Suppr超能文献

对WQ-3810的研究,一种对耐氟喹诺酮类药物具有高潜力的氟喹诺酮类药物

Investigation of WQ-3810, a Fluoroquinolone with a High Potential Against Fluoroquinolone-Resistant .

作者信息

Jayaweera Sasini, Suwanthada Pondpan, Barnes David Atomanyi, Poussier Charlotte, Nishimura Tomoyasu, Hasegawa Naoki, Nishiuchi Yukiko, Thapa Jeewan, Gordon Stephen V, Kim Hyun, Nakajima Chie, Suzuki Yasuhiko

机构信息

Division of Bioresources, Hokkaido University International Institute for Zoonosis Control, Sapporo 001-0020, Japan.

Keio University Health Center, Yokohama 223-8521, Japan.

出版信息

Antibiotics (Basel). 2025 Jul 14;14(7):704. doi: 10.3390/antibiotics14070704.

Abstract

, a member of complex (MAC), is an emerging opportunistic pathogen causing MAC-pulmonary disease (PD). Fluoroquinolones (FQs), along with ethambutol (EMB) and rifampicin, are recommended for macrolide-resistant MAC-PD; however, FQ-resistant have been reported worldwide. WQ-3810 is an FQ with high potency against FQ-resistant pathogens; however, its activity against has not yet been studied. : In this study, we conducted a DNA supercoiling inhibitory assay to evaluate the inhibitory effect of WQ-3810 on recombinant wild-type (WT) and four mutant DNA gyrases of and compared the ICs of WQ-3810 with those of ciprofloxacin (CIP), levofloxacin (LVX), and moxifloxacin (MXF). In addition, we examined WQ-3810's antimicrobial activity against 11 clinical isolates, including FQ-resistant isolates, with that of other FQs. Furthermore, we assessed the synergistic action of WQ-3810 with the combination of either EMB or isoniazid (INH). : In a DNA supercoiling inhibitory assay, WQ-3810 showed 1.8 to 13.7-fold higher efficacy than LVX and CIP. In the MIC assay, WQ-3810 showed 4 to 8-fold, 2 to 16-fold, and 2 to 4-fold higher antimicrobial activity against FQ-resistant isolates than CIP, LVX, and MXF, respectively. The combination of WQ-3810 and INH exhibited a synergistic relationship. : The overall characteristics of WQ-3810 demonstrated greater effectiveness than three other FQs, suggesting that it is a promising option for treating FQ-resistant infections.

摘要

鸟分枝杆菌复合体(MAC)的成员鸟分枝杆菌是一种新兴的机会致病菌,可引起MAC肺部疾病(PD)。对于大环内酯耐药的MAC-PD,推荐使用氟喹诺酮类药物(FQs)以及乙胺丁醇(EMB)和利福平;然而,全球已报道了对FQ耐药的鸟分枝杆菌。WQ-3810是一种对FQ耐药病原体具有高效力的FQ;然而,其对鸟分枝杆菌的活性尚未得到研究。目的:在本研究中,我们进行了DNA超螺旋抑制试验,以评估WQ-3810对重组野生型(WT)和鸟分枝杆菌的四种突变DNA促旋酶的抑制作用,并将WQ-3810的半数抑制浓度(IC)与环丙沙星(CIP)、左氧氟沙星(LVX)和莫西沙星(MXF)的IC进行比较。此外,我们研究了WQ-3810对11株鸟分枝杆菌临床分离株(包括FQ耐药分离株)的抗菌活性,并与其他FQs进行比较。此外,我们评估了WQ-3810与EMB或异烟肼(INH)联合使用的协同作用。结果:在DNA超螺旋抑制试验中,WQ-3810的疗效比LVX和CIP高1.8至13.7倍。在最低抑菌浓度(MIC)试验中,WQ-3810对FQ耐药分离株的抗菌活性分别比CIP、LVX和MXF高4至8倍、2至16倍和2至4倍。WQ-3810与INH联合使用表现出协同关系。结论:WQ-3810的总体特性显示出比其他三种FQs更高的有效性,表明它是治疗FQ耐药鸟分枝杆菌感染的一个有前景的选择。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/71cf/12291913/08c8bee50b0c/antibiotics-14-00704-g001.jpg

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型,支持多种主流文档格式。

立即体验