α-Terpineol, a monoterpene alcohol, complexed with β-cyclodextrin exerts antihyperalgesic effect in animal model for fibromyalgia aided with docking study
| Autor: | Makson G. B. Oliveira, Heitor G. Araújo-Filho, Yasmim Maria Barbosa Gomes de Carvalho, Renan G. Brito, Parimelazhagan Thangaraj, Priscila L. Santos, Jullyana S.S. Quintans, Adriano Antunes de Souza Araújo, Jackson Roberto Guedes da Silva Almeida, Lucindo José Quintans-Júnior, Paula dos Passos Menezes, Juliane Cabral Silva, Saravanan Shanmugam, Luciana Scotti, Marcus Tullius Scotti, Mairim Russo Serafini |
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| Rok vydání: | 2016 |
| Předmět: |
Male
0301 basic medicine Fibromyalgia Receptors Opioid mu Cyclohexane Monoterpenes Pharmacology Toxicology Ondansetron Mice 03 medical and health sciences 0302 clinical medicine Receptors Opioid delta Cyclohexenes medicine Animals Receptor 5-HT receptor Analgesics Binding Sites Behavior Animal Naloxone Chemistry Receptors Opioid kappa beta-Cyclodextrins Chronic pain General Medicine medicine.disease Protein Structure Tertiary Molecular Docking Simulation Disease Models Animal 030104 developmental biology Opioid Mechanism of action Hyperalgesia Monoterpenes Systemic administration medicine.symptom 030217 neurology & neurosurgery medicine.drug |
| Zdroj: | Chemico-Biological Interactions. 254:54-62 |
| ISSN: | 0009-2797 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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