天然产物研究与开发
天然產物研究與開髮
천연산물연구여개발
NATURAL PRODUCT RESEARCH AND DEVELOPMENT
2010年
1期
33-36
,共4页
膜型前列腺素E_2合酶-1%炎症%中药%药物筛选
膜型前列腺素E_2閤酶-1%炎癥%中藥%藥物篩選
막형전렬선소E_2합매-1%염증%중약%약물사선
mPGES-1%inflammation%traditional Chinese medicine%drug screening
通过建立的选择性膜型前列腺素E_2合酶-1(mPGES-1)表达抑制剂的体外细胞筛选模型,对50味中药共236个样品进行筛选.初筛中,筛选中药不同极性提取物对mPGES-1表达的抑制作用,抑制率>50%的样品进入复筛;复筛中,检测初筛活性样品对环氧化酶(COX)-1和COX-2表达的抑制作用,抑制率均<20%的样品认为是阳性物.结果表明,吲哚美辛对3种酶的抑制活性与文献报道相近;筛选发现泽泻组分1、蒲黄组分2对mPGES-1的表达有可重复的选择性抑制作用,对泽泻组分1、蒲黄组分2进行进一步研究,有望确定其抗炎的有效部位或化合物.
通過建立的選擇性膜型前列腺素E_2閤酶-1(mPGES-1)錶達抑製劑的體外細胞篩選模型,對50味中藥共236箇樣品進行篩選.初篩中,篩選中藥不同極性提取物對mPGES-1錶達的抑製作用,抑製率>50%的樣品進入複篩;複篩中,檢測初篩活性樣品對環氧化酶(COX)-1和COX-2錶達的抑製作用,抑製率均<20%的樣品認為是暘性物.結果錶明,吲哚美辛對3種酶的抑製活性與文獻報道相近;篩選髮現澤瀉組分1、蒲黃組分2對mPGES-1的錶達有可重複的選擇性抑製作用,對澤瀉組分1、蒲黃組分2進行進一步研究,有望確定其抗炎的有效部位或化閤物.
통과건립적선택성막형전렬선소E_2합매-1(mPGES-1)표체억제제적체외세포사선모형,대50미중약공236개양품진행사선.초사중,사선중약불동겁성제취물대mPGES-1표체적억제작용,억제솔>50%적양품진입복사;복사중,검측초사활성양품대배양화매(COX)-1화COX-2표체적억제작용,억제솔균<20%적양품인위시양성물.결과표명,신타미신대3충매적억제활성여문헌보도상근;사선발현택사조분1、포황조분2대mPGES-1적표체유가중복적선택성억제작용,대택사조분1、포황조분2진행진일보연구,유망학정기항염적유효부위혹화합물.
To determine selective inhibitors of mPGES-1 expression in vitro from Traditional Chinese Medicine (TCM).In the primary screening,the samples with inhibitory ratio >50% of mPGES-1 expression can enter into the secondary screening,then the samples with inhibitory ratio <20% of COX-1 and COX-2 expression together can be regarded as hits.Total 236 samples from 50 species of TCM were detected.The results showed that indomethacin was shown to be an inhibitor of all 3 enzymes similar with the references.The selective inhibitory activities against mPGES-1 expression of the extracts of Alisma orientale and pollen typhae were significant.The further study on the active extracts of Alisma ori-entale and pollen typhae can contribute to determine the anti-inflammatory effective location or compounds.
