利用自体外泌体强力霉素克服空泡屏障靶向抑制细胞内伯纳氏杆菌

IF 4.5 2区 医学 Q2 CHEMISTRY, MEDICINAL
ACS Infectious Diseases Pub Date : 2026-10-09 Epub Date: 2026-09-16 DOI:10.1021/acsinfecdis.6c00459
Yuchen Zhang, Xiaoxiao Chen, Jinru Lin, Jun Jiao, Yonghui Yu, Wenbo Wei, Shan Zhang, Yufei Jiang, Yinhui Lin, Ziyuan Zhang, Shaoya Liu, Hui Yue, Xuan OuYang, Yajun Song
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引用次数: 0

摘要

伯纳氏克希菌是Q热的病原体,是一种专性细胞内细菌,在含克希菌液泡(CCV)内复制,CCV是一种溶酶体样的隔室。CCV内的酸性微环境损害了弱碱性抗生素(如强力霉素)的活性,需要长时间的高剂量治疗。为了克服这一基本的递送障碍,我们设计了一个仿生纳米平台,通过将多西环素(DOX)包裹在THP-1细胞衍生的巨噬细胞(tExo)的外泌体中。DOX@tExo纳米颗粒显示出独特的外泌体形态和蛋白质标记,并在体外和体内均表现出良好的生物相容性。重要的是,DOX@tExo被巨噬细胞有效地内化,特异地运输到溶酶体,并在ccv中积累。这种精确靶向导致抗菌效力增强,将抑制细胞内细菌生长的最低有效浓度降低至0.015 μg/mL,比游离DOX低一个数量级以上。除了直接给药之外,DOX@tExo治疗还同时减少了自噬性的药物递送,正如p62积累减少所表明的那样,从而潜在地破坏了病原体选择的宿主过程。在小鼠肺部感染模型中,DOX@tExo治疗显著减少了多个器官的细菌负担。总的来说,这项工作建立了来自THP-1细胞的同源外泌体平台,该平台结合了靶向抗生素递送和宿主定向免疫调节,为治疗难治性细胞内细菌感染提供了一种治疗策略。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Targeted Inhibition of Intracellular Coxiella burnetii by Overcoming the Vacuolar Barrier with Autologous Exosomal Doxycycline

Coxiella burnetii, the causative agent of Q fever, is an obligate intracellular bacterium that replicates within the Coxiella-containing vacuole (CCV), a lysosome-like compartment. The acidic microenvironment within the CCV impairs the activity of weak-base antibiotics such as doxycycline, necessitating prolonged, high-dose therapy. To overcome this fundamental delivery barrier, we engineered a biomimetic nanoplatform by encapsulating doxycycline (DOX) within exosomes derived from THP-1 cell-derived macrophages (tExo). DOX@tExo nanoparticles displayed characteristic exosomal morphology and protein markers and demonstrated favorable biocompatibility both in vitro and in vivo. Importantly, DOX@tExo were efficiently internalized by macrophages, trafficked specifically to lysosomes, and accumulated within CCVs. This precise targeting resulted in an enhancement of antibacterial potency, reducing the minimal effective concentration for marked inhibition of intracellular bacterial growth to 0.015 μg/mL, more than an order of magnitude lower than that of free DOX. Beyond direct drug delivery, DOX@tExo treatment concurrently reduced autophagic cargo delivery, as indicated by decreased p62 accumulation, thereby potentially disrupting a host process coopted by the pathogen. In a murine model of pulmonary infection, DOX@tExo treatment significantly reduced bacterial burdens in multiple organs. Collectively, this work establishes a homologous exosome platform derived from THP-1 cells that combines targeted antibiotic delivery with host-directed immunomodulation, offering a therapeutic strategy against refractory intracellular bacterial infections.

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来源期刊
ACS Infectious Diseases
ACS Infectious Diseases CHEMISTRY, MEDICINALINFECTIOUS DISEASES&nb-INFECTIOUS DISEASES
CiteScore
9.70
自引率
3.80%
发文量
213
期刊介绍: ACS Infectious Diseases will be the first journal to highlight chemistry and its role in this multidisciplinary and collaborative research area. The journal will cover a diverse array of topics including, but not limited to: * Discovery and development of new antimicrobial agents — identified through target- or phenotypic-based approaches as well as compounds that induce synergy with antimicrobials. * Characterization and validation of drug target or pathways — use of single target and genome-wide knockdown and knockouts, biochemical studies, structural biology, new technologies to facilitate characterization and prioritization of potential drug targets. * Mechanism of drug resistance — fundamental research that advances our understanding of resistance; strategies to prevent resistance. * Mechanisms of action — use of genetic, metabolomic, and activity- and affinity-based protein profiling to elucidate the mechanism of action of clinical and experimental antimicrobial agents. * Host-pathogen interactions — tools for studying host-pathogen interactions, cellular biochemistry of hosts and pathogens, and molecular interactions of pathogens with host microbiota. * Small molecule vaccine adjuvants for infectious disease. * Viral and bacterial biochemistry and molecular biology.
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