Design, synthesis and biological evaluation of novel peptide MC62 analogues as potential antihyperglycemic agents
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- 作者：Baowei Yang ; Yicheng Mei ; Xuekun Wang ; Xin Deng ; Hai Qian ; Wenlong Huang
- 关键词：Diabetes mellitus ; MC62 peptide ; Antihyperglycemic ; Antioxidative ; Streptozotocin ; Structure&ndash ; activity relationship
- 刊名：European Journal of Medicinal Chemistry
- 出版年：12 February, 2014
- 年：2014
- 卷：73
- 期：Complete
- 页码：105-111
- 全文大小：1548 K
文摘
Two series of peptide MC62 analogues were synthesized, characterized and evaluated for their antihyperglycemic effects. Structure-activity relationship studies of the first series indicated that antihyperglycemic effects were correlated to residues 4, 5, 7 and 8. Peptide I-6 exhibited higher antihyperglycemic activity than the MC62 parent peptide, and was chosen for further modification. Incorporation of Met at position 3 increased potency further and generated II-3, which was screened in聽vivo and in聽vitro using exenatide (Ex-4) and GLP-1 as positive controls. The results showed that the antihyperglycemic and antioxidative activities of II-3 were comparable to the positive controls, suggesting II-3 could be a candidate for use as a future diabetic treatment.