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α-松油醇,一种单萜醇,与β-环糊精络合后,通过对接研究辅助纤维肌痛动物模型发挥抗痛觉过敏作用。

α-Terpineol, a monoterpene alcohol, complexed with β-cyclodextrin exerts antihyperalgesic effect in animal model for fibromyalgia aided with docking study.

机构信息

Department of Physiology, Federal University of Sergipe, Av. Tancredo Neves, S/N, Rosa Elza, São Cristóvão, Sergipe, CEP 49.000-100, Brazil.

Department of Pharmacy, Federal University of Sergipe, Av. Tancredo Neves, S/N, Rosa Elza, São Cristóvão, Sergipe, CEP 49.100-000, Brazil.

出版信息

Chem Biol Interact. 2016 Jul 25;254:54-62. doi: 10.1016/j.cbi.2016.05.029. Epub 2016 May 23.

Abstract

The anti-hyperalgesic effect of the complex containing α-terpineol (αTPN) and β-cyclodextrin (βCD) was analyzed in a non-inflammatory chronic muscle pain model, as well as its mechanism of action through docking study for a possible interaction with receptors. The αTPN-βCD complex was prepared and characterized through the thermogravimetry/derivate thermogravimetry (TG/DTG), Fourier transform infrared spectroscopy (FTIR) and scanning electron microscope (SEM). The model of chronic muscle pain was induced by two injections of pH 4.0 saline (20 μl) into the left gastrocnemius 5 days apart. After confirming hyperalgesia, male mice were treated with αTPN-βCD (25, 50 or 100 mg/kg; p.o.) or vehicle (saline 0.9%, p.o.) daily for 10 days. 1 h after the mechanical hyperalgesia, motor performance was evaluated. In addition, the systemic administration of naloxone and ondansetron tested the analgesic effect on the active opioid and serotonin receptors, respectively. The characterization tests indicated that αTPN was efficiently incorporated into βCD. The oral treatment with αTPN-βCD, at all doses tested, produced a significant (p < 0.001) decrease in the mechanical hyperalgesia, without causing any alteration in the force and in motor performance. This analgesic effect was reversed by the systemic administration of naloxone or ondansetron. These findings are corroborated by the docking study described in the present study, which verified a possible interaction of αTPN-βCD with opioid (MU, Kappa, Delta) and 5-HT receptors. Thus, it can be concluded that αTPN-βCD reduced the hyperalgesia followed by the chronic muscle pain model, probably evoked by the descending inhibitory pain system, specifically by opioid and serotoninergic receptors.

摘要

含有α-松油醇(αTPN)和β-环糊精(βCD)的复合物的抗痛觉过敏作用在非炎症性慢性肌肉疼痛模型中进行了分析,并通过对接研究分析了其作用机制,以研究其与受体的可能相互作用。通过热重/导数热重(TG / DTG)、傅里叶变换红外光谱(FTIR)和扫描电子显微镜(SEM)对αTPN-βCD 复合物进行了制备和表征。通过在 5 天内将 pH 4.0 盐水(20 μl)两次注射到左腓肠肌中诱导慢性肌肉疼痛模型。在确认痛觉过敏后,雄性小鼠每天用αTPN-βCD(25、50 或 100 mg/kg;po)或载体(生理盐水 0.9%,po)治疗 10 天。在机械性痛觉过敏后 1 小时,评估运动性能。此外,全身性给予纳洛酮和昂丹司琼分别测试了对活性阿片和 5-羟色胺受体的镇痛作用。特征测试表明,αTPN 被有效地掺入到βCD 中。在所有测试剂量下,口服给予αTPN-βCD 都会显著(p <0.001)降低机械性痛觉过敏,而不会引起力和运动性能的任何改变。这种镇痛作用被纳洛酮或昂丹司琼的全身给药逆转。本研究中描述的对接研究证实了 αTPN-βCD 与阿片(MU、Kappa、Delta)和 5-HT 受体可能存在相互作用。因此,可以得出结论,αTPN-βCD 减轻了慢性肌肉疼痛模型后的痛觉过敏,可能是由下行抑制性疼痛系统引起的,特别是由阿片类和 5-羟色胺能受体引起的。

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