The COVID-19 pandemic involving SARS-CoV-2 has raised interest in using antimicrobial lipid formulations to inhibit viral entry into their host cells or to inactivate them. Lipids are a part of the innate defense mechanism against pathogens. Here, we evaluated the use of nano-monocaprin (NMC) in inhibiting enveloped (phi6) and unenveloped (MS2) bacteriophages. NMC was prepared using the sonochemistry technique. Size and morphology analysis revealed the formation of ~ 8.4 ± 0.2-nm NMC as measured by dynamic light scattering. We compared the antiviral activity of NMC with molecular monocaprin (MMC) at 0.5 mM and 2 mM concentrations against phi6, which we used as a surrogate for SARS-CoV-2. The synthesized NMC exhibited 50% higher antiviral activity against phi6 than MMC at pH 7 using plaque assay. NMC inactivated phi6 stronger at pH 4 than at pH 7. To determine if NMC is toxic to mammalian cells, we used MTS assay to assess its IC for HPDE and HeLa cell lines, which were ~ 203 and 221 µM, respectively. NMC may be used for prophylactic application either as a drop or spray since many viruses enter the human body through the mucosal lining of the nose, eyes, and lungs.
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http://dx.doi.org/10.1007/s10123-022-00300-6 | DOI Listing |
J Med Chem
January 2025
State Key Laboratory of Antiviral Drugs, Pingyuan Laboratory, NMPA Key Laboratory for Research and Evaluation of Innovative Drug, School of Chemistry and Chemical Engineering, Henan Normal University, Xinxiang, Henan 453007, China.
A novel 2'-α-fluoro-2'-β--(fluoromethyl) purine nucleoside phosphoramidate prodrug has been designed and synthesized to treat SARS-CoV-2 infection. The SARS-CoV-2 central replication transcription complex (C-RTC, nsp12-nsp7-nsp8) catalyzed in vitro RNA synthesis was effectively inhibited by the corresponding bioactive nucleoside triphosphate (). The cryo-electron microscopy structure of the C-RTC: complex was also determined.
View Article and Find Full Text PDFChem Rec
January 2025
Department of Pharmacy, Banasthali Vidyapith, Rajasthan, India.
Seven-membered nitrogen-containing heterocycles, particularly azepine-based compounds, represent an intriguing class of molecules with vast arrays of applications. These compounds have garnered considerable attention in synthetic and medicinal chemistry due to their non-planar, non-aromatic features, which offer structural flexibility and diversity to design new drugs with improved pharmacological properties. This review summarizes the recent advances in the synthesis of azepine derivatives, including eco-friendly methodologies that align with the principles of green chemistry, which emphasize atom economy, sustainability, and waste reduction.
View Article and Find Full Text PDFCyclic oligonucleotide-based antiviral signaling systems (CBASS) are bacterial anti-phage defense operons that use nucleotide signals to control immune activation. Here we biochemically screen 57 diverse and phages for the ability to disrupt CBASS immunity and discover anti-CBASS 4 (Acb4) from the phage SPO1 as the founding member of a large family of >1,300 immune evasion proteins. A 2.
View Article and Find Full Text PDFThe coronavirus main protease (MPro) plays a pivotal role in viral replication and is the target of several antivirals against SARS-CoV-2. In some species, CRCs of MPro enzymatic activity can exhibit biphasic behavior in which low ligand concentrations activate the enzyme whereas higher ones inhibit it. While this behavior has been attributed to ligand-induced dimerization, quantitative enzyme kinetics models have not been fit to it.
View Article and Find Full Text PDFCureus
December 2024
Infectious Disease, Staten Island University Hospital, Staten Island, USA.
Shingles, also known as herpes zoster, is a reactivation of the chickenpox virus that causes a painful, blistering rash. After a chickenpox infection, the virus lies dormant in nerve cells. When reactivated, usually in older adults or those with weakened immune systems, it travels along nerves, typically affecting a single strip of skin called a dermatome.
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