Article

Flavokawain B alleviates LPS-induced acute lung injury via targeting myeloid differentiation factor 2

Wu Luo1,2, Li-bin Yang1, Chen-chen Qian1, Bao Ma1, Gloria M. Manjengwa1, Xiao-min Miao1, Jie Wang1, Cheng-hong Hu1, Bo Jin1, Ling-xi Zhang1, Chao Zheng3, Guang Liang1,4,5, Yi Wang1
1 Chemical Biology Research Center, School of Pharmaceutical Sciences, Wenzhou Medical University, Wenzhou 325035, China
2 Medical Research Center, the First Affiliated Hospital of Wenzhou Medical University, Wenzhou 325000, China
3 Department of Endocrinology, the Second Affiliated Hospital of Zhejiang University, Hangzhou 310009, China
4 School of Pharmaceutical Sciences, Hangzhou Medical College, Hangzhou 311399, China
5 enzhou Institute, University of Chinese Academy of Sciences, Wenzhou 325001, China
Correspondence to: Yi Wang: yi.wang1122@wmu.edu.cn,
DOI: 10.1038/s41401-021-00792-4
Received: 24 June 2021
Accepted: 8 October 2021
Advance online: 4 November 2021

Abstract

Acute lung injury (ALI) is a sudden onset systemic inflammatory response. ALI causes severe morbidity and death and currently no effective pharmacological therapies exist. Natural products represent an excellent resource for discovering new drugs. Screening anti-inflammatory compounds from the natural product bank may offer viable candidates for molecular-based therapies for ALI. In this study, 165 natural compounds were screened for anti-inflammatory activity in lipopolysaccharide (LPS)-challenged macrophages. Among the screened compounds, flavokawain B (FKB) significantly reduced LPS-induced pro-inflammatory IL-6 secretion in macrophages. FKB also reduced the formation of LPS/TLR4/MD2 complex by competitively binding to MD2, suppressing downstream MAPK and NF-κB signaling activation. Finally, FKB treatment of mice reduced LPS-induced lung injury, systemic and local inflammatory cytokine production, and macrophage infiltration in lungs. These protective activities manifested as increased survival in the ALI model, and reduced mortality upon bacterial infection. In summary, we demonstrate that the natural product FKB protects against LPS-induced lung injury and sepsis by interacting with MD2 and inhibiting inflammatory responses. FKB may potentially serve as a therapeutic option for the treatment of ALI.
Keywords: acute lung injury; inflammation; flavokawain B; MD2; sepsis

Article Options

Download Citation

Cited times in Scopus