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Quercetin, Main Active Ingredient of Moutan Cortex, Alleviates Chronic Orofacial Pain via Block of Voltage-Gated Sodium Channel

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AUTHORS: Liu, Zhanli MD et al 

Anesthesia & Analgesia November 17, 2023.

BACKGROUND:

Chronic orofacial pain (COP) therapy is challenging, as current medical treatments are extremely lacking. Moutan Cortex (MC) is a traditional Chinese medicine herb widely used for chronic inflammatory diseases. However, the mechanism behind MC in COP therapy has not been well-established. The purpose of this study was to identify the active ingredients of MC and their specific underlying mechanisms in COP treatment.

METHODS:

In this study, the main active ingredients and compound-target network of MC in COP therapy were identified through network pharmacology and bioinformatics analysis. Adult male Sprague-Dawley rats received oral mucosa lipopolysaccharide (LPS) injection to induce COP. Pain behaviors were evaluated by orofacial mechanical nociceptive assessment after intraganglionar injection. In vitro inflammatory cytokines in LPS-pretreated human periodontal ligament stem cells (hPDLSCs) and rat primary cultural trigeminal ganglion (TG) neurons were quantified by real-time quantitative polymerase chain reaction (RT-qPCR). Schrödinger software was used to verify the molecular docking of quercetin and critical targets. Whole-cell recording electrophysiology was used to evaluate the effect of quercetin on voltage-gated sodium (Nav) channel in rat TG neurons.

RESULTS:

The assembled compound-target network consisted of 4 compounds and 46 targets. As 1 of the active components of MC correlated with most related targets, quercetin alleviated mechanical allodynia in LPS-induced rat model of COP (mechanical allodynia threshold median [interquartile range (IQR) 0.5 hours after drug administration: vehicle 1.3 [0.6–2.0] g vs quercetin 7.0 [6.0–8.5] g, P = .002). Gene ontology (GO) enrichment and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway analysis revealed that immune response and membrane functions play essential roles in MC-COP therapy. Five of the related targets were identified as core targets by protein-protein interaction analysis. Quercetin exerted an analgesic effect, possibly through blocking Nav channel in TG sensory neurons (peak current density median [IQR]: LPS −850.2 [−983.6 to −660.7] mV vs LPS + quercetin −589.6 [−711.0 to −147.8] mV, P = .006) while downregulating the expression level of proinflammatory cytokines-FOS (normalized messenger RNA [mRNA] level mean ± standard error of mean [SEM]: LPS [2. 22 ± 0.33] vs LPS + quercetin [1. 33 ± 0.14], P = .034) and TNF-α (normalized mRNA level mean ± SEM: LPS [8. 93 ± 0.78] vs LPS + quercetin [3. 77 ± 0.49], P < .0001).

CONCLUSIONS:

Identifying Nav as the molecular target of quercetin clarifies the analgesic mechanism of MC, and provides ideas for the development of novel selective and efficient chronic pain relievers.

KEY POINTS

  • Question: What is the efficacy and underlying mechanism of Moutan Cortex and its active ingredients on chronic orofacial pain therapy?
  • Findings: As 1 of the active components of Moutan Cortex, quercetin effectively alleviated chronic orofacial pain through blocking voltage-gated sodium channel (Nav) channel in trigeminal ganglion sensory neurons, while downregulating the expression level of proinflammatory cytokines-FOS and TNF-α.
  • Meaning: Identifying Nav as the molecular target of quercetin clarifies the analgesic mechanism of Moutan Cortex, and provides ideas for the development of novel selective and efficient chronic pain relievers.

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