Programa de Pós-Graduação em Biociências, Universidade Federal do Oeste do Pará, Santarém, PA, 68040-255, Brazil; Laboratório de Pesquisa e Desenvolvimento de Produtos Naturais e Bioativos (P&DBio), Instituto de Biodiversidade e Floresta, Universidade Federal do Oeste do Pará, 68040-255, Santarém, PA, Brazil.
Laboratório de Pesquisa e Desenvolvimento de Produtos Naturais e Bioativos (P&DBio), Instituto de Biodiversidade e Floresta, Universidade Federal do Oeste do Pará, 68040-255, Santarém, PA, Brazil.
Exp Parasitol. 2020 Mar;210:107847. doi: 10.1016/j.exppara.2020.107847. Epub 2020 Jan 28.
Leishmaniasis is an infectious disease that has high endemicity and is among the six parasitic diseases of higher occurrence in the world. The current treatments are limited due to their toxicity, treatment resistance and high cost which have increased the search for new substances of natural origin for its therapy. Based on this, an in vitro biological and chemical investigation was carried out to evaluate the potential of Piper marginatum against Leishmania amazonesis. P. marginatum leaves were collected to obtain the essential oil (EO) and the ethanolic extract (CE). The chemical profile of the CE and fractions was obtained by 1H NMR. The analysis of the EO chemical composition was performed by GC-MS. EO, CE and fractions were submitted to antileishmanial and cytotoxicity assays against macrophages. The chromatographic profiles of EO, CE and fractions showed the presence of phenolic compounds and terpenoids, having 3,4-Methylenedioxypropiophenone as a major compound. All P. marginatum samples showed low toxicity to macrophages. The CE and the methanolic, hexane and ethyl acetate fractions had low cytotoxicity when compared to Pentamidine. All tested samples inhibited growth of L. amazonensis promastigotes. The antileishmanial activity of EO, CE and fractions were evaluated in macrophages infected with L. (L.) amazonensis and treated with the concentrations 1, 10 and 100 μg/mL for 48 h. All samples were active, but EO and CE showed superior activity against amastigote forms when compared to the promastigote forms of L. amazonensis. This work describes for the first time the antileishmanial activity of the species P. marginatum and its cytotoxicity against macrophages, suggesting that it can be an alternative source of natural products in the phytotherapeutic treatment of leishmaniasis.
利什曼病是一种传染性疾病,具有高地方性,是世界上六种高发性寄生虫病之一。由于其毒性、治疗耐药性和高成本,目前的治疗方法受到限制,这增加了对新的天然来源物质用于治疗的研究。基于此,进行了一项体外生物学和化学研究,以评估 Piper marginatum 对 Leishmania amazonesis 的潜在作用。采集 Piper marginatum 的叶子以获得精油(EO)和乙醇提取物(CE)。通过 1H NMR 获得 CE 和馏分的化学特征。通过 GC-MS 进行 EO 化学成分分析。EO、CE 和馏分均进行抗利什曼原虫和对巨噬细胞的细胞毒性测定。EO、CE 和馏分的色谱图显示存在酚类化合物和萜类化合物,其中 3,4-亚甲二氧基丙基苯酮是主要化合物。所有 Piper marginatum 样品对巨噬细胞的毒性都较低。与戊烷脒相比,CE 和甲醇、己烷和乙酸乙酯馏分的细胞毒性较低。所有测试的样品均抑制 L. amazonensis 前鞭毛体的生长。在感染了 L.(L.)amazonensis 的巨噬细胞中,用浓度为 1、10 和 100μg/mL 处理 48h 后,评价 EO、CE 和馏分的抗利什曼原虫活性。所有样品均具有活性,但 EO 和 CE 对利什曼原虫前鞭毛体的活性优于对利什曼原虫的活性。本研究首次描述了 Piper marginatum 的抗利什曼原虫活性及其对巨噬细胞的细胞毒性,表明它可能是植物疗法治疗利什曼病的天然产物的替代来源。