Anti-inflammatory effect of novel andrographolide derivatives through inhibition of NO and PGE2 production
Anti-inflammatory effect of novel andrographolide derivatives through inhibition of NO and PGE2 production
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DOI：
10.1016/j.intimp.2011.09.010
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发表时间：
2011-12-01
影响因子：
5.6
通讯作者：
Liu, Hong-Min
中科院分区：
文献类型：
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作者：
Dai, Gui-Fu;Zhao, Jin;Liu, Hong-Min
穿心莲内酯(1)是一种主要的二萜内酯，具有抗炎作用，存在于穿心莲（草本植物）中。f) Nees，在中医中广泛使用。从穿心莲内酯合成更有效的药物是非常有趣的，并且可以证明是非常有用的。在本研究中，我们研究了穿心莲内酯及其衍生物（化合物2-6）通过二甲苯诱导小鼠耳部水肿的抗炎作用。将所研究的物质灌胃，并分析其构效关系。结果表明，与化合物1相比，化合物5和6能显著抑制耳部水肿(p
Andrographolide (1) is a major diterpene lactone exhibiting anti-inflammatory effects and is found in the plant Andrographis paniculata (Burm. f) Nees, which is widely used in Traditional Chinese Medicine. Synthesis of more effective drugs from andrographolide is very interesting and can prove to be highly useful. In this study, we investigated the anti-inflammatory effects of andrographolide and its derivatives (compounds 2-6) through dimethylbenzene-induced ear edema in mice. Substances under study were administrated intragastrically and the structure-activity relationship was analyzed. Results showed that compounds 5 and 6 significantly inhibited ear edema compared with compound 1 (p