ReferenceID 2646

Piperlongumine Is an NLRP3 Inhibitor With Anti-inflammatory Activity

Front Pharmacol

Piperlongumine (PL) is an alkaloid from Piper longum L. with anti-inflammatory and antitumor properties. Numerous studies have focused on its antitumor effect. However, the underlying mechanisms of its anti-inflammation

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Reference Id
2646
Evidence Id
19236
Core Evidence Id
19236
Source Reference Id
5297
Herb2 Reference Id
HBREF006094
Subject Paper Key
HBIN040107_35095532
Pubmed Id
35095532
Doi
10.3389/fphar.2021.818326
Paper Title
Piperlongumine Is an NLRP3 Inhibitor With Anti-inflammatory Activity
Paper Abstract
Piperlongumine (PL) is an alkaloid from Piper longum L. with anti-inflammatory and antitumor properties. Numerous studies have focused on its antitumor effect. However, the underlying mechanisms of its anti-inflammation remain elusive. In this study, we have found that PL is a natural inhibitor of Nod-like receptor family pyrin domain-containing protein-3 (NLRP3) inflammasome, an intracellular multi-protein complex that orchestrates host immune responses to infections or sterile inflammations. PL blocks NLRP3 activity by disrupting the assembly of NLRP3 inflammasome including the association between NLRP3 and NEK7 and subsequent NLRP3 oligomerization. Furthermore, PL suppressed lipopolysaccharide-induced endotoxemia and MSU-induced peritonitis in vivo, which are NLRP3-dependent inflammation. Thus, our study identified PL as an inhibitor of NLRP3 inflammasome and indicated the potential application of PL in NLRP3-relevant diseases.
Journal
Front Pharmacol
Publish Year
2022
Experiment Subject
Experiment Type
Cell Experiment
Phenotype Related
Piperlongumine; Peritonitis; Sterile Inflammations
Paper Title Cn
Paper Title En
Piperlongumine Is an NLRP3 Inhibitor With Anti-inflammatory Activity
Bilingual Status
semi_complete