| 异柠檬酸裂解酶肽类抑制剂结构的修饰 |
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| 引用本文： | 刘志远,张爱臣,刘新涛,关晓侠,李玲玲,殷玉和.异柠檬酸裂解酶肽类抑制剂结构的修饰[J].吉林大学学报(理学版),2014,52(4):847-851. |
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| 作者姓名： | 刘志远 张爱臣 刘新涛 关晓侠 李玲玲 殷玉和 |
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| 作者单位： | 1. 长春工业大学 化学与生命科学学院, 长春 130012； 2. 吉林大学 中日联谊医院, 长春 130033 |
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| 基金项目： | 吉林省教育厅科技发展计划项目(批准号:2009110) |
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| 摘 要： | 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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| 关 键 词： | 异柠檬酸裂解酶 肽类 抑制剂 环肽 |
| 收稿时间： | 2013-09-29 |
Modification of Isocitrate Lyase Peptide Inhibitor |
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| LIU Zhiyuan,ZHANG Aichen,LIU Xintao,GUAN Xiaoxia,LI Lingling,YIN Yuhe.Modification of Isocitrate Lyase Peptide Inhibitor[J].Journal of Jilin University: Sci Ed,2014,52(4):847-851. |
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| Authors: | LIU Zhiyuan ZHANG Aichen LIU Xintao GUAN Xiaoxia LI Lingling YIN Yuhe |
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| Institution: | 1. School of Chemistry and Life Science, Changchun University of Technology, Changhun 130012, China;2. China Japan Union Hospital, Jilin University, Changhun 130033, China |
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| Abstract: | 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 11 min, which is increased by 175% compared with that of linear peptide. |
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| Keywords: | isocitrate lyase peptide inhibitor cyclic peptide |
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