Vanillosmopsis arborea Baker（菊科）精油与β-环糊精复合物对口颌面镇痛活性的分子机制。
Molecular mechanism underlying orofacial antinociceptive activity of Vanillosmopsis arborea Baker (Asteraceae) essential oil complexed with β-cyclodextrin.
机构信息
Experimental Biology Center, University of Fortaleza, Fortaleza, Ceará, Brazil; Institute of Educators Training, Federal University of Cariri, Brejo Santo, Ceará, Brazil.
Experimental Biology Center, University of Fortaleza, Fortaleza, Ceará, Brazil.
出版信息
Phytomedicine. 2019 Mar 1;55:293-301. doi: 10.1016/j.phymed.2018.09.173. Epub 2018 Sep 17.
BACKGROUND
Vanillosmopsis arborea Baker has recognized economic value owing to the high content of (-)-α-bisabolol (BISA) in the essential oil of its stem (EOVA). The antinociceptive effect of EVOA has already been demonstrated, and β-cyclodextrin (βCD) is known to improve the analgesic effect of various substances.
PURPOSE
Thus, we aimed to evaluate the orofacial antinociceptive effect of a complex containing EOVA-βCD in rodents.
METHODS
EOVA was obtained by simple hydrodistillation, and the essential oil was complexed with βCD. The animals (n = 6/group) were treated orally with EOVA-βCD (10 or 50 mg/kg), or vehicle (control), and subjected to cutaneous orofacial nociception (formalin, capsaicin, acidic saline or glutamate), corneal (hypertonic saline) or temporomandibular (formalin) tests. The expression of FOS protein was analyzed in the spinal cord. Molecular docking was performed using the 5-HT and M receptors and BISA.
RESULTS
The oral administration of EOVA-βCD reduced nociceptive behaviour. Moreover, EOVA-βCD decreased FOS expression. The molecular docking study indicates that BISA interacts with 5-HT3 and M2 receptors, indicating the potential mechanism of action of the tested compound.
CONCLUSIONS
Our results indicate that EOVA-βCD possesses orofacial antinociceptive effect, indicating that this complex can be used in analgesic drug development.
背景
Vanillosmopsis arborea Baker 因其茎精油（EOVA）中高含量的 (-)-α- 倍半水芹醇（BISA）而具有经济价值。EOVA 已被证明具有抗伤害感受作用，并且 β-环糊精（βCD）已知可以提高各种物质的镇痛作用。
目的
因此，我们旨在评估含有 EOVA-βCD 的复合物在啮齿动物中的口腔镇痛作用。
方法
EOVA 通过简单的水蒸馏法获得，精油与 βCD 络合。将动物（n=6/组）口服给予 EOVA-βCD（10 或 50mg/kg）或载体（对照），并进行皮肤口腔伤害感受（福尔马林、辣椒素、酸性盐水或谷氨酸）、角膜（高渗盐水）或颞下颌（福尔马林）测试。分析脊髓中 FOS 蛋白的表达。使用 5-HT 和 M 受体和 BISA 进行分子对接。
结果
口服 EOVA-βCD 可减轻伤害感受行为。此外，EOVA-βCD 减少了 FOS 表达。分子对接研究表明，BISA 与 5-HT3 和 M2 受体相互作用，表明了测试化合物的潜在作用机制。
结论
我们的结果表明 EOVA-βCD 具有口腔镇痛作用，表明该复合物可用于开发镇痛药物。
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