The minimal inhibitory concentrations of 32 antimicrobial agents were established for 73 strains of Propionibacterium acnes and four related species (P. granulosum, P. avidum, Corynebacterium minutissimum, and C. parvum). Most strains showed good susceptibility to those agents usually considered active against gram-positive organisms. With the exception of C. minutissimum, the strains tested revealed more or less identical susceptibility ranges. The lowest minimal inhibitory concentrations were observed with benzylpenicillin, ampicillin, cephalothin, rifampin, erythromycin, clindamycin, and minocycline. C. minutissimum was more susceptible to gentamicin, sisomicin, tobramycin, and fusidic acid but more resistant to most other drugs than were the other species examined.
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http://dx.doi.org/10.1128/AAC.10.3.387 | DOI Listing |
J Med Chem
January 2025
College of Pharmacy, National & Local Joint Engineering Research Center of Targeted and Innovative Therapeutics, IATTI, Chongqing University of Arts and Sciences, Chongqing 402160, China.
The concomitant inhibition of PI3Kδ and bromodomain and extra-terminal (BET) that exerts a synergistic effect on the B-cell receptor signaling pathway provides a new strategy for the treatment of aggressive diffuse large B-cell lymphoma (DLBCL). Herein, a merged pharmacophore strategy was utilized to discover a series of thieno[3,2-]pyrimidine derivatives as the first-in-class bifunctional PI3Kδ-BET inhibitors. Through optimization, a highly potent compound () was identified to possess excellent and balanced activities against PI3Kδ [inhibitory concentration (IC) = 112 ± 8 nM] and BRD4-BD1 (IC = 19 ± 1 nM) and exhibited strong antiproliferative activities in DLBCL cells.
View Article and Find Full Text PDFToxins (Basel)
January 2025
Institute of Biomedicine, Hubei Key Laboratory of Embryonic Stem Cell Research, College of Basic Medicine, Hubei University of Medicine, Shiyan 442000, China.
Coagulation factor XIa is a new serine-protease family drug target for next-generation anticoagulants. With the snake venom Kunitz-type peptide BF9 as the scaffold, we obtained a highly active XIa inhibitor BF9-N17K in our previous work, but it also inhibited the hemostatic target plasmin. Here, in order to enhance the selectivity of BF9-N17K toward XIa, four mutants, BF9-N17K-L19A, BF9-N17K-L19S, BF9-N17K-L19D, and BF9-N17K-L19K, were further designed using the P2' amino acid classification scanning strategy.
View Article and Find Full Text PDFMetabolites
January 2025
Univ Rennes, Ecole Nationale Supérieure de Chimie de Rennes, CNRS, ISCR-UMR6226, 35000 Rennes, France.
Background/objectives: extract, obtained via microwave-enhanced extraction, was evaluated for its antioxidant, antidiabetic, and antimicrobial activities to explore its therapeutic potential.
Methods: The extraction was performed using microwave-enhanced techniques, and LC-MS/MS was employed to profile the metabolites in the extract. Total phenolic and flavonoid contents were quantified using spectrophotometric methods.
Gels
January 2025
Gene Engineering Laboratory, Feed Research Institute, Chinese Academy of Agricultural Sciences, Beijing 100081, China.
, a prevalent zoonotic pathogen, poses a significant threat to skin wound infections. This study evaluates the bactericidal efficacy of self-assembled peptide hydrogels, PPI45 and PPI47, derived from the defensin-derived peptide PPI42, against ATCC43300. The high-level preparation of PPI45 and PPI47 was achieved with yields of 1.
View Article and Find Full Text PDFJ Toxicol Environ Health A
January 2025
Department of Morphology, Federal University of Santa Maria, Santa Maria, Brazil.
This study aimed to identify chemical compounds derived from Vassobia breviflora methanolic extract using ESI-ToF-MS and their antioxidant potential activity utilizing the following methods: total phenols, DPPH, and ABTS. The MTT assay measured cytotoxic activity, while DCFH-DA and nitric oxide assays were employed to determine reactive oxygen species (ROS) and reactive nitrogen species (RNS) levels using African green monkey kidney (VERO) and human keratinocyte (HaCat) cell lines. The minimal inhibitory concentration (MIC) and minimal bactericidal concentration (MBC) were assessed in seven clinical isolates and nine ATCC strains.
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