Development of bioceramics with antibacterial activity and without cytotoxicity would be beneficial for preventing infection associated with implants. This study aimed to capitalize on the antibacterial properties of silver (Ag) incorporated in or coexisting in metallic form with calcium phosphates (CaPs). The in vitro dissolution behavior, antibacterial activity, and cytotoxicity of Ag-containing CaPs with different phase fractions of hydroxyapatite (HA) and β-tricalcium phosphate (β-TCP) were evaluated. The antibacterial activity of Ag-containing CaPs depended on the main phase of CaP, the chemical state of Ag, and the amount of incorporated Ag. Superior antibacterial activity was obtained from sustained release of Ag ions through continuous dissolution of Ag-incorporated β-TCP compared to that obtained for HA coexisting with metallic Ag particles. Ag-containing CaPs did not exhibit any toxic effect on V79 fibroblasts. Thus, these results demonstrated the effectiveness of Ag-incorporated β-TCP in preventing infection, with respect to long-term applications.
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http://dx.doi.org/10.1016/j.msec.2017.02.059 | DOI Listing |
Sci Rep
December 2024
Laboratory of Bioinorganic Chemistry, Department of Pharmacy and Biotechnology, University of Bologna, 40127, Bologna, Italy.
This manuscript details the application of Isothermal Titration Calorimetry (ITC) to characterize the kinetics of 3CL, the main protease from the Severe Acute Respiratory Syndrome CoronaVirus-2 (SARS-CoV-2), and its inhibition by Ensitrelvir, a known non-covalent inhibitor. 3CL is essential for producing the proteins necessary for viral infection, which led to the COVID-19 pandemic. The ITC-based assay provided rapid and reliable measurements of 3CL activity, allowing for the direct derivation of the kinetic enzymatic constants K and k by monitoring the thermal power required to maintain a constant temperature as the substrate is consumed.
View Article and Find Full Text PDFBMJ Open
December 2024
Infectious Diseases Institute, Makerere University College of Health Sciences, Kampala, Central, Uganda.
Introduction: Tuberculosis (TB) is the leading infectious cause of death globally. Despite WHO recommendations for TB preventive therapy (TPT), challenges persist, including incompletion of treatment and adverse drug reactions (ADRs). There is limited data on the 3-month isoniazid and rifapentine (3HP) pharmacokinetics, pharmacogenomics and their relation with ADRs.
View Article and Find Full Text PDFInt J Biol Macromol
December 2024
School of Mechanical Engineering, Jiangnan University, Wuxi, Jiangsu 214122, China; Jiangsu Key Laboratory of Advanced Food Manufacturing Equipment Technology, Jiangnan University, Wuxi, Jiangsu 214122, China.
The antioxidant activity of ε-polylysine (EPL) can be enhanced by grafting phenolic compound caffeic acid (CA) onto its amino groups. To enhance the antioxidant activity of EPL, this study synthesized caffeic acid-ε-polylysine conjugate (CA-EPL) by grafting CA onto EPL using carbodiimide coupling reaction. Fourier transform infrared spectroscopy, H nuclear magnetic resonance (NMR) spectroscopy confirmed the successful conjugation of caffeic acid and ε-polylysine.
View Article and Find Full Text PDFBioorg Chem
December 2024
Department of Pharmaceutical Chemistry, KLE College of Pharmacy, Belagavi, KLE Academy of Higher Education and Research, Belagavi 590 010, Karnataka, India.
Indole, a fundamental heterocyclic core, has emerged as a cornerstone in the medicinal chemistry due to its diverse biological activities and structural versatility. This aromatic compound, present in natural as well as synthetic compounds, offers a versatile platform for the drug discovery. By strategically incorporating functional groups or pharmacophores, researchers can tailor indole-derivatives to target a wide range of diseases.
View Article and Find Full Text PDFProc Natl Acad Sci U S A
January 2025
Department of Biochemistry, University of Illinois, Urbana, IL 61801.
Infections caused by gram-negative pathogens continue to be a major risk to human health because of the innate antibiotic resistance endowed by their unique cell membrane architecture. Nature has developed an elegant solution to target gram-negative strains, namely by conjugating toxic antibiotic warheads to a suitable carrier to facilitate the active import of the drug to a specific target organism. Microcin C7 (McC) is a Trojan horse peptide-conjugated antibiotic that specifically targets enterobacteria by exploiting active import through oligopeptide transport systems.
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