Quinolone antibiotics pose a threat to health and the environment due to their difficulty in decomposition and misuse. A novel fluorescence composite material CQD_x@Co/Mn-MOF has been developed, which uses cobalt (Co) and manganese (Mn) as metal centers and 1,3,5-triazobenzene as organic ligands. Meaningfully, CQD_x@Co/Mn-MOF can be designed as a ratiometric fluorescence sensor for detecting quinolone antibiotics, especially norfloxacin (NFX). In a series of CQD_x@Co/Mn-MOF, CQD_6μL@Co/Mn-MOF sensor exhibits good linearity within the NFX concentration range of 1-4 × 10^-5 M, with a detection limit of 0.70 μM. Compared with Co/Mn-MOF, introducing CQDs significantly reduces the detection limit from 3.50 μM to 0.70 μM and increases the detection sensitivity by five times. The CQD_6μL@Co/Mn-MOF sensor exhibits fast response time (2 s), high selectivity and sensitivity to NFX, making it an ideal ratiometric fluorescent sensor for the detection of these antibiotics. Based on its excellent detection performance, the sensor was further applied to the quantitative determination of NFX in chicken, beef and honey samples and satisfactory results were obtained with recoveries ranging from 97.51 % to 108.60 %. In addition, based on CQD_6μL@Co/Mn-MOF test strips, convenient and real-time detection of quinolone antibiotics has been achieved. In conclusion, the CQD_6μL@Co/Mn-MOF ratiometric fluorescent sensor provides a reliable, sensitive and efficient analytical method for the detection and evaluation of trace NFX in food, which is of great significance for ensuring food safety and public health.

2025-05-01·European Journal of Medicinal Chemistry

Naturally inspired chimeric quinolone derivatives to reverse bacterial drug resistance

Article

作者: Wang, Kairong ; Xie, Junqiu ; Xiang, Yanghui ; Zhang, Ying ; Teng, Peng ; He, Yuhang ; Wang, Luyao ; Ren, Yixuan ; Chi, Jiaying ; Chen, Kang ; Chen, Wenteng ; Zhu, Qi ; Wen, Qi ; Niu, Xiaoke ; Lin, Juncheng ; Wang, Bo ; Zhou, Ruhong ; Yang, Yanqing ; Wang, Baohong ; Lu, Chao ; Yu, Yongping

Antimicrobial resistance poses an urgent threat to global health, underscoring the critical need for new antibacterial drugs. Ciprofloxacin, a third-generation quinolone antibiotic, is used to treat different types of bacterial infections; however, it often results in the rapid emergence of resistance in clinical settings. Inspired by low susceptibility to antimicrobial resistance of natural antimicrobial peptides, we herein propose a host defense peptide-mimicking strategy for designing chimeric quinolone derivatives which may reduce the likelihood of antibacterial resistance. This strategy involves the incorporation of deliberately designed amphiphilic moieties into ciprofloxacin to mimic the structural characteristics and resistance-evading properties of host defense peptides. A resulting chimeric compound IPMCL-28b, carrying a rigid linker and three cationic amino acids along with a lipophilic acyl n-decanoyl tail, exhibited potent activity against a panel of multidrug-resistant bacterial strains by endowing the ciprofloxacin derivatives with additional ability to disrupt bacterial cell membranes. Molecular dynamics simulations showed that IPMCL-28b demonstrates significantly stronger disruptive interactions with cell membranes than ciprofloxacin. This compound not only demonstrated high selectivity with low hemolysis side effect, but also significantly reduced the likelihood of resistance development compared with ciprofloxacin. Excitingly, IPMCL-28b demonstrated highly enhanced in vivo antimicrobial activity against methicillin-resistant Staphylococcus aureus (MRSA) with a 99.99 % (4.4 log) reduction in skin bacterial load after a single dose. These findings highlight the potential of host defense peptides-mimicking amphiphilic ciprofloxacin derivatives to reverse antibiotic resistance and mitigate the development of antimicrobial resistance.

2025-05-01·Journal of Colloid and Interface Science

Floating BiOBr/Ti3C2 aerogel spheres for efficient degradation of quinolone antibiotics: Rapid oxygen transfer via triphase interface and effective charges separation by internal electric field

Article

作者: Sun, Jing ; Yang, Wenhao ; Tong, Zhangfa ; Huang, Ting ; Wang, Linxing ; Xu, Zisong ; Zhang, Hanbing ; Liu, Kun ; Fu, Tian

The limited transport of oxygen at the solid-liquid interface and the poor charge separation efficiency of single catalyst significantly impedes the generation of reactive oxygen species (ROS), thereby weakening the application potential of photocatalytic technology in water pollution control. Herein, a hollow porous photocatalytic aerogel sphere (calcium alginate/cellulose nanofibers (CA/CNF)) loaded BiOBr/Ti₃C₂, combining a favourable mass transfer structure with effective catalytic centers was firstly presented. The floatability and hollow pore structure facilitated rapid O₂ transfer via a triphase interface, thereby promoting the generation of ROS. The oxygen diffusion flux of aerogel spheres' upper surface in triphase system exhibited a 0.151 μmol·(m²·S)^-1 increase compared to that of the diphase one based on Finite element simulation (FEM). Furthermore, owing to the regulation of charge spatial distribution by Schottky junction of BiOBr/Ti₃C₂, internal electric field (IEF) of CA/CNF@BiOBr/Ti₃C₂ achieved 1.8-fold improvement compared with CA/CNF@BiOBr, thus enhancing the separation of photogenerated charges. Accordingly, the degradation efficiency and catalytic rate constant of moxifloxacin (MOX) by CA/CNF@BiOBr/Ti₃C₂ in triphase system have improved by 20.1% and 1.5 times compared to those of diphase system, respectively. Moreover, the potential to mineralize multiple quinolone antibiotics (FQs), high resistance to complex water disturbances and excellent stability were revealed in CA/CNF@BiOBr/Ti₃C₂. Besides, the triphase system based on CA/CNF@BiOBr/Ti₃C₂ confirmed the potential for large-scale water treatment application in 500 mL MOX circular flow, reaching 90% MOX removal within 120 min. This research clarifies the oxygen mass transfer mechanism and pathways to the enhanced ROS production in a triphase system, and provides new insights into designing efficient floatable photocatalyst and adaptive reaction devices for new pollutants remediation.

项与 Quinolone antibiotics(Compound 73 ）相关的新闻（医药）

2024-12-05

·ntcpharma.com

Positive results of the Phase II Mirakle study

NTC presents positive results from Phase II Mirakle study evaluating an innovative drug for bacterial conjunctivitis Milan, December 5, 2024 – NTC, an international R&D focused pharmaceutical company headquartered in Italy, presents positive results from Phase II MIRAKLE study, a multicentre, randomized, blinded-assessor, phase II non-inferiority study evaluating the efficacy and tolerability of NTC014 (quinolone antibiotic + NSAID in eye drops solution) in the treatment of bacterial conjunctivitis in adults. Despite NTC014, due to its simplified therapeutic regimen, has been administered at a lower posology than the antibiotic comparator –25% of less antibiotic administered - the main results showed the non-inferiority of NTC014 eye drops vs antibiotic alone in microbiological eradication, with unexpected efficacy results even against pathogens classified as Intermediate or Resistant to the quinolone antibiotic under study. “These interim findings reaffirm that NTC014 is eligible to be a new treatment for bacterial conjunctivitis”, Alessandro Colombo, Chief Scientific Officer, NTC, states. “We aim at demonstrating with robust clinical evidence value and potential for NTC014, considering also that this drug responds to our mission to contribute to fighting antibiotic resistance by using less antibiotics, for a shorter treatment duration with no limitation of usage, also in case of non-confirmation of bacterial etiology.” “We are encouraged by the overall results of the Mirakle study”, says Riccardo Carbucicchio, Chief Executive Officer in NTC, “NTC 014 is first in class combination worldwide of an antibiotic and an NSAID. Given the significant unmet medical need, NTC014 aims to provide physicians with an effective treatment for moderate-severe bacterial conjunctivitis, a common eye infection. We believe that NTC 014 has a great potential and we aim to finalize the commercial partnering for this asset in most countries of the world before end of 2025. We do not exclude to develop this asset for surgical use too”. Conjunctivitis is a common disease in Western Countries and imposes economic and social burdens. Viral conjunctivitis is the most common cause of infectious conjunctivitis both overall and in the adult population, bacterial conjunctivitis is the second most common cause and is responsible for the majority (50%-75%) of cases in children. NTC has already successfully developed and launched the first combination of a quinolone and steroid for post cataract surgery, licensed in almost 90 countries and currently marketed in 60 countries, in Europe, Asia, Americas and Africa. About NTC A pharmaceutical company headquartered in Milan - Italy, with distributors and partners in more than 100 countries, engaged in research, development, registration, and commercialization of drugs, medical devices, and food supplements in ophthalmology, and other therapeutic areas including pediatrics, gynecology, and gastroenterology. NTC offers more than 200 partners innovative and high quality standard pharmaceutical products. For more information, please visit www.ntcpharma.com

临床2期临床结果上市批准

2024-09-24

·ntcpharma.com

Cataract surgery: the fixed-dose combination of an antibiotic with an anti-inflammatory drug in eye drops is currently available in 50 countries worldwide

The combination has been registered in nearly 60 countries for the prevention and treatment of inflammation and the prevention of infection associated with cataract surgery in adults. It is currently marketed in 50 countries worldwide. Cataracts are a degenerative disease of the lens of the eye, the age limit for which is constantly decreasing. If not properly treated, cataracts can lead to discomfort, and visual impairment, and even blindness. Currently, cataract surgery is the only effective treatment and the most prevalent surgical procedure of all medical specialties with an estimated 20 million cases per year worldwide. Despite updated guidelines, many ophthalmologists use protocols for postoperative management based primarily on their personal experience. In this context, providing new scientific evidence can give ophthalmologists new opportunities for choice. The LEADER7 study, a multicentre, randomized, blinded-assessor, international phase 3 parallel group clinical trial involving more than 800 patients in over 50 centres, demonstrated that one-week course of the fixed combination of an ophthalmic quinolone antibiotic with an anti-inflammatory steroid is sufficient to resolve inflammation and prevent infection in patients undergoing cataract surgery. The reduction in post-surgery treatment from 14 to 7 days on the one hand gives the opportunity to optimize the use of corticosteroids and hence reduce their side-effects, and on the other hand to reduce the exposure to antibiotics and, therefore, reduce the probability of the emergence of antibiotic resistance. Finally, the shorter duration of treatment, along with the convenience of having both active ingredients in the same solution, represents an important element in improving adherence to therapy for patients undergoing cataract surgery, who are generally elderly. In the next nine months, we expect approval and launch in almost ten additional new countries, and we are submitting applications for approval in a further 12 countries. In 2025 we expect approval in 3 countries.

临床3期临床结果

100 项与 Quinolone antibiotics(Compound 73 ）相关的药物交易

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