Laboratório de Bioensaios em Leishmania, ICBIM, Universidade Federal de Uberlândia, Uberlândia, MG, Brazil.
Departamento de Fisiologia e Biofísica, ICB, Universidade Federal de Minas Gerais, Belo Horizonte, MG, Brazil.
J Ethnopharmacol. 2019 Mar 25;232:155-164. doi: 10.1016/j.jep.2018.12.026. Epub 2018 Dec 21.
Leishmaniasis is a parasitic disease that affects people all over the world. The number of cases of leishmaniasis is increasing and the drugs used for its treatment are toxic and not always effective. The recognition of the global nature of this disease and its direct or indirect effects on health economics and actions focuses attention on the development of new therapeutic options. In Brazil, this parasitic disease is endemic in many regions. The plants used by the population against leishmaniasis can be good starting points in the search of new lead compounds for antileishmanial drugs.
The aim of the present study was to investigate the antileishmanial activity of extracts from leaves and stems of seven Brazilian plant species used by the population to treat leishmaniasis, and symptoms that might be related to Leishmania infections.
Twenty two extracts from seven plants belonging to five different botanical families were prepared by different methods and evaluated for their effect on the viability of promastigote forms of Leishmania infantum (MHOM/BR/1967/BH46) using the resazurin-based colorimetric assay. The extracts were considered active when they inhibited the growth of promastigotes in a percentage greater than or equal to 50% at 100 and 200 µg/mL. The active samples were further investigated to determine IC, CC and SI values against promastigote forms of L. infantum. The active and non-cytotoxic extracts (SI> 10) were evaluated against amastigote forms of L. infantum. In addition, the active extracts against the amastigote forms were analyzed by TLC and HPLC, while the EtOAc extract of stems from Aspidosperma tomentosum was also evaluated by GC/MS.
Among the twenty two extracts evaluated, two were considered active against L. infantum. The EtOH extract of leaves from Dyospiros hispida (IC 55.48 ± 2.77 µg/mL and IC 80.63 ± 13.17 µg/mL, respectively) and the EtOAc extract of stems from Aspidosperma tomentosum (IC 9.70 ± 2.82 µg/mL and IC 15.88 ± 1.53 µg/mL, respectively) inhibited significantly the growth of promastigote and amastigote forms of L. infantum. Some extracts, although active in the initial screening, were considered toxic since the SI was lower than 10. In TLC and HPLC analysis the leaf extract of Dyospiros hispida showed the presence of anthraquinones, terpenes and saponins, and in the EtOAc extract of stems from Aspidosperma tomentosum alkaloids and flavonoids were detected. In addition, in the latter extract the indole alkaloids uleine and dasycarpidone could be identified by GC/MS.
The ethnopharmacological data of Aspidosperma tomentosum and Dyospiros hispida in part support the results found in the biological models used. Extracts of Aspidosperma tomentosum and Dyospiros hispida presented promising results against L. infantum.
利什曼病是一种影响全世界人民的寄生虫病。利什曼病的病例数正在增加,用于治疗该病的药物具有毒性,并不总是有效。这种疾病的全球性及其对卫生经济学和行动的直接或间接影响引起了人们对新治疗选择的关注。在巴西,这种寄生虫病在许多地区流行。巴西民众用于治疗利什曼病的植物可能是寻找新型抗利什曼病药物先导化合物的良好起点。
本研究旨在研究七种巴西植物叶和茎的提取物对利什曼原虫(MHOM/BR/1967/BH46)前鞭毛体活力的抗利什曼活性,以及可能与利什曼虫感染相关的症状。
采用不同方法制备了来自五个不同植物科的七种植物的 22 种提取物,并使用基于 Resazurin 的比色法评估它们对利什曼原虫前鞭毛体活力的影响。当 100 和 200 μg/mL 时,提取物抑制前鞭毛体生长的百分比大于或等于 50%,则认为提取物具有活性。进一步研究活性样品以确定对 L. infantum 前鞭毛体的 IC、CC 和 SI 值。对活性和非细胞毒性提取物(SI>10)进行了对抗 L. infantum 无鞭毛体的评估。此外,还通过 TLC 和 HPLC 分析了对抗无鞭毛体的活性提取物,同时还通过 GC/MS 评估了 Aspidosperma tomentosum 茎的 EtOAc 提取物。
在所评估的 22 种提取物中,有两种被认为对 L. infantum 具有活性。Dyospiros hispida 叶的 EtOH 提取物(IC 55.48±2.77μg/mL 和 IC 80.63±13.17μg/mL)和 Aspidosperma tomentosum 茎的 EtOAc 提取物(IC 9.70±2.82μg/mL 和 IC 15.88±1.53μg/mL)显著抑制了 L. infantum 的前鞭毛体和无鞭毛体的生长。尽管一些提取物在初步筛选中具有活性,但由于 SI 低于 10,因此被认为具有毒性。在 TLC 和 HPLC 分析中,Dyospiros hispida 的叶提取物显示出蒽醌、萜类化合物和皂苷的存在,而 Aspidosperma tomentosum 茎的 EtOAc 提取物中检测到生物碱和类黄酮。此外,在后者提取物中,吲哚生物碱 uleine 和 dasycarpidone 可以通过 GC/MS 来识别。
Aspidosperma tomentosum 和 Dyospiros hispida 的民族药理学数据在一定程度上支持了在使用的生物模型中发现的结果。Aspidosperma tomentosum 和 Dyospiros hispida 的提取物对 L. infantum 表现出有希望的结果。