Arabic Arabic English English French French German German

Oridonin is a covalent NLRP3 inhibitor with strong anti-inflammasome activity.


Nat Commun. 2018 06 29 ;9(1):2550. Epub 2018 Jun 29. PMID: 29959312

Abstract Title: 

Oridonin is a covalent NLRP3 inhibitor with strong anti-inflammasome activity.


Oridonin (Ori) is the major active ingredient of the traditional Chinese medicinal herb Rabdosia rubescens and has anti-inflammatory activity, but the target of Ori remains unknown. NLRP3 is a central component of NLRP3 inflammasome and has been involved in a wide variety of chronic inflammation-driven human diseases. Here, we show that Ori is a specific and covalent inhibitor for NLRP3 inflammasome. Ori forms a covalent bond with the cysteine 279 of NLRP3 in NACHT domain to block the interaction between NLRP3 and NEK7, thereby inhibiting NLRP3 inflammasome assembly and activation. Importantly, Ori has both preventive or therapeutic effects on mouse models of peritonitis, gouty arthritis and type 2 diabetes, via inhibition of NLRP3 activation. Our results thus identify NLRP3 as the direct target of Ori for mediating Ori’s anti-inflammatory activity. Ori could serve as a lead for developing new therapeutics against NLRP3-driven diseases.

read more

Read More

Leave a Reply

Your email address will not be published. Required fields are marked *

Previous Post

Oridonin inhibits VEGF-A-associated angiogenesis and epithelial-mesenchymal transition of breast cancer.

Next Post

Oridonin enhances the cytotoxicity of 5-FU in renal carcinoma cells by inducting necroptotic death.

Related Posts