摘要
通过建立的选择性膜型前列腺素E2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。
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 ...
出处
《天然产物研究与开发》
CAS
CSCD
2010年第1期33-36,共4页
Natural Product Research and Development
基金
江苏省海洋资源开发研究院基金(JSIMR09A04)
淮海工学院自然科学基金(KX07031)
