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Discovery of Metabolic Reprogramming 2-Quinolones as Effective Antimicrobials for MRSA-Infected Wound Therapy.

J Med Chem

January 2025

State Key Laboratory for Diagnosis and Treatment of Severe Zoonotic Infectious Diseases, Key Laboratory for Zoonosis Research of the Ministry of Education, Institute of Zoonosis, and College of Veterinary Medicine, Jilin University, Changchun 130062, China.

To date, the abuse of antibiotics and a gradual decline in novel antibiotic discovery enlarge the threat of drug-resistant bacterial infections, especially methicillin-resistant (MRSA). Herein, inspired by the unique structures and antibacterial activities of 2-quinolones, a class of novel 2-quinolones with substituted pyridines was synthesized. Notably, compound , the derivative with a methylpyridine fragment, showed potent antibacterial and antibiofilm activities, especially for MRSA strains (MIC = 0.

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Introduction: Wound treatment is a significant health burden in any healthcare system, which requires proper management to minimize pain and prevent bacterial infections that can complicate the wound healing process.

Rationale: There is a need to develop innovative therapies to accelerate wound healing cost-effectively. Herein, two polymer-based nanofibrous systems were developed using poly-lactic-co-glycolic-acid (PLGA) and polyvinylpyrrolidone (PVP) loaded with a combination of an antibiotic (Fusidic acid, FA) and a local anesthetic (Lidocaine, LDC) via electrospinning technique for an expedited healing process by preventing bacterial infections while reducing the pain sensation.

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Purpose: Gastrostomy is the commonly used enteral feeding technology. The clinical risks caused by tube dislodgement and peristomal site infection are the common complications before complete tract maturation after gastrostomy. However, there is currently no relevant research to promote gastrostomy wound treatment and tract maturation.

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Click chemistry-enabled gold nanorods for sensitive detection and viability evaluation of copper(II)-reducing bacteria.

Mater Today Bio

February 2025

Department of Laboratory Medicine, Zhongshan Hospital, Fudan University, 136 Yi Xue Yuan Road, Shanghai, 200032, PR China.

The rise of antibiotic resistance poses a significant and ongoing challenge to public health, with pathogenic bacteria remaining a persistent threat. Traditional culture methods, while considered the gold standard for bacterial detection and viability assessment, are time-consuming and labor-intensive. To address this limitation, we developed a novel point-of-care (POC) detection method leveraging citrate- and alkyne-modified gold nanorods (AuNRs) synthesized with click chemistry properties.

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Background: Doxorubicin (DOX) is a potent chemotherapeutic agent for breast cancer, but its effectiveness is often diminished by resistance mechanisms, particularly through p-glycoprotein (P-gp) mediated drug efflux. Clarithromycin (CAM), a macrolide antibiotic, inhibits multiple metabolic pathways including CYP3A and P-gp, potentially countering DOX resistance.

Objective: This study aimed to evaluate the potentiation of DOX and its effectiveness against the MCF-7 breast cancer cell line by encapsulating both DOX and CAM in PEGylated liposomes.

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