Study on the Inhibitory Activity of Acacetin on Mitogen-Activated Protein Kinase p38α
GAO Conghui
XIE Yun
REN Jianping
REN Mao
WANG Tianyi
SU Yanlei
Abstract：Objective To investigate the inhibitory activity of acacetin on mitogen-activated protein kinase p38α(p38αMAPK).Methods The macromolecular docking software Autodock Vina was used for macromolecular docking be-tween acacetin and the active site 1KV2 of the target enzyme 3D structure,and then the lipopolysaccharide(LPS)-induced mouse RAW264.7 cell inflammation model was used to validate the inhibitory activity of acacetin on p38αMAPK.Results Acacia can bind to the active site of 1KV2 and inhibit the entry of substrate adenosine triphosphate,thus inhibiting the biologi-cal function of p38αMAPK.Compared with the model group,the levels of nitric oxide and tumor necrosis factor-α in the su-pernatant of RAW 264.7 cell inflammatory model cells were significantly reduced after the intervention of Dexamethasone and acacillin at different concentrations and doses(P<0.05).Conclusion Acacetin can act on the active site of p38αMAPK to produce the anti-inflammatory activity.
Keywords：Mitogen-activated protein kinase p38 α subtypeCrystal structureAcacetinMacromolecular dockingLipopolysaccharideNitric oxideTumor necrosis factor-αPharmacological activity
Publication Date：2024-02-20
Online Publishing Date：2025-08-15(First online date of this platform, not the publication date of the document)
Pages：4( 7-10 )