Pharmacological Interaction of Quercetin Derivatives of <i>Tilia americana</i> and Clinical Drugs in Experimental Fibromyalgia
Fibromyalgia (FM) is a pain syndrome characterized by chronic widespread pain and CNS comorbidities. <i>Tilia americana</i> var. <i>mexicana</i> is a medicinal species used to treat anxiety, insomnia, and acute or chronic pain. However, its spectrum of analgesic efficacy for...
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MDPI AG
2022-09-01
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| Series: | Metabolites |
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| Online Access: | https://www.mdpi.com/2218-1989/12/10/916 |
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| author | Yara Elena Quinto-Ortiz María Eva González-Trujano Edith Sánchez-Jaramillo Gabriel Fernando Moreno-Pérez Salomón Jacinto-Gutiérrez Francisco Pellicer Alonso Fernández-Guasti Alberto Hernandez-Leon |
| author_facet | Yara Elena Quinto-Ortiz María Eva González-Trujano Edith Sánchez-Jaramillo Gabriel Fernando Moreno-Pérez Salomón Jacinto-Gutiérrez Francisco Pellicer Alonso Fernández-Guasti Alberto Hernandez-Leon |
| author_sort | Yara Elena Quinto-Ortiz |
| collection | DOAJ |
| description | Fibromyalgia (FM) is a pain syndrome characterized by chronic widespread pain and CNS comorbidities. <i>Tilia americana</i> var. <i>mexicana</i> is a medicinal species used to treat anxiety, insomnia, and acute or chronic pain. However, its spectrum of analgesic efficacy for dysfunctional pain is unknown. To investigate a possible therapeutic alternative for FM-type pain, an aqueous <i>Tilia</i> extract (TE) and its flavonoid fraction (FF) containing rutin and isoquercitrin were evaluated alone and/or combined with clinical drugs (tramadol—TRA and pramipexol—PRA) using the reserpine-induced FM model in rats. Chromatographic analysis allowed the characterization of flavonoids, while a histological analysis confirmed their presence in the brain. TE (10–100 mg/kg, i.p.) and FF (10–300 mg/kg, i.p.) produced significant and dose-dependent antihyperalgesic and antiallodynic effects equivalent to TRA (3–10 mg/kg, i.p.) or PRA (0.01–1 mg/kg, s.c.). Nevertheless, the combination of FF + TRA or FF + PRA resulted in an antagonistic interaction by possible competitive action on the serotonin transporter or µ-opioid and D<sub>2</sub> receptors, respectively, according to the <i>in silico</i> analysis. Flavonoids were identified in cerebral regions because of their self-epifluorescence. In conclusion, <i>Tilia</i> possesses potential properties to relieve FM-type pain. However, the consumption of this plant or flavonoids such as quercetin derivatives in combination with analgesic drugs might reduce their individual benefits. |
| first_indexed | 2024-03-09T19:49:26Z |
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| institution | Directory Open Access Journal |
| issn | 2218-1989 |
| language | English |
| last_indexed | 2024-03-09T19:49:26Z |
| publishDate | 2022-09-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Metabolites |
| spelling | doaj.art-9b84988ccda2442695f0fbae6720f38e2023-11-24T01:15:07ZengMDPI AGMetabolites2218-19892022-09-01121091610.3390/metabo12100916Pharmacological Interaction of Quercetin Derivatives of <i>Tilia americana</i> and Clinical Drugs in Experimental FibromyalgiaYara Elena Quinto-Ortiz0María Eva González-Trujano1Edith Sánchez-Jaramillo2Gabriel Fernando Moreno-Pérez3Salomón Jacinto-Gutiérrez4Francisco Pellicer5Alonso Fernández-Guasti6Alberto Hernandez-Leon7Laboratorio de Neurofarmacología de Productos Naturales, Dirección de Investigaciones en Neurociencias, Instituto Nacional de Psiquiatría Ramón de la Fuente Muñiz, Calz. México-Xochimilco 101, Col. San Lorenzo Huipulco, Tlalpan, Mexico City 14370, MexicoLaboratorio de Neurofarmacología de Productos Naturales, Dirección de Investigaciones en Neurociencias, Instituto Nacional de Psiquiatría Ramón de la Fuente Muñiz, Calz. México-Xochimilco 101, Col. San Lorenzo Huipulco, Tlalpan, Mexico City 14370, MexicoLaboratorio de Neuroendocrinología Molecular, Dirección de Investigaciones en Neurociencias, Instituto Nacional de Psiquiatría Ramón de la Fuente Muñiz, Calz. México-Xochimilco 101, Col. San Lorenzo Huipulco, Tlalpan, Mexico City 14370, MexicoLaboratorio de Neurofarmacología de Productos Naturales, Dirección de Investigaciones en Neurociencias, Instituto Nacional de Psiquiatría Ramón de la Fuente Muñiz, Calz. México-Xochimilco 101, Col. San Lorenzo Huipulco, Tlalpan, Mexico City 14370, MexicoLaboratorio de Neurofarmacología de Productos Naturales, Dirección de Investigaciones en Neurociencias, Instituto Nacional de Psiquiatría Ramón de la Fuente Muñiz, Calz. México-Xochimilco 101, Col. San Lorenzo Huipulco, Tlalpan, Mexico City 14370, MexicoLaboratorio de Neurofarmacología de Productos Naturales, Dirección de Investigaciones en Neurociencias, Instituto Nacional de Psiquiatría Ramón de la Fuente Muñiz, Calz. México-Xochimilco 101, Col. San Lorenzo Huipulco, Tlalpan, Mexico City 14370, MexicoLaboratorio de Farmacología Conductual, Departamento de Farmacobiología, Centro de Investigación y de Estudios Avanzados (CINVESTAV) Sede Sur, Calz. de los Tenorios 235, Col. Granjas Coapa, Tlalpan, Mexico City 14330, MexicoLaboratorio de Neurofarmacología de Productos Naturales, Dirección de Investigaciones en Neurociencias, Instituto Nacional de Psiquiatría Ramón de la Fuente Muñiz, Calz. México-Xochimilco 101, Col. San Lorenzo Huipulco, Tlalpan, Mexico City 14370, MexicoFibromyalgia (FM) is a pain syndrome characterized by chronic widespread pain and CNS comorbidities. <i>Tilia americana</i> var. <i>mexicana</i> is a medicinal species used to treat anxiety, insomnia, and acute or chronic pain. However, its spectrum of analgesic efficacy for dysfunctional pain is unknown. To investigate a possible therapeutic alternative for FM-type pain, an aqueous <i>Tilia</i> extract (TE) and its flavonoid fraction (FF) containing rutin and isoquercitrin were evaluated alone and/or combined with clinical drugs (tramadol—TRA and pramipexol—PRA) using the reserpine-induced FM model in rats. Chromatographic analysis allowed the characterization of flavonoids, while a histological analysis confirmed their presence in the brain. TE (10–100 mg/kg, i.p.) and FF (10–300 mg/kg, i.p.) produced significant and dose-dependent antihyperalgesic and antiallodynic effects equivalent to TRA (3–10 mg/kg, i.p.) or PRA (0.01–1 mg/kg, s.c.). Nevertheless, the combination of FF + TRA or FF + PRA resulted in an antagonistic interaction by possible competitive action on the serotonin transporter or µ-opioid and D<sub>2</sub> receptors, respectively, according to the <i>in silico</i> analysis. Flavonoids were identified in cerebral regions because of their self-epifluorescence. In conclusion, <i>Tilia</i> possesses potential properties to relieve FM-type pain. However, the consumption of this plant or flavonoids such as quercetin derivatives in combination with analgesic drugs might reduce their individual benefits.https://www.mdpi.com/2218-1989/12/10/916fibromyalgiaantinociceptionreserpine-induced myalgia<i>Tilia americana</i> var. <i>mexicana</i>flavonoids |
| spellingShingle | Yara Elena Quinto-Ortiz María Eva González-Trujano Edith Sánchez-Jaramillo Gabriel Fernando Moreno-Pérez Salomón Jacinto-Gutiérrez Francisco Pellicer Alonso Fernández-Guasti Alberto Hernandez-Leon Pharmacological Interaction of Quercetin Derivatives of <i>Tilia americana</i> and Clinical Drugs in Experimental Fibromyalgia Metabolites fibromyalgia antinociception reserpine-induced myalgia <i>Tilia americana</i> var. <i>mexicana</i> flavonoids |
| title | Pharmacological Interaction of Quercetin Derivatives of <i>Tilia americana</i> and Clinical Drugs in Experimental Fibromyalgia |
| title_full | Pharmacological Interaction of Quercetin Derivatives of <i>Tilia americana</i> and Clinical Drugs in Experimental Fibromyalgia |
| title_fullStr | Pharmacological Interaction of Quercetin Derivatives of <i>Tilia americana</i> and Clinical Drugs in Experimental Fibromyalgia |
| title_full_unstemmed | Pharmacological Interaction of Quercetin Derivatives of <i>Tilia americana</i> and Clinical Drugs in Experimental Fibromyalgia |
| title_short | Pharmacological Interaction of Quercetin Derivatives of <i>Tilia americana</i> and Clinical Drugs in Experimental Fibromyalgia |
| title_sort | pharmacological interaction of quercetin derivatives of i tilia americana i and clinical drugs in experimental fibromyalgia |
| topic | fibromyalgia antinociception reserpine-induced myalgia <i>Tilia americana</i> var. <i>mexicana</i> flavonoids |
| url | https://www.mdpi.com/2218-1989/12/10/916 |
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