体内生物发光成像揭示了抗利什曼病参考药物杀灭幼年利什曼病寄生虫动力学的差异。

IF 4 2区 医学 Q2 CHEMISTRY, MEDICINAL ACS Infectious Diseases Pub Date : 2024-05-11 DOI:10.1021/acsinfecdis.4c00109
Sarah Hendrickx, Pim-Bart Feijens, Fanny Escudié, Eric Chatelain, Louis Maes and Guy Caljon*, 
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引用次数: 0

摘要

利用生物发光婴儿利什曼原虫 BALB/c 小鼠模型来评估参考药物米替福新、巴龙霉素、司替葡糖酸钠和脂质体两性霉素 B 的杀寄生虫药物作用动力学。感染小鼠从感染后 7 天开始接受 5 天的治疗,并通过生物发光成像(BLI)监测寄生虫负担。通过对生物发光成像信号进行非线性回归分析,确定寄生虫在肝脏、骨髓和全身的消除半衰期(t1/2),并对不同治疗方案进行比较。在杀寄生虫动力学方面存在显著差异。单次静脉注射 0.5 毫克/千克脂质体两性霉素 B 的作用最快,t1/2 小于 1 天。事实证明,腹腔注射 320 毫克/千克的副霉素 5 天的疗效最慢,在肝脏的 t1/2 约为 5 天,在骨髓的 t1/2 为 16 天。总之,对不同抗利什曼病菌参考药物的杀灭动力学进行评估后发现,它们在消灭寄生虫的半衰期上存在显著差异。这种 BLI 方法还能对新型药物进行深入的药效学比较,并可能成为设计潜在药物组合的重要工具。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

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In Vivo Bioluminescence Imaging Reveals Differences in Leishmania infantum Parasite Killing Kinetics by Antileishmanial Reference Drugs

The bioluminescent Leishmania infantum BALB/c mouse model was used to evaluate the parasiticidal drug action kinetics of the reference drugs miltefosine, paromomycin, sodium stibogluconate, and liposomal amphotericin B. Infected mice were treated for 5 days starting from 7 days post-infection, and parasite burdens were monitored over time via bioluminescence imaging (BLI). Using nonlinear regression analyses of the BLI signal, the parasite elimination half-life (t1/2) in the liver, bone marrow, and whole body was determined and compared for the different treatment regimens. Significant differences in parasiticidal kinetics were recorded. A single intravenous dose of 0.5 mg/kg liposomal amphotericin B was the fastest acting with a t1/2 of less than 1 day. Intraperitoneal injection of paromomycin at 320 mg/kg for 5 days proved to be the slowest with a t1/2 of about 5 days in the liver and 16 days in the bone marrow. To conclude, evaluation of the cidal kinetics of the different antileishmanial reference drugs revealed striking differences in their parasite elimination half-lives. This BLI approach also enables an in-depth pharmacodynamic comparison between novel drug leads and may constitute an essential tool for the design of potential drug combinations.

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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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