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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, a novel somatostatin analogue by Fmoc solid phase synthesis. Methods: The cyclic peptide fragment cyclo [[(N-Me) Phe-Tyr-D-Trp-Lys-Val-Hcy] and the linear peptide moiety [CH2-CO.-βDap-Lys- Cys-Lys.amide]. The two fragments were connected by liquid-phase ligation, and the products were purified and identified by high pressure liquid chromatography and mass spectrometry. Results: The products synthesized by Fmoc solid-phase method and liquid-phase ligation method were determined by mass spectrometry. The relative molecular mass was 1 358, which was depreotide. The product purity was 95.29% by HPLC. Conclusion: High purity depreotide can be obtained by solid phase synthesis method and liquid phase ligation method.