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利用体内家蚕筛选系统发现靶向抗菌活性调节剂的新型抗菌药物耐药性药物

Discovery of new AMR drugs targeting modulators of antimicrobial activity using in vivo silkworm screening systems.

作者信息

Tabuchi Fumiaki, Mikami Kazuhiro, Miyauchi Masanobu, Sekimizu Kazuhisa, Miyashita Atsushi

机构信息

Teikyo University Institute of Medical Mycology, Hachioji, Tokyo, Japan.

Graduate School of Medical Care and Technology, Teikyo University, Itabashi, Tokyo, Japan.

出版信息

J Antibiot (Tokyo). 2025 Jan;78(2):69-77. doi: 10.1038/s41429-024-00788-2. Epub 2024 Nov 14.

Abstract

Global concerns about drug-resistant bacteria have underscored the need for new antimicrobial drugs. Emerging strategies in drug discovery include considering the third factors that influence drug activity. These factors include host-derived elements, adjuvants, and drug combinations, which are crucial in regulating antimicrobial efficacy. Traditional in vivo assessments have relied on animal models to study drug absorption, distribution, metabolism, excretion, and toxicity (ADMET). Alternative models, such as silkworms, are being explored to overcome the ethical and financial barriers associated with mammalian models. The silkworm has been proven effective in evaluating ADMET and in highlighting the therapeutic potential enhanced by third factors. Host factors (either mammalian or non-mammalian) enhance the antimicrobial activity of antimicrobial agents such as lysocin E. Additionally, using D-cycloserine to potentiate vancomycin has successfully combated vancomycin-resistant infections in silkworms. Leveraging silkworms in drug discovery could establish a novel screening method incorporating interactions with third factors, whether host related or non-host-related, thus promising new pathways for identifying antimicrobial drugs with unique mechanisms of action.

摘要

全球对耐药菌的关注凸显了新型抗菌药物的必要性。药物研发的新兴策略包括考虑影响药物活性的第三类因素。这些因素包括宿主衍生成分、佐剂和药物组合,它们在调节抗菌效果方面至关重要。传统的体内评估依赖动物模型来研究药物的吸收、分布、代谢、排泄和毒性(ADMET)。人们正在探索如蚕等替代模型,以克服与哺乳动物模型相关的伦理和经济障碍。蚕已被证明在评估ADMET以及突出第三类因素增强的治疗潜力方面有效。宿主因素(无论是哺乳动物还是非哺乳动物)可增强诸如溶菌素E等抗菌剂的抗菌活性。此外,使用D-环丝氨酸增强万古霉素已成功对抗蚕体内的耐万古霉素感染。在药物研发中利用蚕可以建立一种结合与第三类因素(无论与宿主相关还是与非宿主相关)相互作用的新型筛选方法,从而有望为鉴定具有独特作用机制的抗菌药物开辟新途径。

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