Structural modifications of paeonol and its analogs, and their stability in the simulated body fluids and anti-inflammatory activity
HU Ding-wang
PENG Yong-lian
LIN You-wen
CHEN Li-min
Abstract：Objective:To connect paeonol and its analogs with 1,4-dibromobutane,then to afford a series of target products by reacting with naproxen,and investigate the anti-inflammatory activities of the products.Methods:Paeonol,2-hydroxy-5-methoxyacetophenone,3-hydroxyacetophenone,2-hydroxyacetophenone,and 2,4-dihydroxyacetophenone were condensated with 1,4-dibromobutane,then reacted with naproxen to yield series of target products.An HPLC method was established for determining the content of the target products.Their degradation dynamics was assessed under pH 1.2,5.0 and 7.4 buffer conditions at 37 ℃.The anti-inflammatory activities of the compounds were evaluated in xylene-induced mouse ear swelling model.Results:Five new compounds were synthesized and confirmed by MS and 1H-NMR.Degradation kinetic experiments showed that these compounds were stable in buffers of different pHs.All the compounds showed anti-inflammatory activities.Conclusion:All the compounds are stable and exhibit potent anti-inflammatory activities.
Keywords：paeonolnaproxensynthesisHPLCanti-inflammatory activity
Publication Date：2017-01-01
Online Publishing Date：2026-08-14(First online date of this platform, not the publication date of the document)
Pages：4( 1968-1971 )