Departamento de Microbiologia, Instituto Aggeu Magalhães IAM-FIOCRUZ/PE, Av. Moraes Rego s/n, Campus da UFPE, 50670-420 Pernambuco, Brazil.
Departamento de Química Fundamental, Universidade Federal de Pernambuco - UFPE, Brazil.
Biomed Pharmacother. 2017 Dec;96:1055-1064. doi: 10.1016/j.biopha.2017.11.121. Epub 2017 Dec 6.
Essential/volatile oils (EOs) from plants used in the traditional medicine are known as a rich source of chemically diverse compounds with relevant biological activities. In this work we analysed the chemical composition and the in vitro effects of EOs from leaves of Eugenia brejoensis (EBEO), Hyptis pectinata (HPEO), Hypenia salzmannii (HSEO), Lippia macrophylla (LMEO) and seeds of Syagrus coronata (SCEO) on Trypanosoma cruzi, the etiological agent of Chagas disease. The EOs were extracted through hydrodistillation and its chemical composition analysed by GC/MS. The trypanocidal activity against epi- and trypomastigotes was evaluated by optical microscopy and the cytotoxicity to mammalian cells by MTT. The effects of EOs on parasite infection in macrophages were estimated by determining the survival index and the percentage of infection inhibition. The cytotoxicity against mammalian cells was compared to those of parasite by determining the Selectivity Index (SI). Overall, 114 compounds were identified: The main constituents of EOS were: δ-cadinene (15.88%), trans-caryophyllene (9.77%) e α-Muurolol (9.42%) for EBEO; trans-caryophyllene (15.24%), bicyclogermacrene (7.33%) e cis-calamenene (7.15%) for HFEO; trans-caryophyllene (30.91%), caryophyllene oxide (13.19%) and spathulenol (5.68%) for HPEO; Xanthoxylin (17.20%) trans-caryophyllene (14.34%) and methyl-eugenol (5.60%) for HSEO; Thymol (49.81%), carvacrol (31.6%) and σ-cimene (10.27%) for LMEO and octanoic acid (38.83%) dodecanoic acid (38.45%) and decanoic acid (20.51%) for SCEO. All the tested oils showed an inhibitory effect on the growth and survival of all forms of T. cruzi and moderate cytotoxicity towards the mammalian cells (100 < CC < 500 μg/mL). The EO of E. brejoensis was the most effective against the parasite presenting higher Selectivity Index for trypo- (SI = 14.45) and amastigote forms (SI = 20.11). Except for SCEO, which was the most cytotoxic for both parasite and mammalian cells, all the oils demonstrated to be more selective for the parasite than the reference drug benznidazole. Taken together our results point the essential oils from Caatinga plants, especially Eugenia brejoensis, as promissory agents for the development of new drugs against Chagas disease.
植物中的必需/挥发性油（EOs）被用于传统医学，它们是化学多样性化合物的丰富来源，具有相关的生物活性。在这项工作中，我们分析了叶片 EO 对 Trypanosoma cruzi 的化学成分和体外作用，Eugenia brejoensis（EBEO）、Hyptis pectinata（HPEO）、Hypenia salzmannii（HSEO）、Lippia macrophylla（LMEO）和 Syagrus coronata（SCEO）的种子。EO 通过水蒸馏提取，通过 GC/MS 分析其化学成分。通过光学显微镜评估对epi 和 trypomastigote 的杀锥虫活性，通过 MTT 评估对哺乳动物细胞的细胞毒性。通过确定生存指数和感染抑制百分比来估计 EO 对巨噬细胞中寄生虫感染的影响。通过确定选择性指数（SI）将对哺乳动物细胞的细胞毒性与寄生虫进行比较。总的来说，鉴定出 114 种化合物：EOS 的主要成分是：δ-杜松烯（15.88%），反式石竹烯（9.77%）和α-Muurolol（9.42%）用于 EBEO；反式石竹烯（15.24%），双环倍半萜烯（7.33%）和顺式芹烷（7.15%）用于 HFEO；反式石竹烯（30.91%），石竹烯氧化物（13.19%）和 spathulenol（5.68%）用于 HPEO；黄樟素（17.20%），反式石竹烯（14.34%）和甲基丁香酚（5.60%）用于 HSEO；百里酚（49.81%），香芹酚（31.6%）和σ-柠檬烯（10.27%）用于 LMEO，辛酸（38.83%），月桂酸（38.45%）和癸酸（20.51%）用于 SCEO。所有测试的油都对所有形式的 T. cruzi 的生长和存活表现出抑制作用，对哺乳动物细胞具有中等细胞毒性（100<CC<500μg/mL）。E. brejoensis 的 EO 对寄生虫最有效，对锥虫（SI=14.45）和阿米巴（SI=20.11）形式的选择性指数更高。除了对寄生虫和哺乳动物细胞均最具细胞毒性的 SCEO 外，所有油均表现出比参考药物苯并咪唑对寄生虫的选择性更高。总的来说，我们的结果表明，来自 Caatinga 植物的精油，特别是 Eugenia brejoensis，是开发治疗恰加斯病新药的有希望的候选药物。
