Modification of Glucagon-like Peptide-1 in Ethanol with Polyethylene Glycol
WANG You-ao, ZHAI Yan-qin LEI Jian-du MA Guang-hui SU Zhi-guo
State Key Lab of BiochemicaL Engineering, Institute of Process Engineering, Chinese Academy of Sciences Multi-phase Reaction Laboratory, Institute of Process Engineering
Chinese Academic of Science
National Laboratoru of Biochemical Engineering, Insitute of Process
Engineering
National Laboratoru of Biochemical Engineering, Insitute of Process
Engineering
National Laboratoru of Biochemical State Key Lab. Biochem. Eng., Inst. Process Eng., Chinese Academy of Sciences State Key Lab. Biochem. Eng., Inst. Process Eng., Chinese Academy of Sciences
Abstract： Glucagon-like peptide-1 (GLP-1) was modified with monomethoxy polye(ethylene glycol succinimidyl carbonate) by using ethanol as a reaction medium. The reaction conditions were investigated and optimized, and the separation procedures of product Mono-PEG-GLP-1 were developed. After that, the stability in vitro and activity in vivo of Mono-PEG-GLP-1 were investigated. The optimized reaction conditions were obtained as follows: concentration of GLP-1 1.0 mg/mL, molar ratio of PEG to GLP-1 1:1, and reaction time 24 h at 37℃. Under the optimized conditions, the yield of Mono-PEG-GLP-1 was up to 77%. The Mono-PEG-GLP-1 was separated from reaction mixture by a preliminary centrifugation under frozen temperature and successive purification by reverse phase chromatography. The purity of Mono-PEG-GLP-1 was higher than 97%, as characterized by size exclusion chromatography. The Mono-PEG-GLP-1 showed better stability in plasma, decreased proteolysis to trypsin and better activity in vivo.
王友傲 翟艳琴 雷建都 马光辉 苏志国. 胰高血糖素样肽-1在乙醇中的聚乙二醇修饰[J]. , 2010, 10(3): 593-597.
WANG You-ao; ZHAI Yan-qin LEI Jian-du MA Guang-hui SU Zhi-guo. Modification of Glucagon-like Peptide-1 in Ethanol with Polyethylene Glycol. , 2010, 10(3): 593-597.
2010, Vol. 10 
