Comparative Study on the Effects of Phenylallyl Compounds from Guizhi Decoction on COX-2 and PGES

ZHANG Chang-bin1; LI Cang-hai2; SUI Feng2; LU Yin1; LI Lan-fang2; GUO Shu-ying2; YANG Na2; GENG Dai-tao2; JIANG Ting-liang2

doi:10.13422/j.cnki.syfjx.2012.09.030

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Comparative Study on the Effects of Phenylallyl Compounds from Guizhi Decoction on COX-2 and PGES

更新时间：2024-09-23

- Comparative Study on the Effects of Phenylallyl Compounds from Guizhi Decoction on COX-2 and PGES
- Chinese Journal of Experimental Traditional Medical Formulae Vol. 18, Issue 9, Pages: 157-161(2012)
- 作者机构：
  
  1. 南京中医药大学
  2. 中国中医科学院中药研究所唐氏中药研究中心
- 作者简介：
- 基金信息：
- DOI：10.13422/j.cnki.syfjx.2012.09.030
  CLC： R285.5
- Published：2012
- 稿件说明：
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[1]张畅斌,李沧海,隋峰,陆茵,李兰芳,郭淑英,杨娜,耿代涛,姜廷良.桂枝汤苯丙烯类化合物对环氧合酶-2及前列腺素抑制的作用[J].中国实验方剂学杂志,2012,18(09):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.
[1]张畅斌,李沧海,隋峰,陆茵,李兰芳,郭淑英,杨娜,耿代涛,姜廷良.桂枝汤苯丙烯类化合物对环氧合酶-2及前列腺素抑制的作用[J].中国实验方剂学杂志,2012,18(09):157-161. DOI： 10.13422/j.cnki.syfjx.2012.09.030.

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.

摘要

目的:对比桂枝汤中6种苯丙烯类化合物对环氧合酶-2（COX-2）及前列腺素合酶（PGES）的影响

为其抗炎、解热、镇痛作用"构效关系"提供相关实验依据。方法:将小鼠巨噬细胞RAW264.7以5×105个/mL

1.90 mL/孔接种于6孔培养板

用1 mg.L-1脂多糖（LPS）分别刺激0

24 h

提取其总RNA并用TaqMan real time PCR法检测COX-2及PGESmRNA表达情况

选择1 mg.L-1LPS刺激4 h作为实验条件

建立体外炎症模型。并用桂皮醇、邻甲氧基桂皮醇、桂皮醛、邻甲氧基桂皮醛、桂皮酸、邻甲氧基桂皮酸6种苯丙烯类化合物以0

150 mg.L-1进行干预

检测其对COX-2及mPGES-1 mRNA表达情况的影响。结果:COX-2与mPGES-1 mRNA表达随LPS刺激时间变化

COX-2于4 h时达峰值后下降

而mPGES-1则一直呈上升趋势。mPGES-2与cPGES mRNA则并不随LPS刺激而变化。桂皮醛作用最强

在32 mg.L-1时显著抑制COX-2（P<0.05）和mPGES-1（P<0.01）;邻甲氧基桂皮醛次之

在54 mg.L-1时显著抑制COX-2（P<0.05）和mPGES-1（P<0.05）。其余4种化合物对COX-2和mPGES-1也均有一定的抑制作用

但其强度远弱于桂皮醛和邻甲氧基桂皮醛

在实验所设浓度范围内均无统计学意义。结论:抑制COX-2和mPGES-1

是桂枝汤苯丙烯类化合物抑制前列腺素E2（PGE2）分泌

进而发挥抗炎解热作用的重要机制。其作用强弱顺序为醛>醇>酸

结构中有邻甲氧基则作用减弱

其作用强弱似与丙烯基末端的氧化态关系密切

同时也受到甲氧基的影响。

Abstract

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

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.

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Related Author

ZHANG Chang-bin

LI Cang-hai

JIANG Ting-liang

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YANG Na

GUO Shu-ying

LI Lan-fang

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Related Institution

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