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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Main Authors: 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
Format: Article
Language:English
Published: MDPI AG 2022-09-01
Series:Metabolites
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Online Access:https://www.mdpi.com/2218-1989/12/10/916
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Summary: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.
ISSN:2218-1989