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Novel methyldithiocarbazate derivatives as NDM-1 inhibitors to combat multidrug-resistant bacterial infection with β-lactams.
Bioorg Chem
December 2024
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. Electronic address:
Given the ever-evolving landscape of antimicrobial resistance, the emergence of New Delhi metallo-β-lactamase-1 (NDM-1) has introduced a formidable challenge to global public health. In previous research, we identified the Compound Zndm19 as an NDM-1 inhibitor and reported Zndm19 derivatives, which exhibited moderate antibacterial activity when combined with meropenem (MEM). This moderate activity may have been due to the inability of Zndm19 to efficiently penetrate the bacterial outer membrane or its susceptibility to hydrolysis, which prevented it from exerting strong enzyme inhibition in synergy with bacterial cells.
View Article and Find Full Text PDFReV as a Novel S. cerevisiae-Derived Drug Carrier to Enhance Anticancer Therapy through Daunorubicin Delivery.
Appl Biochem Biotechnol
December 2024
Graduate School of Semiconductor and Chemical Engineering, Jeonbuk National University, 567 Baekje-Daero, Deokjin-Gu Jeonju, Jeonbuk, 54896, South Korea.
This study explores the potential of vacuoles derived from Saccharomyces cerevisiae (S. cerevisiae) as a novel form of drug carrier, specifically focusing on their application in enhancing the delivery of the chemotherapeutic agent Daunorubicin (DNR). We isolated and reassembled these vacuoles, referred to as Reassembled Vacuoles (ReV), aiming to overcome the challenges of drug degradation caused by hydrolytic enzymes within traditional vacuoles.
View Article and Find Full Text PDFParaoxonase 1 ameliorates neurological symptoms and motor coordination impairment caused by cerebral ischemia-reperfusion injury.
Biomed Pharmacother
December 2024
Research Division, Mitsubishi Tanabe Pharma Corporation, 1000, Kamoshida-cho, Aoba-ku, Yokohama-shi, Kanagawa 227-0033, Japan. Electronic address:
Article Synopsis
- HDL (high-density lipoprotein) has protective effects against cerebral infarction due to its antioxidant, anti-inflammatory, and antithrombotic properties, but there's a lack of effective clinical treatments.
- Researchers focused on paraoxonase 1 (PON1), an enzyme linked to HDL, to develop it as a new therapy for ischemia-reperfusion injury in stroke.
- The study found that PON1 can effectively bind to HDL, reduce infarct volume in a mouse model, and improve neurological function, suggesting its potential as a treatment for acute stroke.
Glucosinolates and Their Hydrolytic Derivatives: Promising Phytochemicals With Anticancer Potential.
Phytother Res
December 2024
Department of Clinical Pharmacy, University of Medicine and Pharmacy of Craiova, Craiova, Romania.
Recent research has increasingly focused on phytochemicals as promising anticancer agents, with glucosinolates (GSLs) and their hydrolytic derivatives playing a central role. These sulfur-containing compounds, found in plants of the Brassicales order, are converted by myrosinase enzymes into biologically active products, primarily isothiocyanates (ITCs) and indoles, which exhibit significant anticancer properties. Indole-3-carbinol, diindolylmethane, sulforaphane (SFN), phenethyl isothiocyanate (PEITC), benzyl isothiocyanate, and allyl isothiocyanate have shown potent anticancer effects in animal models, particularly in breast, prostate, lung, melanoma, bladder, hepatoma, and gastrointestinal cancers.
View Article and Find Full Text PDFThe endocannabinoid system in the brain undergoes long-lasting changes following neuropathic pain.
iScience
December 2024
Department of Neurobiology and Collaborative Innovation Center for Brain Science, School of Basic Medicine, The Fourth Military Medical University, Xi'an 710032, China.
The endocannabinoid system (ECS), which is composed of endocannabinoids (eCBs), cannabinoid receptors (CBRs), and associated signaling molecules, has been identified within the brain. In neuropathic pain animal models and patients, long-lasting alterations in the ECS have been observed. These changes of neurons and glial cells in the ECS contribute to the modulation of neuropathic pain.
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