Transient receptor potential vanilloid 1 involved in the analgesic effects of total flavonoids extracted from Longxuejie ().

Journal of traditional Chinese medicine = Chung i tsa chih ying wen pan Pub Date : 2024-06-01 DOI:10.19852/j.cnki.jtcm.20240423.004

M O Xiaoqiang, Chen Yating, Yin Qian, Chen Haibo, Ban Qiang, L I Jun, Chen Su, Yao Jinguang

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Abstract

Objective: To evaluate the analgesic effects of total flavonoids of Longxuejie (Resina Dracaenae Cochinchinensis) (TFDB) and explore the possible analgesic mechanism associated with transient receptor potential vanilloid 1 (TRPV1).

Methods: Whole-cell patch clamp technique was used to observe the effects of TFDB on capsaicin-induced TRPV1 currents. Rat experiments in vivo were used to observe the analgesic effects of TFDB. Western blot and immunofluorescence experiments were used to test the change of TRPV1 expression in DRG neurons induced by TFDB.

Results: Results showed that TFDB inhibited capsaicin-induced TRPV1 receptor currents in acutely isolated dorsal root ganglion (DRG) neurons of rats and the half inhibitory concentration was (16.7 ± 1.6) mg/L. TFDB (2-20 mg/kg) showed analgesic activity in the phase Ⅱ of formalin test and (0.02-2 mg per paw) reduced capsaicin-induced licking times of rats. TFDB (20 mg/kg) was fully efficacious on complete Freund's adjuvant (CFA)-induced inflammatory thermal hyperalgesia and capsaicin could weaken the analgesic effects. The level of TRPV1 expressions of DRG neurons was also decreased in TFDB-treated CFA-inflammatory pain rats.

Conclusion: All these results indicated that the analgesic effect of TFDB may contribute to their modulations on both function and expression of TRPV1 channels in DRG neurons.

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瞬时受体电位类香草素 1 参与了从龙血树（）中提取的总黄酮的镇痛作用。

目的评估龙血树总黄酮（TFDB）的镇痛作用，并探讨与瞬态受体电位类香草素1（TRPV1）相关的可能镇痛机制：方法：采用全细胞膜片钳技术观察 TFDB 对辣椒素诱导的 TRPV1 电流的影响。大鼠体内实验用于观察 TFDB 的镇痛作用。用 Western 印迹和免疫荧光实验检测 TFDB 诱导的 DRG 神经元中 TRPV1 表达的变化：结果表明，TFDB 可抑制辣椒素诱导的大鼠急性离体背根神经节（DRG）神经元 TRPV1 受体电流，半抑制浓度为（16.7 ± 1.6）mg/L。TFDB（2-20 毫克/千克）在福尔马林试验Ⅱ期显示出镇痛活性，（每只爪 0.02-2 毫克）可减少辣椒素诱导的大鼠舔舐时间。TFDB（20 毫克/千克）对完全弗氏佐剂（CFA）诱导的炎性热痛完全有效，而辣椒素会削弱其镇痛作用。TFDB处理的CFA炎性痛大鼠DRG神经元的TRPV1表达水平也有所下降：所有这些结果表明，TFDB 的镇痛作用可能是其对 DRG 神经元中 TRPV1 通道的功能和表达的调节作用。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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Journal of traditional Chinese medicine = Chung i tsa chih ying wen pan

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