Polyoxometalates (POMs), molecular metal oxide anions, are inorganic clusters with promising antiviral activity. Herein we report increased anti-HIV-1 activity of a POM when electrostatically combined with organic counter-cations. To this end, Keggin-type cerium tungstate POMs have been combined with organic methyl-caffeinium (Caf) cations, and their cytotoxicity, antiviral activity and mode of action have been studied. The novel compound, Caf K[β -CeSiW O ]×H O, exhibits sub-nanomolar antiviral activity and inhibits HIV-1 infectivity by acting on an early step of the viral infection cycle. This work demonstrates that combination of POM anions and organic bioactive cations can be a powerful new strategy to increase antiviral activity of these inorganic compounds.
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http://dx.doi.org/10.1002/cmdc.202100281 | DOI Listing |
Mol Divers
January 2025
Department of Pharmacy, Fujian Medical University Union Hospital, Fuzhou, 350001, Fujian, China.
Influenza is a highly contagious respiratory illness that imposes a significant global burden. Antiviral neuraminidase inhibitors (NAIs) such as oseltamivir (OC) have been proven essential, but the emergence of resistant viral strains necessitates the development of novel therapies. This study explored the potential of natural products as alternative NAIs.
View Article and Find Full Text PDFChem Biodivers
January 2025
Shaanxi University of Chinese Medicine, school of pharmacry, shiji Ave., 712046, xianyang, CHINA.
Phillyrin (PHI) is one of the main active components in Forsythia suspensa (Thunb.) Vahl, belonging to the class of lignans, which has anti-inflammatory, antioxidant, anti-tumor, antiviral, antibacterial, weight loss and other pharmacological effects, involving a variety of potential signaling pathways, such as TLR, NF-κB, PI3K/AKT, NRF2, PPAPs signaling pathways. The review search systematically and comprehensively CNKI, Wanfang, PubMed, Web of Science and other databases, screened nearly 100 relevant literature in the past five years, and summarized and evaluated the information of PHI extraction and purification, pharmacological activity, potential mechanism and structure-activity relationship.
View Article and Find Full Text PDFClin Pharmacol Ther
January 2025
Gilead Sciences, Inc., Foster City, California, USA.
Obeldesivir is an oral nucleoside analog prodrug inhibitor of SARS-CoV-2 RNA-dependent RNA polymerase and other viral polymerases. Here, two Phase I studies evaluated potential drug-drug interactions between obeldesivir and substrates or inhibitors of cytochrome P450 and drug transporters in healthy participants. When obeldesivir was tested as a precipitant, pharmacokinetic parameter point estimates for midazolam (CYP3A4 inhibition/induction), caffeine (CYP1A2 inhibition), and metformin (organic cation transporter 1 inhibition) exposures were within 80-125% no-effect bounds representing the interval within which a systemic exposure change does not warrant clinical action based on EMA/FDA guidance.
View Article and Find Full Text PDFJ Virol
January 2025
Institute for Medical Virology and Epidemiology of Viral Diseases, University Hospital Tübingen, Tübingen, Germany.
The human genome is like a museum of ancient retroviral infections. It contains a large number of endogenous retroviruses (ERVs) that bear witness to past integration events. About 5,000 of them are so-called long terminal repeat 12 (LTR12) elements.
View Article and Find Full Text PDFJ Med Chem
January 2025
Graduate School of Pharmaceutical Sciences, Kyoto University, Sakyo-ku, Kyoto 606-8501, Japan.
Measles is a highly infectious disease and remains a major cause of childhood mortality worldwide. In some cases, the measles virus (MV) induces subacute sclerosing panencephalitis within several years of the acute infection. The infection of the target cells by MV is mediated by the F protein, in which two heptad repeat regions, HR1 and HR2, form a six-helix bundle before membrane fusion.
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