The Synthesis And Optimizing Reaction Condition Of Oligopeptide Containing Arg-Gly-Asp Sequence

The bioactivities and pharmacology of the ploypeptides have been noticed. Because the ploypeptides have good biology compatibility and low side-effect, they have become an important project in the research and development of new drugs.One well-known peptide is the minimal cell recognition sequence Arg-Gly-Asp(RGD), which is found in many protein located on cell surfaces, within extracellular matrices ,and in blood. It is the minimum ammonia serial on the ligand, which can be recognized by most of the integrins. It has important influence on the recognition of endothelial cell and anti-thrombus, anti-tumour function and therapy of burn and skin helcosis.In this paper, Protection over Gly, Arg and Asp were carried and Liquid phase synthesis and purification of RGD and GRGD were taken. The graft on the materials surface and the endothelial cells growth on the materials surface were taken. They will have important use to improve the blood compatability of cardiovascular materials and enhance ratio of the success in the replant surgery. TLC method was used to trace the reaction process and test the products purity. RGD and GRGD were purified with column chromatography. Testing of melting point, polarimeter, IR, MS and analyzing of amino acid were used to analysis the synthesis productions.Optical microscope and SEM were used to observe the status of endothelial cell growth. We optimized the esterify reaction condition of Aspartic acid with theorthogonal design. And for the first time we optimized the DCC coupling reaction system condition with the system engineering technology. ROD and GRGD are obtained in the solution phase synthesis. The endothelialization result shows that RGD serial can improve the effect of materials endothelialization ?Structure-activity relationship studies suggest that the sole critical prerequisite for receptor recognition is molecule that contains a guanidinican group and another carboxyl group.