Department of Microbiology and Cell Biology, Montana State University, Bozeman, MT 59717, USA.
Department of Pharmacognosy, Faculty of Pharmacy, Anadolu University, Eskisehir 26470, Turkey.
Molecules. 2021 Jun 15;26(12):3652. doi: 10.3390/molecules26123652.
(Ericaceae) extracts contain flavonoids, chromones, terpenoids, steroids, and essential oils and are used in traditional ethnobotanical medicine. However, little is known about the immunomodulatory activity of essential oils isolated from these plants. Thus, we isolated essential oils from the flowers and leaves of (cascade azalea) and analyzed their chemical composition and innate immunomodulatory activity. Compositional analysis of flower (REO) versus leaf (REO) essential oils revealed significant differences. REO was comprised mainly of monoterpenes (92%), whereas sesquiterpenes were found in relatively low amounts. In contrast, REO was primarily composed of sesquiterpenes (90.9%), with a small number of monoterpenes. REO and its primary sesquiterpenes (viridiflorol, spathulenol, curzerene, and germacrone) induced intracellular Ca mobilization in human neutrophils, C20 microglial cells, and HL60 cells transfected with -formyl peptide receptor 1 (FPR1) or FPR2. On the other hand, pretreatment with these essential oils or component compounds inhibited agonist-induced Ca mobilization and chemotaxis in human neutrophils and agonist-induced Ca mobilization in microglial cells and FPR-transfected HL60 cells, indicating that the direct effect of these compounds on [Ca] desensitized the cells to subsequent agonist activation. Reverse pharmacophore mapping suggested several potential kinase targets for these compounds; however, these targets were not supported by kinase binding assays. Our results provide a cellular and molecular basis to explain at least part of the beneficial immunotherapeutic properties of the essential oils and suggest that essential oils from leaves of this plant may be effective in modulating some innate immune responses, possibly by inhibition of neutrophil migration.
(杜鹃花科)提取物含有类黄酮、色酮、萜类、甾体和精油,用于传统的民族植物医学。然而,对于从这些植物中分离出的精油的免疫调节活性知之甚少。因此,我们从 ( cascade azalea)的花和叶中分离出精油,并分析了它们的化学成分和先天免疫调节活性。花(REO)与叶(REO)精油的成分分析显示出显著差异。REO 主要由单萜组成(92%),而倍半萜含量相对较低。相比之下,REO 主要由倍半萜组成(90.9%),单萜含量较少。REO 及其主要倍半萜(viridiflorol、spathulenol、curzerene 和 germacrone)在人类中性粒细胞、C20 小胶质细胞和转染 FPR1 或 FPR2 的 HL60 细胞中诱导细胞内 Ca 动员。另一方面,这些精油或成分化合物预处理抑制了人类中性粒细胞激动剂诱导的 Ca 动员和趋化作用,以及小胶质细胞和 FPR 转染的 HL60 细胞中激动剂诱导的 Ca 动员,表明这些化合物对 [Ca] 的直接作用使细胞对随后的激动剂激活脱敏。反向药效团映射表明这些化合物的几个潜在激酶靶标;然而,这些靶标没有被激酶结合测定支持。我们的研究结果为解释至少部分 精油的有益免疫治疗特性提供了细胞和分子基础,并表明该植物叶片的精油可能通过抑制中性粒细胞迁移来有效调节某些先天免疫反应。