2. Academic Validation
  3. Licochalcone B specifically inhibits the NLRP3 inflammasome by disrupting NEK7-NLRP3 interaction

Licochalcone B specifically inhibits the NLRP3 inflammasome by disrupting NEK7-NLRP3 interaction

  • EMBO Rep. 2022 Feb 3;23(2):e53499. doi: 10.15252/embr.202153499.
Qiang Li  # 1 2 3,  Hui Feng  # 4,  Hongbo Wang  # 2,  Yinghao Wang  # 1,  Wenqing Mou 3,  Guang Xu 2 3,  Ping Zhang 2 3,  Ruisheng Li 5,  Wei Shi 3,  Zhilei Wang 3,  Zhie Fang 3,  Lutong Ren 3,  Yan Wang 3,  Li Lin 3,  Xiaorong Hou 3,  Wenzhang Dai 3,  Zhiyong Li 3,  Ziying Wei 3,  Tingting Liu 3,  Jiabo Wang 3,  Yuming Guo 2 3,  Pengyan Li 2 3,  Xu Zhao 2 3,  Xiaoyan Zhan 2 3,  Xiaohe Xiao 1 2 3,  Zhaofang Bai 2 3
Affiliations

Affiliations

  • 1 School of Pharmacy, Fujian University of Traditional Chinese Medicine, Fuzhou, China.
  • 2 Department of Hepatology, Fifth Medical Center of Chinese PLA General Hospital, Beijing, China.
  • 3 China Military Institute of Chinese Materia, Fifth Medical Center of Chinese PLA General Hospital, Beijing, China.
  • 4 Department of Ultrasound, Fifth Medical Center of Chinese PLA General Hospital, Beijing, China.
  • 5 Research Center for Clinical and Translational Medicine, Fifth Medical Center of Chinese PLA General Hospital, Beijing, China.
  • # Contributed equally.
PMID: 34882936 DOI: 10.15252/embr.202153499
Abstract

The activation of the nucleotide oligomerization domain (NOD)-like receptor (NLR) family, pyrin domain-containing protein 3 (NLRP3) inflammasome is related to the pathogenesis of a wide range of inflammatory diseases, but drugs targeting the NLRP3 inflammasome are still scarce. In the present study, we demonstrated that Licochalcone B (LicoB), a main component of the traditional medicinal herb licorice, is a specific inhibitor of the NLRP3 inflammasome. LicoB inhibits the activation of the NLRP3 inflammasome in macrophages but has no effect on the activation of AIM2 or NLRC4 inflammasome. Mechanistically, LicoB directly binds to NEK7 and inhibits the interaction between NLRP3 and NEK7, thus suppressing NLRP3 inflammasome activation. Furthermore, LicoB exhibits protective effects in mouse models of NLRP3 inflammasome-mediated diseases, including lipopolysaccharide (LPS)-induced septic shock, MSU-induced peritonitis and non-alcoholic steatohepatitis (NASH). Our findings indicate that LicoB is a specific NLRP3 Inhibitor and a promising candidate for treating NLRP3 inflammasome-related diseases.

Keywords

LPS-induced septic shock; Licochalcone B; MSU-induced peritonitis; NASH; NEK7; NLRP3 inflammasome.

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