The First College of Clinical Medicine, Nanjing University of Chinese Medicine, Nanjing 210029, PR China.
School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210029, PR China.
Int Immunopharmacol. 2021 Nov;100:108107. doi: 10.1016/j.intimp.2021.108107. Epub 2021 Sep 3.
Activation of NACHT, LRR, and PYD domains-containing protein 3 (NLRP3) inflammasome plays a crucial role in the inflammatory responses of monosodium urate (MSU) crystal-induced gouty arthritis. Therefore, the molecular basis of NLRP3 inflammasome is very valuable in developing potential therapeutic drugs for gout. Tetrahydropalmatine (THP), the main active component of the traditional Chinese medicinal herb Corydalis yanhusuo, has shown prominent anti-inflammatory and analgesic activities, but to date, these effects have not been investigated exhaustively on gout. This study indicated that THP attenuated pain and swelling in an MSU-induced acute gout model by decreasing pro-inflammatory cytokine production and inflammatory cell infiltration. THP exerted its actions by suppressing NLRP3 inflammasome activation and subsequent formation of caspase-1. Furthermore, results showed that THP alleviated MSU-induced reactive oxygen species (ROS) generation, upstream of NLRP3 inflammasome activation, by an increase in the activities of antioxidant enzymes both in vitro and in vivo. In conclusion, our study suggests that THP suppressed ROS-mediated NLRP3 inflammasome activation in MSU-induced inflammatory responses, which highlights its therapeutic potential in gouty arthritis.
NACHT、LRR 和 PYD 结构域包含蛋白 3(NLRP3)炎症小体的激活在单钠尿酸盐(MSU)晶体诱导的痛风性关节炎的炎症反应中起着至关重要的作用。因此,NLRP3 炎症小体的分子基础对于开发痛风的潜在治疗药物非常有价值。延胡索乙素(THP)是传统中药延胡索的主要活性成分,具有显著的抗炎和镇痛作用,但迄今为止,这些作用尚未在痛风中进行详尽研究。本研究表明,THP 通过降低促炎细胞因子的产生和炎症细胞的浸润来减轻 MSU 诱导的急性痛风模型中的疼痛和肿胀。THP 通过抑制 NLRP3 炎症小体的激活及其随后的半胱天冬酶-1 的形成来发挥作用。此外,结果表明,THP 通过增加抗氧化酶的活性,在体内和体外减轻了 MSU 诱导的活性氧(ROS)的产生,ROS 的产生是 NLRP3 炎症小体激活的上游。总之,我们的研究表明,THP 抑制了 MSU 诱导的炎症反应中 ROS 介导的 NLRP3 炎症小体的激活,这突出了其在痛风性关节炎中的治疗潜力。