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Eur J Med Chem. 2014 Feb 12;73:105-11. doi: 10.1016/j.ejmech.2013.11.043. Epub 2013 Dec 12.

Design, synthesis and biological evaluation of novel peptide MC62 analogues as potential antihyperglycemic agents.

Author information

1
Center of Drug Discovery, State Key Laboratory of Natural Medicines, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing, Jiangsu 210009, China.
2
Center of Drug Discovery, State Key Laboratory of Natural Medicines, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing, Jiangsu 210009, China. Electronic address: qianhai24@163.com.
3
Center of Drug Discovery, State Key Laboratory of Natural Medicines, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing, Jiangsu 210009, China. Electronic address: ydhuangwenlong@126.com.

Abstract

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 vivo and in 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.

KEYWORDS:

Antihyperglycemic; Antioxidative; Diabetes mellitus; MC62 peptide; Streptozotocin; Structure–activity relationship

PMID:
24384551
DOI:
10.1016/j.ejmech.2013.11.043
[Indexed for MEDLINE]
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