CNRS, Institut Galien Paris-Saclay, Université Paris-Saclay, 92296, Châtenay-Malabry, France.
Laboratoire Matériaux Molécules et applications, Institut préparatoire des études scientifiques et techniques (IPEST), Univ. de Carthage, La Marsa, Tunisia.
Parasitol Res. 2021 Apr;120(4):1455-1469. doi: 10.1007/s00436-020-06952-5. Epub 2021 Jan 10.
Leishmaniasis is a tropical parasitic disease that affects up to 12 million people worldwide. Current chemotherapies have limitations such as toxicity, high cost, and parasite resistance. This work aims to select an essential oil (EssOil) isolated from the Tunisian flora as a new antileishmanial candidate. Two plants were chosen for their antileishmanial potential: Citrus limon (Citrus) and Pistacia lentiscus (Pistacia). Each of these plants was harvested from two different sites (area 1 and area 2). Extracted EssOils were characterized using GC-MS. Their antiparasitic activity against axenic and intracellular Leishmania major amastigotes and their cytotoxicity were assessed. Citrus EssOil from area 1 displayed an interesting activity against L. major intramacrophage amastigotes with IC value at 4.2 ± 1.3 μg/mL. Interestingly, this activity was close to that of miltefosine. Moderate activities against intracellular amastigote were observed for Pistacia EssOil from area 1 and Citrus EssOil from area 2. However, low cytotoxicity with high selectivity index was proved only for Citrus EssOil from area 1, revealing its safety for macrophages. This study also demonstrated for the first time the antileishmanial activity of EssOil extracted from Citrus limon leaves. The EssOil interesting activity could be related to the lipophilic properties of terpenes that were shown in literature to contribute to the disruption of parasite intracellular metabolic pathways.
利什曼病是一种热带寄生虫病，影响全球多达 1200 万人。目前的化疗方法存在毒性、成本高和寄生虫耐药性等局限性。本工作旨在选择一种从突尼斯植物群中分离出来的精油（EssOil）作为新的抗利什曼原虫候选药物。选择了两种具有抗利什曼原虫潜力的植物：柠檬（Citrus）和乳香黄连木（Pistacia）。从这两种植物的两个不同地点（区域 1 和区域 2）采集这些植物。使用 GC-MS 对提取的 EssOils 进行了表征。评估了它们对体外和细胞内利什曼原虫无鞭毛体的抗寄生虫活性及其细胞毒性。来自区域 1 的柠檬 EssOil 对 L. major 细胞内无鞭毛体具有有趣的活性，IC 值为 4.2±1.3μg/mL。有趣的是，这种活性与米替福新相当。来自区域 1 的乳香黄连木 EssOil 和来自区域 2 的柠檬 EssOil 对细胞内无鞭毛体表现出中等活性。然而，仅来自区域 1 的柠檬 EssOil 表现出低细胞毒性和高选择性指数，表明其对巨噬细胞安全。本研究还首次证明了从柠檬（Citrus limon）叶片中提取的 EssOil 的抗利什曼原虫活性。EssOil 的有趣活性可能与萜类化合物的亲脂性有关，文献表明萜类化合物有助于破坏寄生虫细胞内的代谢途径。
