ZHANG Chang-bin1, LI Cang-hai2, SUI Feng2, et al. Comparative Study on the Effects of Phenylallyl Compounds from Guizhi Decoction on COX-2 and PGES[J]. Chinese journal of experimental traditional medical formulae, 2012, 18(9): 157-161.
ZHANG Chang-bin1, LI Cang-hai2, SUI Feng2, et al. Comparative Study on the Effects of Phenylallyl Compounds from Guizhi Decoction on COX-2 and PGES[J]. Chinese journal of experimental traditional medical formulae, 2012, 18(9): 157-161. DOI: 10.13422/j.cnki.syfjx.2012.09.030.
Objective: To compare the effects of 6 phenylallyl compounds on cyclooxygenase-2(COX-2) and prostaglandin synthase(PGES) mRNA expression
and provide some evidence for their structure-activity relationship.Method: Macrophages stimulated by lipopolysaccharide(LPS) model was used to test the effects of cinnamic alchohol
O-methoxy cinnamic alchohol
cinnamaldehyde
O-methoxy cinnamaldehyde
cinnamic acid and O-methoxy cinnamic acid on COX-2 and PGES at mRNA level.The RAW264.7 cells was treated with 1 mg·L-1 LPS and phenylallyl compounds(0
12
19
32
54
90
150 mg·L-1) for 4 h
and the mRNA was detected by TaqMan real time PCR.Result: The cinnamaldehyde had the strongest effect
showed significant effect on COX-2(P<0.05) and membrane-associated PGES-1(mPGES-1)(P<0.01) at 32 mg·L-1.The O-methoxy cinnamaldehyde took second place
showed significant effect on COX-2(P<0.05) and mPGES-1(P<0.05) at 54 mg·L-1.The other 4 phenylallyl compounds had effects in different degree
but was much weaker than cinnamaldehyde and O-methoxy cinnamaldehyde.Conclusion: It is key mechanism of anti-inflammatory and antipyretic for the phenylallyl compounds to down-regulate PGE2 production by inhibiting COX-2 and mPGES-1.The efficacy of the phenylallyl compounds was aldehyde>alcohol>acidum
and it is degraded by the methoxyl.The action intensity may be closely related to the different oxidation state of propenyl and impacted by methoxyl.