The narrow therapeutic/toxic ratio of existing aminoglycosides has led to a search for safer drugs of this class. Isepamicin is a semi-synthetic aminoglycoside with a significantly low nephro as well as ototoxicity in animals and which is expected to have a clinical efficacy comparable to that of amikacin. We therefore compared its antibacterial activity with amikacin against 817 recent clinical isolates of gram-positive and gram-negative bacteria. The in vitro activity of isepamicin was comparable or slightly greater than amikacin against Staphylococcus aureus and most Enterobacteriaceae. However, it was significantly more inhibitory towards Serratia marcescens, Enterobacter and Klebsiella pneumoniae.
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http://dx.doi.org/10.1159/000239319 | DOI Listing |
J Med Chem
January 2025
Inner Mongolia Key Laboratory for Molecular Regulation of the Cell, Inner Mongolia University, Hohhot 010021, People's Republic of China.
In this study, we synthesized 12 monofunctional tridentate ONS-donor salicylaldimine ligand ()-based Ru(II) complexes with general formula [(Ru()(-cymene)]·Cl (-), characterized by H NMR, C NMR, UV, FT-IR spectroscopy, HR-ESI mass spectrometry, and single-crystal X-ray analysis showing ligand's orientation around the Ru(II) center. All 12 of these 12 complexes were tested for their anticancer activities in multiple cancer cells. The superior antitumor efficacy of , , and was demonstrated by reduced mitochondrial membrane potential, impaired proliferative capacity, and disrupted redox homeostasis, along with enhanced apoptosis through caspase-3 activation and downregulation of Bcl-2 expression.
View Article and Find Full Text PDFJ Med Chem
January 2025
College of Chemistry, Zhengzhou University, Zhengzhou 450001, China.
The P2YR is activated by UDP and UDP glucose and is involved in many human inflammatory diseases. Based on the molecular docking analysis of currently reported P2YR antagonists and the crystallographic overlap study between PPTN and compound , a series of 3-substituted 5-amidobenzoate derivatives were designed, synthesized, and identified as promising P2YR antagonists. The optimal compound (methyl 3-(1-benzo[]imidazol-2-yl)-5-(2-(-tolyl) acetamido)benzoate, IC = 0.
View Article and Find Full Text PDFMol Carcinog
January 2025
Department of Neurosurgery, Huanggang Central Hospital of Yangtze University, Huanggang, China.
Glioblastoma (GBM) is the most common malignant primary brain tumor, with a mean survival of less than 2 years. Unique brain structures and the microenvironment, including blood-brain barriers, put great challenges on clinical drug development. Sophoricoside (Sop), an isoflavone glycoside isolated from seeds of Sophora japonica L.
View Article and Find Full Text PDFBiomater Sci
January 2025
School of Chemistry, Chemical Engineering and Life Science, Hubei Key Laboratory of Nanomedicine for Neurodegenerative Diseases, Wuhan University of Technology, 122 Luoshi Road, Wuhan 430070, China.
To enhance the antibacterial efficacy of tildipirosin against (S.A.) infections, optimized solid lipid nanoparticles loaded with tildipirosin (SLN-TD) were developed, using docosanoic acid (DA), octadecanoic acid (OA), hexadecanoic acid (HA), and tetradecanoic acid (TA) as lipid components.
View Article and Find Full Text PDFHum Mol Genet
January 2025
Department of Cell & Developmental Biology, Vanderbilt University School of Medicine, 1161 21st Ave S, Nashville, Tennessee, 37232, United States of America.
Tuberous Sclerosis Complex (TSC) is a debilitating developmental disorder characterized by a variety of clinical manifestations. While benign tumors in the heart, lungs, kidney, and brain are all hallmarks of the disease, the most severe symptoms of TSC are often neurological, including seizures, autism, psychiatric disorders, and intellectual disabilities. TSC is caused by loss of function mutations in the TSC1 or TSC2 genes and consequent dysregulation of signaling via mechanistic Target of Rapamycin Complex 1 (mTORC1).
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