Natural Potent NAAA Inhibitor Atractylodin Counteracts LPS-Induced Microglial Activation
Laboratory studyOther animalsWith atractylodin (a NAAA inhibitor that raises cellular PEA, tested alone)
This study tested palmitoylethanolamide together with atractylodin (a NAAA inhibitor that raises cellular PEA, tested alone). Its results cannot be assigned to palmitoylethanolamide alone. More combination studies.
- Design
- Laboratory study
- Subjects
- Enzyme assays with human NAAA and BV-2 mouse microglial cells stimulated with lipopolysaccharide
- Dose used in the study
- Atractylodin in cell culture; IC50 for NAAA 2.81 micromolar; cytokine doses not stated in the abstract
- Duration
- Not stated in the abstract
- What was measured
- NAAA enzyme inhibition by a fluorescence screening assay, kinetics, dialysis and docking; cellular PEA and OEA levels; nitrate, TNF-alpha, IL-1-beta and IL-6 release from microglia
What the authors reported
Atractylodin inhibited NAAA with an IC50 of 2.81 micromolar by reversible competitive inhibition, docking to the catalytic cavity near Trp181 and Leu152. It raised PEA and OEA levels and dose-dependently reduced LPS-induced nitrate, TNF-alpha, IL-1-beta and IL-6 release in BV-2 microglia.
Limits of this study
A cell and enzyme study; it cannot show effect in people or animals treated in practice. PEA was not administered; the compound raised the cells' own PEA. Funding and conflicts not stated in the abstract.
Source
PubMed 33117168 · doi:10.3389/fphar.2020.577319
Entry checked against the abstract on PubMed on 2026-09-22. The dose shown is the dose the researchers used. It is not a recommendation. How to read this page.