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下一代抗菌肽作为分子靶向药物。

Next generation of antimicrobial peptides as molecular targeted medicines.

机构信息

Japan Society for the Promotion of Science, Sakyo-ku, Kyoto 606-8502, Japan.

出版信息

J Biosci Bioeng. 2012 Oct;114(4):365-70. doi: 10.1016/j.jbiosc.2012.05.001. Epub 2012 May 31.

Abstract

Antibiotics have significantly improved our living environments. However, overuse of antibiotics has led to the emergence of multi-drug resistant microorganisms, and the subsequent constant demand for the exploration of novel antibiotics. To this end, antimicrobial peptides (AMPs) have attracted much attention as a novel class of antibiotics. AMPs have strong antimicrobial activity against a wide-range of species, including gram-positive and gram-negative bacteria, fungi, and viruses. In addition, they are also effective against pathogenic organisms that are resistant to conventional drugs. Despite their great potential, the hemolytic activity and a highly broad spectrum of activity of AMPs dictate the need for amendments to develop safe pharmaceuticals. The human body contains commensal microflora as an integral part of complex mucosal surfaces that offers protection against pathogenic organisms. Administration of antibiotics with broad spectra of activity disrupts the indigenous microflora and increases the risks of diarrhea and other fatal infections. Therefore, it is difficult, but vital, to develop treatments capable of rapidly eliminating pathogenic organisms while maintaining the commensal microbiota. As such, novel pharmaceuticals, safe designer AMPs have been heavily researched. In this article, we review recent attempts to spatially and temporally regulate AMPs to enhance the quality-of-life of patients.

摘要

抗生素显著改善了我们的生活环境。然而,抗生素的过度使用导致了多药耐药微生物的出现,随后不断需要探索新型抗生素。为此,抗菌肽 (AMPs) 作为一种新型抗生素引起了广泛关注。AMPs 对多种物种具有很强的抗菌活性,包括革兰氏阳性和革兰氏阴性细菌、真菌和病毒。此外,它们对对抗生素耐药的致病生物也有效。尽管具有巨大的潜力,但 AMPs 的溶血活性和广谱活性决定了需要进行修正以开发安全的药物。人体共生微生物群作为复杂黏膜表面的一个组成部分,为机体提供了对致病生物的保护。广谱抗生素的使用会破坏体内原有的微生物群,增加腹泻和其他致命感染的风险。因此,开发能够快速消除致病生物同时维持共生微生物群的治疗方法是困难但至关重要的。因此,新型药物,即安全的设计 AMPs,受到了广泛的研究。在本文中,我们综述了最近在时空调控 AMPs 以提高患者生活质量方面的尝试。

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