首页> 美国卫生研究院文献>Marine Drugs >Magnificamide a β-Defensin-Like Peptide from the Mucus of the Sea Anemone Heteractis magnifica Is a Strong Inhibitor of Mammalian α-Amylases
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Magnificamide a β-Defensin-Like Peptide from the Mucus of the Sea Anemone Heteractis magnifica Is a Strong Inhibitor of Mammalian α-Amylases

机译:Magnificamide一种来自于海葵Heteractis magnifica粘液的β-防御素样肽是哺乳动物α-淀粉酶的强抑制剂。

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摘要

Sea anemones’ venom is rich in peptides acting on different biological targets, mainly on cytoplasmic membranes and ion channels. These animals are also a source of pancreatic α-amylase inhibitors, which have the ability to control the glucose level in the blood and can be used for the treatment of prediabetes and type 2 diabetes mellitus. Recently we have isolated and characterized magnificamide (44 aa, 4770 Da), the major α-amylase inhibitor of the sea anemone mucus, which shares 84% sequence identity with helianthamide from . Herein, we report some features in the action of a recombinant analog of magnificamide. The recombinant peptide inhibits porcine pancreatic and human saliva α-amylases with Ki’s equal to 0.17 ± 0.06 nM and 7.7 ± 1.5 nM, respectively, and does not show antimicrobial or channel modulating activities. We have concluded that the main function of magnificamide is the inhibition of α-amylases; therefore, its functionally active recombinant analog is a promising agent for further studies as a potential drug candidate for the treatment of the type 2 diabetes mellitus.
机译:海葵的毒液富含作用于不同生物靶标的肽,主要作用于细胞质膜和离子通道。这些动物也是胰腺α-淀粉酶抑制剂的来源,它们具有控制血液中葡萄糖水平的能力,可用于治疗糖尿病前期和2型糖尿病。最近,我们已经分离并鉴定了magnificamide(44 aa,4770 Da),这是海葵粘液的主要α-淀粉酶抑制剂,与来自的Helianthamide具有84%的序列同一性。在本文中,我们报道了甲氨酰胺的重组类似物的作用中的一些特征。重组肽抑制猪的胰腺和人唾液中的α-淀粉酶,其Ki分别等于0.17±0.06 nM和7.7±1.5 nM,并且不显示抗菌或通道调节活性。我们得出的结论是,magnificamide的主要功能是抑制α-淀粉酶。因此,其功能活性的重组类似物作为治疗2型糖尿病的潜在候选药物,是有希望进一步研究的有希望的药物。

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