GNOS Research Group, Louvain Drug Research Institute, Université catholique de Louvain, UCLouvain, 1200 Bruxelles, Belgium.
Department of Pharmacognosy, Hanoi University of Pharmacy, 13-15 Le Thanh Tong, Hoan Kiem, Hanoi 100000, Vietnam.
Molecules. 2019 Mar 23;24(6):1158. doi: 10.3390/molecules24061158.
Human African trypanosomiasis (HAT), known as sleeping sickness and caused by , is threatening low-income populations in sub-Saharan African countries with 61 million people at risk of infection. In order to discover new natural products against HAT, thirty-seven Vietnamese essential oils (EOs) were screened for their activity in vitro on () and cytotoxicity on mammalian cells (WI38, J774). Based on the selectivity indices (SIs), the more active and selective EOs were analyzed by gas chromatography. The anti-trypanosomal activity and cytotoxicity of some major compounds (isolated or commercial) were also determined. Our results showed for the first time the selective anti-trypanosomal effect of four EOs, extracted from three Zingiberaceae species (, , and ) and one Lauraceae species () with IC values of 3.17 ± 0.72, 2.51 ± 1.08, 3.10 ± 0.08, and 2.67 ± 1.12 nL/mL respectively and SI > 10. Identified compounds accounted for more than 85% for each of them. Among the five major components of EO, curlone is the most promising anti-trypanosomal candidate with an IC of 1.38 ± 0.45 µg/mL and SIs of 31.7 and 18.2 compared to WI38 and J774 respectively.
人类非洲锥虫病（HAT），又称昏睡病，由 引起，正在威胁撒哈拉以南非洲国家的低收入人群，有 6100 万人面临感染风险。为了发现针对 HAT 的新天然产物，对 37 种越南精油（EOs）进行了体外抗 活性和对哺乳动物细胞（WI38、J774）的细胞毒性筛选。基于选择性指数（SIs），通过气相色谱对更活跃和选择性的 EOs 进行了分析。还测定了一些主要化合物（分离或商业）的抗锥虫活性和细胞毒性。我们的结果首次表明，四种从三种姜科植物（ 、 和 ）和一种樟科植物（ ）中提取的 EOs 具有选择性抗锥虫作用，其 IC 值分别为 3.17 ± 0.72、2.51 ± 1.08、3.10 ± 0.08 和 2.67 ± 1.12 nL/mL，SI > 10。鉴定出的化合物分别占它们各自的 85%以上。在 精油的五个主要成分中，卷曲酮是最有前途的抗锥虫候选物，其 IC 为 1.38 ± 0.45 µg/mL，与 WI38 和 J774 相比，SI 分别为 31.7 和 18.2。
