As drug‐resistant bacteria have become a serious health problem and have caused thousands of deaths, finding new antibiotics has become an urgent research priority. A novel antimicrobial peptide, named Brevinin‐1H, was identified in the skin secretion of Amolops hainanensis through ‘shotgun’ cloning. It has broad‐spectrum antimicrobial activity against tested micro‐organisms and has anticancer cell activity. To improve its bioactivity and decrease its cytotoxicity, two structural analogues—Brevinin‐1Ha and Brevinin‐1HY—were designed based on the secondary structure of the natural peptide. Brevinin‐1HY, in which tyrosine substituted Pro¹¹, had similar activity to the natural peptide against Gram‐negative bacteria and cancer cells, but showed a dramatic increase in haemolytic activity and cytotoxicity at its minimum inhibitory concentration. Brevinin‐1Ha, which transferred the Rana‐box from the C‐terminal to a central position, had significantly decreased haemolytic activity, but also in antimicrobial and anticancer activity. The present data suggest that increasing the proportion of α‐helix structure in an AMP can increase its target micro‐organism bioactivity to some extent.

中文翻译：

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一种新型肽 Brevinin-1H 的表征，来自海南黄花梨的皮肤分泌物和几种类似物的合理设计

由于耐药细菌已成为一个严重的健康问题并已导致数千人死亡，因此寻找新的抗生素已成为一项紧迫的研究重点。通过“霰弹枪”克隆在海南黄花菜的皮肤分泌物中鉴定出一种名为 Brevinin-1H 的新型抗菌肽。它对测试的微生物具有广谱抗菌活性，并具有抗癌细胞活性。为了提高其生物活性并降低其细胞毒性，基于天然肽的二级结构设计了两种结构类似物——Brevinin-1Ha 和 Brevinin-1HY。Brevinin-1HY，其中酪氨酸取代 Pro ¹¹, 与天然肽对革兰氏阴性菌和癌细胞的活性相似，但在其最低抑制浓度下显示出溶血活性和细胞毒性的显着增加。Brevinin-1Ha 将 Rana-box 从 C 端转移到中心位置，显着降低了溶血活性，但也具有抗菌和抗癌活性。目前的数据表明，增加 AMP 中 α-螺旋结构的比例可以在一定程度上提高其目标微生物的生物活性。