Spirodalesol, an NLRP3 Inflammasome Activation Inhibitor

Ai Hua Zhang; Wen Liu; Nan Jiang; Qiang Xu; Ren Xiang Tan

doi:10.1021/acs.orglett.6b03435

Spirodalesol, an NLRP3 Inflammasome Activation Inhibitor

Org Lett. 2016 Dec 16;18(24):6496-6499. doi: 10.1021/acs.orglett.6b03435. Epub 2016 Dec 7.

Authors

Ai Hua Zhang^{1

2}, Wen Liu¹, Nan Jiang³, Qiang Xu¹, Ren Xiang Tan^{1

4}

Affiliations

¹ Institute of Functional Biomolecules, State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University , Nanjing 210046, China.
² State Key Laboratory of Elemento-organic Chemistry, Nankai University , Tianjin 300071, China.
³ School of Pharmacy, Nanjing Medical University , Nanjing 210029, China.
⁴ School of Pharmacy, Nanjing University of Chinese Medicine , Nanjing 210023, China.

PMID: 27978645
DOI: 10.1021/acs.orglett.6b03435

Abstract

Autoimmune and inflammatory diseases are associated with inappropriate activation of the NOD-like receptor protein 3 (NLRP3) inflammasome, but suitable inhibitors against such improper activations remain scarce. Here, spirodalesol (1) from Daldinia eschscholzii was structurally characterized and is biosynthetically proposed as an NLRP3 inflammasome activation inhibitor with an unprecedented carbon skeleton.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Dose-Response Relationship, Drug
Inflammasomes / antagonists & inhibitors*
Inflammasomes / metabolism
Lipopolysaccharides / antagonists & inhibitors
Lipopolysaccharides / pharmacology
Macrophages / drug effects*
Macrophages / metabolism
Mice
Models, Molecular
Molecular Structure
NLR Family, Pyrin Domain-Containing 3 Protein / antagonists & inhibitors*
NLR Family, Pyrin Domain-Containing 3 Protein / metabolism
Polyketides / chemistry
Polyketides / metabolism
Polyketides / pharmacology*
Structure-Activity Relationship
Xylariales / chemistry*

Substances

Inflammasomes
Lipopolysaccharides
NLR Family, Pyrin Domain-Containing 3 Protein
Nlrp3 protein, mouse
Polyketides
spirodalesol