Amphibian skin secretions are known to contain numerous peptides with a large array of biological activities. Bombinins are a group of amphibian-derived peptides with broad spectrum antimicrobial activities that have been only identified from the ancient toad species, Bombina. In this study, we described the identification and characterization of a novel bombinin precursor which encoded a bombinin-like peptide (BLP-7) and a novel bombinin H-type peptide (named as Bombinin H-BO) from the skin secretion of Oriental fire-bellied toad, Bombina orientalis. The primary structures of both mature peptides were determined by combinations of molecular cloning of peptide precursor-encoding cDNAs and mass spectrometry techniques. Secondary structure prediction revealed that both peptides had cationic amphipathic α-helical structural features. The synthetic replicate of BLP-7 displayed more potent antimicrobial activity than Bombinin H-BO against Gram-positive and Gram-negative bacteria and yeast. Also, in vitro antitumour assay showed that both peptides possessed obvious antiproliferative activity on three human hepatoma cells (Hep G2/SK-HEP-1/Huh7) at the non-toxic doses. These results indicate the peptide family of bombinins could be a potential source of drug candidates for anti-infection and anticancer therapy.

译文

已知两栖动物皮肤分泌物含有大量具有大量生物活性的肽。Bombinins是一组具有广谱抗菌活性的两栖动物衍生肽,仅从古代蟾蜍物种Bombina中鉴定出。在这项研究中,我们描述了一种新的bombinin前体的鉴定和表征,该前体编码了一种bombinin样肽 (BLP-7) 和一种新的bombinin H型肽 (称为Bombinin H-BO),来自东方火腹蟾蜍的皮肤分泌物,东方Bombina。通过编码肽前体的cdna的分子克隆和质谱技术的组合确定了两种成熟肽的一级结构。二级结构预测表明,两种肽均具有阳离子两亲性 α-螺旋结构特征。BLP-7的合成复制比Bombinin H-BO对革兰氏阳性和革兰氏阴性细菌和酵母表现出更有效的抗菌活性。此外,体外抗肿瘤测定表明,两种肽在无毒剂量下对三种人肝癌细胞 (Hep G2/SK-HEP-1/Huh7) 具有明显的抗增殖活性。这些结果表明,bombinins的肽家族可能是抗感染和抗癌治疗的候选药物的潜在来源。

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