细胞粘附肽RGD的液相合成

The Liquid Phase Synthesis of Cell Adhesion Peptide RGD

精氨酸-甘氨酸-天冬氨酸(RGD)是近年来发现的具有较高应用价值的生物活性短肽,可抑制肿瘤细胞与内皮细胞和基底膜的粘附,加速肿瘤细胞脱附,阻止肿瘤细胞滞留,从而抑制肿瘤细胞的转移。研究RGD序列肽的合成具有重要意义。本文以氯乙酰氯和天冬氨酸为原料经缩合、胺化合成GD二肽,其纯度为98.6%,产率约为84.8%。然后采用液相N-羧基内酸酐化学法合成了游离的RGD三肽,其纯度为94.2%,产率约为71.4%。采用红外光谱、质谱、高效液相色谱等手段对中间产物及RGD三肽进行了表征和分析,证实产物结构正确。

Arginine-Glycine-Aspartic acid( RGD),which has been paid much attention in recent years,can inhibit tumor cells and endothelial cells to adhere to basement membrane,accelerate desorption of tumor cells,and prevent retention of tumor cells,thereby inhibiting metastasis of tumor cells. In this paper,GD dipeptide was obtained with chloroacetyl chloride and aspartic acid by condensation and amination reactions with the purity of98. 6% and the yield of 84. 8%. Free RGD tripeptide was synthesized in liquid phase by the chemical method of Ncarboxy anhydride with the purity of 94. 2% and the yield of 71. 4%. The intermediate and RGD tripeptide were characterized by IR,MS and HPLC.