摘要
为了得到持续稳定控制血糖的胰高血糖素样肽-1(glucagon-like peptide-1,GLP-1)类似物,将平均相对分子质量为350、550和750的单甲氧基聚乙二醇(m PEG)分别缀合到GLP-1肽链上,设计并合成了12个衍生物。初步药理活性表明,所得化合物均保留GLP-1受体激动活性,其中化合物I-12降糖活性维持时间与艾塞那肽(Ex-4)和利拉鲁肽(Liraglutide)相当,具备成为新型长效化GLP-1受体激动剂的潜力。
In order to obtain glucagon-like peptide-1(GLP-1)analogs which can sustainedly control the levels of glucose,12 derivatives were designed and synthesized by coupling monomethoxy polyethylene glycol(mPEG,with average molecular weights of 350,550 and 750)to GLP-1 analogs.Preliminary pharmacological activities showed that all compounds retained GLP-1 receptor agonist activities,and the hypoglycemic activity of compound I-12 was similar to those of Ex-4 and Liraglutide,suggesting I-12 could be a potential long-acting GLP-1 receptor agonist.
作者
刘颜
李承业
蔡星光
孙李丹
黄文龙
LIU Yan;LI Chengye;CAI Xingguang;SUN Lidan;HUANG Wenlong(College of Pharmacy,Chongqing Medical University,Chongqing 400016;Center of Drug Discovery,China Pharmaceutical University,Nanjing 210009;Jiaxing University,Jiaxing 314000,China)
出处
《中国药科大学学报》
CAS
CSCD
北大核心
2018年第5期558-567,共10页
Journal of China Pharmaceutical University
基金
国家自然科学基金资助项目(No.81673299
No.81703346)~~
