Active Compounds From Fructus Forsythiae & Pharmic Studies On Dengxin Zhixue Capsule

Fructus Forsythiae, the dried fruit of Forsythia suspensa(Thunb.)Vahl, is a widely-used traditional Chinese medicine for anti-inflammatory, antiviviral , detoxifmg and liver-defence purpose.We have observed it could selectively blocked SDF-1/CXCR4 recently.Chemokines constitute a superfamily of small, chemoattractant cytokine-like proteins that orchestrate immunological and inflammatory processes such as leukocyte trafficking, adhesion, hematopoiesis and angiogenesis. Interaction of chemokines with specific G protein coupled receptors on target cells produces their biological effects. Increasing evidence suggests that interaction between the chemoattractant CXCL12/SDF-la and its receptor CXCR4 plays a pivotal role in metastasis of various tumors. An antagonist of SDF-1/CXCR4 may be a useful therapeutic agent for treatment of tumors, as well as HIV infection and inflammation.In an effort to find naturally occurring chemokine antagonists,we carried out systemic studies on Fructus Forsythiae. The ethanol extract of Fructus Forsythiae was separated into six parts.We isolated five compounds from CHCla Frac. And EtOAc Frac.and identified as (Iso-Bauerenyl acetate, I ) , ( (3 -Amyrine acetate, II ) , ( |3 -sitosterol,III ), ( Betulinic acid,IV ),( Oleanolic acid,V )respectively. The inhibitory effect of extracts on CXCL12/CXCR4 were measured by ligand binding assay .The EtOAc Frac.showed selectively blocking SDF-1/CXCR4 and was activiest. Research above provide foundation for its bioactivity esploitation and theory base for its clinic applications.