论文标题：total synthesis and antimicrobial evaluation of natural albomycins against clinical pathogens
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作者：zihua lin, xiaobo xu, sheng zhao, xiaohong yang, jian guo, qun zhang, chunmei jing, shawn chen & yun he
发表时间：2018/09/04
数字识别码：10.1038/s41467-018-05821-1
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《自然-通讯》近期发表的一篇论文total synthesis and antimicrobial evaluation of natural albomycins against clinical pathogens指出，真菌化合物白霉素δ2具有成为抗生素的潜力。该研究介绍了一种在实验室高效合成白霉素δ2的新方法，并进一步测定了白霉素δ2对不同细菌的体外抗菌活性。
图1：白霉素δ1，δ2和ε的化学结构及其合成策略。图源：lin et al.
抗生素通常是一类化学结构复杂的天然物质，人工合成（即在实验室从头开始合成）难度较大。由于细菌会对特定抗生素产生耐药性，研究人员必须不断探索新的抗菌化合物。
图2：白霉素δ1，δ2和ε的全合成。图源：lin et al.
白霉素经证实是一类具有抗菌特性的真菌化合物。中国重庆大学的贺耘及同事发现的新技术能够合成大量白霉素，足够用于抗菌活性的测定。研究人员发现，白霉素δ2这种化合物对从患者体内分离出的大肠杆菌、肺炎链球菌、金黄色葡萄球菌等菌株的体外抗菌效果较好。值得注意的是，在对耐甲氧西林金黄色葡萄球菌（mrsa）分离株的抗菌测定中，白霉素δ2比几种已知抗生素（如青霉素）的抗菌效果更好。
不过，白霉素δ2可否成为安全有效的抗菌药物仍待进一步检测。
摘要：development of effective antimicrobial agents continues to be a great challenge, particularly due to the increasing resistance of superbugs and frequent hospital breakouts. there is an urgent need for more potent and safer antibiotics with novel scaffolds. as historically many commercial drugs were derived from natural products, discovery of antimicrobial agents from complex natural product structures still holds a great promise. herein, we report the total synthesis of natural albomycins δ1 (1a), δ2 (1b), and ε (1c), which validates the structures of these peptidylnucleoside compounds and allows for synthetic access to bioactive albomycin analogs. the efficient synthesis of albomycins enables extensive evaluations of these natural products against model bacteria and clinical pathogens. albomycin δ2 has the potential to be developed into an antibacterial drug to treat streptococcus pneumoniaeand staphylococcus aureus infections.
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