2. Academic Validation
  3. Synthesis and evaluation of lansiumamide B analogues to ameliorate acute lung injury by reducing oxidative stress and inflammation via Keap1/Nrf2/NF-κB pathway

Synthesis and evaluation of lansiumamide B analogues to ameliorate acute lung injury by reducing oxidative stress and inflammation via Keap1/Nrf2/NF-κB pathway

  • Eur J Med Chem. 2025 Dec 5:299:118052. doi: 10.1016/j.ejmech.2025.118052.
Liyan Song 1,  Mengjie Li 2,  Jiayu Li 3,  Lifang Liu 1,  Xingya Luo 3,  Jun Wang 3,  Xuan Wu 3,  Binbin Huang 1,  Guoping Zhang 3,  Hongliang Yao 4
Affiliations

Affiliations

  • 1 Key BioAI Synthetica Lab for Natural Product Drug Discovery, College of Bee Science and Biomedicine, Fujian Agriculture and Forestry University, Fuzhou, Fujian, China; Key Laboratory of Biopesticide and Chemical Biology, Ministry of Education, Fujian Agriculture and Forestry University, Fuzhou, Fujian, China.
  • 2 Guilin Municipal Hospital of Traditional Chinese Medicine, Guangxi Zhuang Autonomous Region, Guilin, Guangxi, China; Guangdong Key Laboratory of Animal Conservation and Resource Utilization, Guangdong Public Laboratory of Wild Animal Conservation and Utilization, Institute of Zoology, Guangdong Academy of Sciences, Guangzhou, Guangdong, China.
  • 3 Guangdong Key Laboratory of Animal Conservation and Resource Utilization, Guangdong Public Laboratory of Wild Animal Conservation and Utilization, Institute of Zoology, Guangdong Academy of Sciences, Guangzhou, Guangdong, China.
  • 4 Guangdong Key Laboratory of Animal Conservation and Resource Utilization, Guangdong Public Laboratory of Wild Animal Conservation and Utilization, Institute of Zoology, Guangdong Academy of Sciences, Guangzhou, Guangdong, China. Electronic address: yaohl@giz.gd.cn.
PMID: 40812070 DOI: 10.1016/j.ejmech.2025.118052
Abstract

Acute lung injury (ALI), occurring with oxidative stress and inflammation, is a life-threatening disease, characterized by significant morbidity and mortality rates. There is a deep need to develop novel drugs. In this work we synthesized 46 novel lansiumamide B analogues with newly developed transition-metal-free strategy. Upon investigation, M11 exhibited highest inhibition rate of inflammatory cytokines and ROS release in LPS-induced Raw264.7 cells with good dose dependent manner and safety. In addition, M11 alleviated ALI induced lung injury and oxidative stress, and inhibited Collagen formation and polarization of M1 macrophages. Reverse virtual screening and transcriptomics analysis suggested that M11 might target Keap1/Nrf2 signaling pathway. Further study demonstrated that M11 promoted Nrf2 nuclear translocation and the protein of downstream HO-1. Besides, M11 suppressed phosphorylation NF-κB. Overall, M11 could be an effective anti-oxidative stress and inflammation agent for ALI.

Keywords

Acute lung injury; Anti-inflammation; Lansiummaide B analogues; Oxidative stress.

Figures
Products
嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z