The Anti-inflammatory Activities And Mechanism Of Coumarin From Durian And Triterpenoid From Chinese Acorns

Aim:We have previously studied the chemical constituents of durian and Chinese oak.Propacin is a coumarins isolated from durian and Q43 is a triterpenoid from Chinese oak.To explore the anti-inflammation effects of propacin and Q43,we investigate the effects and mechanisms of propacin and Q43 in LPS-induced cells models in vitro.Methods:In this paper,qRT-PCR,ELISA,Fluorescence microscopy and western blot were used to detect the release of inflammatory kinase,the expression of pro-inflammatory mediator and signal pathway,to investigate the anti-inflammatory activities and mechanisms of propacin and Q43.Result:Propacin suppressed the nitric oxide?NO?and prostaglandin E2?PGE₂?production in lipopolysaccharide?LPS?-stimulated macrophages without cytotoxicity.Propacin deceased the inducible nitric oxide synthase?iNOS?and cyclooxygenase-2?COX-2?expression on mRNA and protein level,downregulated interleukin-1??IL-1??,IL-6 and tumor necrosis factor-??TNF-??mRNA expression as well as the secretions of IL-6 and TNF-?.According to Western blot analysis,propacin deceased the phosphorylation of nuclear factor-kappa B?NF-?B?,inhibitor of?B?I?B??and mitogen-activated protein kinases?MAPKs?,suppressed nuclear translocation of NF-?B.Q43 inhibited NO and PGE₂ releasing in LPS-induced BV2 cells,suppressed i NOS and COX-2 expression on mRNA and protein levels.In addition,Q43decreased the mRNA levels of IL-1?,IL-6 and TNF-?,as well as the production of IL-6 and TNF-?.According to Western blot analysis,Q43 down-regulated the expression of p-NF-?B and p-I?B?,inhibited NF-?B nuclear translocation,inhibited phosphorylation of MAPKs proteins.Conclusion:Through suppress MAPK and NF-?B pathway,propacin inhibits inflammatory response mediated by abnormal macrophage activation,Q43inhibits neuroinflammatory response mediated by abnormal microglia activation.Therefore,propacin and Q43 may provide a potential therapeutic strategy for the treatment of inflammation.