Laboratório de Imunobiologia das Leishmanioses, Instituto de Microbiologia Paulo de Góes, Universidade Federal do Rio de Janeiro, Avenida Carlos Chagas Filho 373, Bloco D, Sala D1-44, Ilha do Fundão, 21941-902 Rio de Janeiro, RJ, Brazil.
Evid Based Complement Alternat Med. 2013;2013:761323. doi: 10.1155/2013/761323. Epub 2013 Jun 22.
This study investigated the leishmanicidal activity against Leishmania amazonensis of four commercial oils from Copaifera spp. named as C1, C2, C3, and C4, the sesquiterpene and diterpene pools obtained from distilling C4, and isolated β -caryophyllene (CAR). Copaiba oils chemical compositions were analyzed by gas chromatography and correlated with biological activities. Diterpenes-rich oils C2 and C3 showed antipromastigote activity. Sesquiterpenes-rich C1 and C4, and isolated CAR presented a dose-dependent activity against intracellular amastigotes, with IC50s of 2.9 µ g/mL, 2.3 µ g/mL, and 1.3 µ g/mL (6.4 µ M), respectively. Based on the highest antiamastigote activity and the low toxicity to the host cells, C4 was steamdistillated to separate pools of sesquiterpenes and diterpenes. Both pools were less active against L. amazonensis and more toxic for the macrophages than the whole C4 oil. The leishmanicidal activity of C3 and C4 oils, as well as C4 fractions and CAR, appears to be independent of nitric oxide production by macrophages. This study pointed out β -caryophyllene as an effective antileishmanial compound and also to its role as potential chemical marker in copaiba oils or fractions derived thereof, aiming further development of this rainforest raw material for leishmaniasis therapy.
本研究调查了四种来自 Copaifera spp. 的商业油（分别命名为 C1、C2、C3 和 C4）对 Leishmania amazonensis 的杀利什曼原虫活性，以及从 C4 蒸馏获得的倍半萜烯和二萜烯池，以及分离出的 β-石竹烯 (CAR)。通过气相色谱法分析 Copaiba 油的化学成分，并将其与生物活性相关联。富含二萜烯的油 C2 和 C3 表现出抗前鞭毛体活性。富含倍半萜烯的 C1 和 C4 以及分离出的 CAR 对细胞内无鞭毛体表现出剂量依赖性活性，IC50 分别为 2.9 µg/mL、2.3 µg/mL 和 1.3 µg/mL（6.4 µM）。基于最高的抗无鞭毛体活性和对宿主细胞的低毒性，C4 被蒸汽蒸馏以分离倍半萜烯和二萜烯池。与整个 C4 油相比，这两个池对 L. amazonensis 的活性较低，对巨噬细胞的毒性较大。C3 和 C4 油以及 C4 馏分和 CAR 的杀利什曼原虫活性似乎与巨噬细胞中一氧化氮的产生无关。本研究指出 β-石竹烯是一种有效的抗利什曼原虫化合物，也是 Copaiba 油或其衍生的馏分的潜在化学标志物，旨在进一步开发这种热带雨林原料用于治疗利什曼病。
