Fmoc solid-phase peptide synthesis was used to synthesize cyclic peptide in light of the known isocitrate lyase linear peptide sequence according to the end to end way.Mass spectrometry demonstrates that the measured value of relative molecular mass is consistent with the theoretical value.Inhibition test confirms that the cyclic peptide shows significant inhibition to the ICL activity (the inhibition rate was more than 50%).At the same time,half-life of linear peptide and that of cyclic peptide in plasma were measured by HPLC.Results indicate that half-life of cyclic peptide in plasma amounts to 1 1 min,which is increased by 175% compared with that of linear peptide.%利用 Fmoc 固相多肽合成法,按已知异柠檬酸裂解酶抑制剂的直链肽氨基酸序列合成首尾相连的环肽抑制剂。经色谱纯化和质谱鉴定,其相对分子质量的实测值与理论值相符。抑制率实验结果表明,合成的环肽对异柠檬酸裂解酶有明显抑制作用,抑制率大于50%。采用高效液相色谱法分别检测直链肽和环肽在血浆中的半衰期,实验结果表明,环肽在血浆中的半衰期为11 min,比直链肽的半衰期延长175%。
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