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引用次数: 0
摘要
全球对耐药性细菌的担忧凸显了对新型抗菌药物的需求。药物发现的新策略包括考虑影响药物活性的第三个因素。这些因素包括宿主衍生元素、佐剂和药物组合,它们对调节抗菌药的疗效至关重要。传统的体内评估依赖于动物模型来研究药物的吸收、分布、代谢、排泄和毒性(ADMET)。为了克服与哺乳动物模型相关的伦理和经济障碍,人们正在探索替代模型,例如家蚕。事实证明,蚕能有效评估 ADMET,并通过第三种因素突出治疗潜力。宿主因素(哺乳动物或非哺乳动物)可增强溶菌酶 E 等抗菌剂的抗菌活性。此外,使用 D-环丝氨酸增效万古霉素已成功地防治了蚕对万古霉素的耐药性感染。利用家蚕进行药物发现可以建立一种新的筛选方法,将与第三因素(无论是与宿主相关还是非宿主相关)的相互作用纳入其中,从而有望找到具有独特作用机制的抗菌药物的新途径。
Discovery of new AMR drugs targeting modulators of antimicrobial activity using in vivo silkworm screening systems.
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.
期刊介绍:
The Journal of Antibiotics seeks to promote research on antibiotics and related types of biologically active substances and publishes Articles, Review Articles, Brief Communication, Correspondence and other specially commissioned reports. The Journal of Antibiotics accepts papers on biochemical, chemical, microbiological and pharmacological studies. However, studies regarding human therapy do not fall under the journal’s scope. Contributions regarding recently discovered antibiotics and biologically active microbial products are particularly encouraged. Topics of particular interest within the journal''s scope include, but are not limited to, those listed below:
Discovery of new antibiotics and related types of biologically active substances
Production, isolation, characterization, structural elucidation, chemical synthesis and derivatization, biological activities, mechanisms of action, and structure-activity relationships of antibiotics and related types of biologically active substances
Biosynthesis, bioconversion, taxonomy and genetic studies on producing microorganisms, as well as improvement of production of antibiotics and related types of biologically active substances
Novel physical, chemical, biochemical, microbiological or pharmacological methods for detection, assay, determination, structural elucidation and evaluation of antibiotics and related types of biologically active substances
Newly found properties, mechanisms of action and resistance-development of antibiotics and related types of biologically active substances.