生长抑素类似物depreotide的合成与鉴定的实验研究

Experimental study on synthesizing and appraising depreotide

目的:采用Fmoc固相合成法合成一种新型生长抑素类似物depreotide。方法:以Fmoc固相法合成depreotide的环肽片段部分cyclo-[(N-Me)Phe-Tyr-D-Trp-Lys-Val-Hcy]和线性肽部分[CH2-CO.-βDap-Lys-Cys-Lys.amide],经过液相片段连接法将2片段连接,经过高压液相色谱分析和质谱分析进行产品纯化鉴定。结果:采用Fmoc固相法和液相片段连接法合成的产品经质谱分析后确定相对分子质量为1 358,为depreotide;经高压液相色谱分析产品纯度达到95.29%。结论:采用固相合成法和液相片段连接法合成法可以获得高纯度的depreotide。

Objective To synthesize depreotide which possesses a high affinity for the somatostatin receptor and contain a chelator for the radionuclide technetium-99m.Methods The cyclopeptide,cyclo-[（N-Me）Phe-Tyr-D-Trp-Lys-Val-Hcy],the linear peptide,and[ClCH2-CO.β-Dap-Lys-Cys-Lys.amide] were synthesised by Fmoc solid-phase synthesis.The cyclopeptide and the linear peptide were linked by liquid-phase synthesis.The product was isolated and purified by high performance liquid chromatography and was confirmed by mass spectrography. Results The molecular weight of synthesized product was 1358. The purity was 95. 29%. The product was depreotide. Conclusion High purity depreotide is synthesized by Fmoc solid-phase synthesis and liquid-phase synthesis.