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Mechanistic action of linalyl acetate: Acyclic monoterpene isolated from bitter orange leaf as anti-inflammatory, analgesic, antipyretic agent: Role of TNF-α, IL1β, PGE2, and COX-2
Industrial Crops and Products ( IF 5.6 ) Pub Date : 2023-07-18 , DOI: 10.1016/j.indcrop.2023.117131
Abdulwahab Alqahtani , Mohamed F. Abdelhameed , Randa Abdou , Ammar M. Ibrahim , Mohamed Dawoud , Saeed M. Alasmari , Mohamed A. El Raey , Hany G. Attia

The intervention of inflammation disorders with conventional synthetic drugs has several hazards. Medicinal plants and their byproducts are beneficial in the treatment of inflammations with greater safety. Herein, the essential oils of bitter orange leaf extract (Citrus aurantium) were characterized via GC-MS, whereby, Linalyl acetate was the most major compound was isolated using column chromatography and identified by NMR analysis. The in vivo inflammation inhibition activity against carrageenan-induced models, and central analgesic effect as well as antipyretic potentiality of linalyl acetate were evaluated in rats. The administration of linalyl acetate (100 and 200 mg/kg) exhibited significant fast onset not long-standing anti-inflammatory effect in rat paw edema model in dose-dependent manner, compared to the control and reference drug. This significant inflammation reduction were supported by improving the antioxidant status of the paw via reduction of malondialdehyde (MDA) level and restoration of glutathione (GSH) levels as well as attenuation of proinflammatory cytokines levels (TNF-α), IL-1b, prostaglandin E2 (PGE2), and COX-2 in paw tissues. Although, the oral administration of linalyl acetate (100 and 200 mg/kg) has minimal analgesic it has potent long-lasting antipyretic activity in rats. The higher dose of linalyl acetate (200 mg/kg) displayed fast-onset anti-inflammatory activity better than the reference drug. Furthermore, linalyl acetate (200 mg/kg) has the best antipyretic activity. These findings shed light on promising medicinal uses of linalyl acetate against numerous inflammatory and hyperthermia ailments that could be attributed to its active constituents.



中文翻译:

乙酸芳樟酯的机制作用:从苦橙叶中分离出的无环单萜作为抗炎、镇痛、解热剂:TNF-α、IL1β、PGE2 和 COX-2 的作用

用常规合成药物干预炎症性疾病存在多种危险。药用植物及其副产品有助于更安全地治疗炎症。在此,通过 GC-MS 对苦橙叶提取物 ( Citrus aurantium )的精油进行了表征,其中乙酸芳樟酯是最主要的化合物,使用柱色谱法分离并通过 NMR 分析进行鉴定。对角叉菜胶诱导模型的体内炎症抑制活性及中枢镇痛作用以及乙酸芳樟酯的解热潜力在大鼠中进行了评估。与对照药物和参考药物相比,乙酸芳樟酯(100 和 200 mg/kg)的给药在大鼠爪水肿模型中以剂量依赖性方式表现出显着的快速起效而非长期持续的抗炎作用。通过降低丙二醛 (MDA) 水平和恢复谷胱甘肽来改善爪子的抗氧化状态,可以显着减少炎症(GSH) 水平以及爪组织中促炎细胞因子水平 (TNF-α)、IL-1b、前列腺素 E2 (PGE2) 和 COX-2 的减弱。尽管口服醋酸芳樟酯(100 和 200 mg/kg)的镇痛作用微乎其微,但对大鼠却具有强效、持久的解热活性。较高剂量的乙酸芳樟酯(200 mg/kg)显示出比参考药物更好的快速起效抗炎活性。此外,乙酸芳樟酯(200 mg/kg)具有最好的解热活性。这些发现揭示了乙酸芳樟酯在治疗多种炎症和高热疾病方面的有前景的药用用途,这些疾病可能归因于其活性成分。

更新日期:2023-07-20
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