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Imeglimin attenuates NLRP3 inflammasome activation by restoring mitochondrial functions in macrophages

Authors
Lee, JY | Kang, Y | Jeon, JY  | Kim, HJ  | Kim, DJ  | Lee, KW  | Han, SJ
Citation
Journal of pharmacological sciences, 155(2). : 35-43, 2024
Journal Title
Journal of pharmacological sciences
ISSN
1347-86131347-8648
Abstract
Imeglimin is a novel oral antidiabetic drug for treating type 2 diabetes. However, the effect of imeglimin on NLRP3 inflammasome activation has not been investigated yet. Here, we aimed to investigate whether imeglimin reduces LPS-induced NLRP3 inflammasome activation in THP-1 macrophages and examine the associated underlying mechanisms. We analyzed the mRNA and protein expression levels of NLRP3 inflammasome components and IL-1β secretion. Additionally, reactive oxygen species (ROS) generation, mitochondrial membrane potential, and mitochondrial permeability transition pore (mPTP) opening were measured by flow cytometry. Imeglimin inhibited NLRP3 inflammasome-mediated IL-1β production in LPS-stimulated THP-1-derived macrophages. In addition, imeglimin reduced LPS-induced mitochondrial ROS production and mitogen-activated protein kinase phosphorylation. Furthermore, imeglimin restored the mitochondrial function by modulating mitochondrial membrane depolarization and mPTP opening. We demonstrated for the first time that imeglimin reduces LPS-induced NLRP3 inflammasome activation by inhibiting mPTP opening in THP-1 macrophages. These results suggest that imeglimin could be a promising new anti-inflammatory agent for treating diabetic complications.
Keywords

MeSH

DOI
10.1016/j.jphs.2024.03.004
PMID
38677784
Appears in Collections:
Journal Papers > School of Medicine / Graduate School of Medicine > Endocrinology & Metabolism
Ajou Authors
김, 대중  |  김, 혜진  |  이, 관우  |  전, 자영  |  한, 승진
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