸乙酯:己烷柱色谱法得到了10个馏分。
这些馏分对L - 6细胞无细胞毒性(IC>100μg/mL)且无溶血特性。三个馏分对恶性疟原虫有中等活性,对杜氏利什曼原虫均无活性,但四个馏分对布氏锥虫血流型表现出高活性(8.0<IC<15μg/mL)。目前正在对活性化合物进行鉴定和表征。
该植物是巴西塞拉多的一种特有树木,具有药用特性。对该植物叶子乙酸乙酯提取物的10个馏分针对恶性疟原虫、杜氏利什曼原虫和布氏锥虫进行了评估。没有馏分显示出相关的细胞毒性和溶血活性。所有馏分均表现出抗疟和抗锥虫活性。三个馏分具有中等抗疟活性(49<IC<56μg/mL)。四个馏分对布氏锥虫血流型具有高活性(8.0<IC<15μg/mL)。CQ:氯喹,DMSO:二甲基亚砜,HEPES:4 - (2 - 羟乙基) - 1 - 哌嗪乙磺酸,HMI:改良伊斯科夫培养基,IC:抑制50%寄生虫生长的浓度,IC:抑制90%寄生虫生长的浓度,MTT:3 - (4,5 - 二甲基噻唑 - 2 - 基) - 2,5 - 二苯基四氮唑溴盐,RPMI:罗斯威尔公园纪念研究所,SD:标准差,SI:细胞毒性与生物活性之比 - TC/IC,TC:引起50%细胞生长抑制的浓度,TC:引起90%细胞生长抑制的浓度,TLC:薄层色谱法。