A potent, non-toxic insulin-releasing peptide isolated from an extract of the skin of the Asian frog, Hylarana guntheri (Anura:Ranidae)
A potent, non-toxic insulin-releasing peptide isolated from an extract of the skin of the Asian frog, Hylarana guntheri (Anura:Ranidae)
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DOI：
10.1016/j.regpep.2008.04.002
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发表时间：
2008-11-29
影响因子：
--
通讯作者：
Vaudry, Hubert
中科院分区：
文献类型：
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作者：
Conlon, J. Michael;Power, Gavin J.;Vaudry, Hubert
1882年的亚洲蛙（Hylarana guntheri Boulenger）皮肤提取物中的肽段通过反相高效液相色谱法进行纯化，并分析各个组分从大鼠BRIN - BD11克隆β细胞系中释放胰岛素的能力。在提取物中鉴定出的最有效的肽段属于布雷维宁 - 2家族（布雷维宁 - 2GUb；GVIIDTLKGAAKTVAAELLRKAHCKLTNSC）。其他具有较弱胰岛素释放活性的肽段属于布雷维宁 - 1（2种肽）、布雷维宁 - 2（2种肽）和 temporin（3种肽）家族。只有布雷维宁 - 1肽对BRIN - BD11细胞显示出细胞溶解活性，这通过胞质酶乳酸脱氢酶释放速率的增加得以证明。布雷维宁 - 2GUb的合成复制品对胰岛素释放产生了显著的刺激作用（为基础速率的139%；P<0.001），并且在10 μM浓度下对细胞活力没有显著影响（P>0.05）。这些结果表明亚洲蛙皮肤提取物中的肽段可能具有作为新型抗糖尿病药物的潜力。
Peptides in extract of the skin of the Asian frog Hylarana guntheri Boulenger,1882 were purified by reversed-phase HPLC and individual components analysed for their ability to release insulin from the rat BRIN-BD11 clonal beta cell line. The most potent peptide identified in the extract belonged to the brevinin-2 family (brevinin-2GUb; GVIIDTLKGAAKTVAAELLRKAHCKLTNSC). Other peptides with weaker insulin-releasing activity belonged to the brevinin-1 (2 peptides), brevinin-2 (2 peptides) and temporin (3 peptides) families. Only the brevinin-1 peptides showed cytolytic activity against the BRIN-BD11 cells, as demonstrated by an increased rate of release of the cytosolic enzyme, lactate dehydrogenase. A synthetic replicate of brevinin-2GUb produced a significant stimulation of insulin release (139% of basal rate; P