详细记录  
题名:Caerulein precursor fragment (CPF) peptides from the skin secretions of Xenopus laevis and Silurana epitropicalis are potent insulin-releasing agents.
作者:SRINIVASAN D; MECHKARSKA M; ABDEL-WAHAB YH; FLATT PR; CONLON JM;
来源:Biochimie. 2013 Feb;95(2):429-35. doi: 10.1016/j.biochi.2012.10.026. Epub 2012 [ IF= 3.02 ] ]
URL :10.1016/j.biochi.2012.10.026
日期:20130228
摘要:Peptidomic analysis of norepinephrine-stimulated skin secretions of the
tetraploid clawed frog Xenopus laevis (Pipidae) led to the identification of 10
peptides with the ability to stimulate the release of insulin from the rat
BRIN-BD11 clonal beta cell line. These peptides were purified to near homogeneity
and structural characterization showed that they belong to the magainin (2
peptides), peptide glycine-leucine-amide (PGLa) (1 peptide), xenopsin precursor
fragment (1 peptide), and caerulein precursor fragment (CPF) (6 peptides)
families. CPF-1, CPF-3, CPF-5 and CPF-6 were the most potent producing a
significant (P < 0.05) increase in the rate of insulin release at concentration
of 0.03 nM. CPF-7 (GFGSFLGKALKAALKIGANALGGAPQQ) produced the maximum stimulation
of insulin release (571 +/- 30% of basal rate at 3 muM). In addition, CPF-SE1
(GFLGPLLKLGLKGVAKVIPHLIPSRQQ), previously isolated from skin secretions of the
tetraploid frog Silurana epitropicalis, produced a significant (P < 0.05)
increase in the rate of insulin release at 0.03 nM with a 514 +/- 13% increase
over basal rate at 3 muM. No CPF peptide stimulated release of the cytosolic
enzyme, lactate dehydrogenase from BRIN-BD11 cells at concentrations up to 3 muM
indicating that the integrity of the plasma membrane had been preserved. The
mechanism of action of the CPF peptides involves, at least in part, membrane
depolarization and an increase in intracellular Ca(2+) concentration. The CPF
peptides show potential for development into agents for the treatment of Type 2
diabetes.

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