Programa de Pós-Graduação em Ciências Farmacêuticas, Laboratório de Produtos Naturais, Department of Pharmacy, Universidade Vila Velha-UVV, Av. Comissário José Dantas de Melo,no. 21, Boa Vista, Vila Velha, Espírito Santo, 29102-920, Brazil.
Department of Pharmaceutical Sciences, Daniel K. Inouye College of Pharmacy, University of Hawaii at Hilo, Hilo, HI, 96720, USA.
Inflammopharmacology. 2019 Apr;27(2):281-289. doi: 10.1007/s10787-018-0483-z. Epub 2018 Apr 19.
Terpenes are considered the main components of essential oils and an important source for the identification of novel lead molecules. This study aimed to investigate the in vitro anti-inflammatory activity of L-carveol, L-carvone, and m-cimene (monoterpenes) and of valencene and guaiene (sesquiterpenes).
The influence on intracellular nitric oxide (NO) and pro- and anti-inflammatory cytokine (TNF-α, IL-1α and IL-10) production and on nuclear factor kappa B (NF-κB) activity was determined using Griess reagent, immunoenzymatic assay kits (ELISA) and chemiluminescence measurements in cell-based assays, respectively. Antioxidant activity was assayed through the protective effect against cellular oxidative damage produced by superoxide anion production (O ) and hydrogen peroxide on macrophages and by the quenching activity of the NO radical.
Terpenes reduced the pro-inflammatory cytokines TNF-α and IL-1α and increased the production of IL-10. In addition, the terpenes, especially guaiene (53.3 ± 2.4%) and m-cymene (38.1 ± 0.6%), significantly inhibited NO production in a macrophage cell culture-based assay, whereas no effect was observed in the scavenging activity of this radical. L-carveol and m-cymene significantly inhibited O production with reductions of approximately 68.6 ± 2.2% and 48.2 ± 4.2%, respectively, at a concentration of 10 μM. Moreover, these terpenes were verified to suppress NF-κB activity. The results indicate that these terpenes have therapeutic potential and may be used to suppress inflammatory diseases or as a leading compounds.
萜类化合物被认为是精油的主要成分，也是鉴定新型先导分子的重要来源。本研究旨在研究 L-香芹醇、L-香芹酮和 m-桧烯（单萜）以及柠檬烯和愈创木烯（倍半萜）的体外抗炎活性。
通过使用 Gries 试剂、免疫酶测定试剂盒（ELISA）和化学发光测量法，分别在细胞基础测定中确定对细胞内一氧化氮（NO）和促炎和抗炎细胞因子（TNF-α、IL-1α 和 IL-10）产生的影响以及核因子 kappa B（NF-κB）的活性。抗氧化活性通过对超氧阴离子（O ）和过氧化氢产生的细胞氧化损伤的保护作用以及通过 NO 自由基的淬灭活性来测定。
萜类化合物降低了促炎细胞因子 TNF-α 和 IL-1α 的产生，增加了 IL-10 的产生。此外，萜类化合物，特别是愈创木烯（53.3±2.4%）和 m-桧烯（38.1±0.6%），在基于巨噬细胞的细胞培养测定中显著抑制了 NO 的产生，而在该自由基的清除活性方面则没有观察到作用。L-香芹醇和 m-桧烯在 10 μM 浓度下分别显著降低了约 68.6±2.2%和 48.2±4.2%的 O 产生。此外，这些萜类化合物被证实可抑制 NF-κB 活性。结果表明，这些萜类化合物具有治疗潜力，可用于抑制炎症性疾病或作为先导化合物。
