Lin Kaiwen, Fu Datian, Wang Zhongtao, Zhang Xueer, Zhu Canyang
Hainan Women and Children's Medical Center, Haikou, China.
Korean J Pain. 2024 Apr 1;37(2):151-163. doi: 10.3344/kjp.23363.
Galangin, commonly employed in traditional Chinese medicine for its diverse medicinal properties, exhibits potential in treating inflammatory pain. Nevertheless, its mechanism of action remains unclear.
Mice were randomly divided into 4 groups for 7 days: a normal control group, a galangin-treated (25 and 50 mg/kg), and a positive control celecoxib (20 mg/kg). Analgesic and anti-inflammatory effects were evaluated using a hot plate test, acetic acid-induced writhing test, acetic acid-induced vascular permeability test, formalininduced paw licking test, and carrageenan-induced paw swelling test. The interplay between galangin, transient receptor potential vanilloid 1 (TRPV1), NF-κB, COX-2, and TNF-α proteins was evaluated via molecular docking. COX- 2, PGE2, IL-1β, IL-6, and TNF-α levels in serum were measured using ELISA after capsaicin administration (200 nmol/L). TRPV1 expression in the dorsal root ganglion was analyzed by Western blot. The quantities of substance P (SP) and calcitonin gene-related peptide (CGRP) were assessed using qPCR.
Galangin reduced hot plate-induced licking latency, acetic acid-induced contortions, carrageenantriggered foot inflammation, and capillary permeability in mice. It exhibited favorable affinity towards TRPV1, NF- κB, COX-2, and TNF-α, resulting in decreased levels of COX-2, PGE2, IL-1β, IL-6, and TNF-α in serum following capsaicin stimulation. Galangin effectively suppressed the upregulation of TRPV1 protein and associated receptor neuropeptides CGRP and SP mRNA, while concurrently inhibiting the expression of NF-κB, TNF-α, COX-2, and PGE2 mRNA.
Galangin exerts its anti-inflammatory pain effects by inhibiting TRPV1 activation and regulating COX-2, NF-κB/TNF-α expression, providing evidence for the use of galangin in the management of inflammatory pain.
高良姜素常用于传统中药，具有多种药用特性，在治疗炎性疼痛方面具有潜力。然而，其作用机制尚不清楚。
将小鼠随机分为4组，持续7天：正常对照组、高良姜素治疗组（25和50mg/kg）以及阳性对照塞来昔布组（20mg/kg）。使用热板试验、醋酸诱导扭体试验、醋酸诱导血管通透性试验、福尔马林诱导舔足试验和角叉菜胶诱导足肿胀试验评估镇痛和抗炎作用。通过分子对接评估高良姜素、瞬时受体电位香草酸受体1（TRPV1）、核因子κB（NF-κB）、环氧化酶-2（COX-2）和肿瘤坏死因子-α（TNF-α）蛋白之间的相互作用。给予辣椒素（200nmol/L）后，采用酶联免疫吸附测定法（ELISA）测量血清中COX-2、前列腺素E2（PGE2）、白细胞介素-1β（IL-1β）、白细胞介素-6（IL-6）和TNF-α的水平。通过蛋白质免疫印迹法分析背根神经节中TRPV1的表达。使用实时定量聚合酶链反应（qPCR）评估P物质（SP）和降钙素基因相关肽（CGRP）的量。
高良姜素可缩短热板诱导的舔足潜伏期、减少醋酸诱导的扭体次数、减轻角叉菜胶引发的足部炎症以及降低小鼠毛细血管通透性。它对TRPV1、NF-κB、COX-2和TNF-α表现出良好的亲和力，导致辣椒素刺激后血清中COX-2、PGE2、IL-1β、IL-6和TNF-α水平降低。高良姜素有效抑制TRPV1蛋白上调以及相关受体神经肽CGRP和SP mRNA，同时抑制NF-κB、TNF-α、COX-2和PGE2 mRNA的表达。
高良姜素通过抑制TRPV1激活并调节COX-2、NF-κB/TNF-α表达发挥抗炎性疼痛作用，为高良姜素用于炎性疼痛管理提供了依据。
