People throughout the world continue to be at risk for death from influenza A virus, which is always creating a new variant. Here we present a new effective and specific anti-influenza viral neuraminidase (viNA) inhibitor, 9-cyclopropylcarbonylamino-4-guanidino-Neu5Ac2en (cPro-GUN). Like zanamivir, it is highly effective against N1-N9 avian and N1-N2 human viNAs, including H274Y oseltamivir-resistant N1 viNA, due to its C-6 portion still being anchored in the active site, different from the disruption of oseltamivir's C-6 anchoring by H274Y mutation. Unlike zanamivir, no sialidase inhibitory activity has been observed for cPro-GUN against huNeu1-huNeu4 enzymes. Broad efficacy of cPro-GUN against avian and human influenza viruses in cell cultures comparable to its sialidase inhibitory activities makes cPro-GUN ideal for further development for safe therapeutic or prophylactic use against both seasonal and pandemic influenza.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1021/acs.jmedchem.5b01863 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Phlorotannin-Rich Seaweed Extract Inhibits Influenza Infection.
Viruses
December 2024
Institute of Infection, Veterinary and Ecological Sciences, University of Liverpool, Liverpool L3 5RF, UK.
Seaweed-derived compounds are a renewable resource utilised in the manufacturing and food industry. This study focuses on an enriched seaweed extract (ESE) isolated from The ESE was screened for antiviral activity by plaque reduction assays against influenza A/Puerto Rico/8/1934 H1N1 (PR8), A/X-31 H3N2 (X31) and A/England/195/2009 H1N1 (Eng195), resulting in the complete inhibition of infection. Time of addition assays and FACS analysis were used to help determine the modes of action.
View Article and Find Full Text PDFEnzyme Inhibitory, Physicochemical, and Phytochemical Properties and Botanical Sources of Honey, Bee Pollen, Bee Bread, and Propolis Obtained from the Same Apiary.
Antioxidants (Basel)
December 2024
Department of Chemistry and Biochemistry, Faculty of Agriculture, University of Belgrade, 11080 Belgrade, Serbia.
Bee products are an important source of nutrients and bioactive phytochemicals. This study aimed to determine the chemical composition (proximate composition, general phytochemical composition, sugar, and phenolic profiles) of four different products (honey, bee pollen, bee bread, and propolis), obtained from the same apiary, as well as to assess their biological activity through antioxidant and enzyme inhibition assays (α-amylase, α-glucosidase, lipase, AchE, neuraminidase, angiotensin-converting enzyme, urease, trypsin, tyrosinase, carbonic anhydrase, thioredoxin reductase, adenosine deaminase). Clear differences were observed among the samples in terms of both chemical composition and biological activity.
View Article and Find Full Text PDFIn vitro neuraminidase inhibitory concentrations (IC) of four neuraminidase inhibitors in the Japanese 2023-24 season: Comparison with the 2010-11 to 2022-23 seasons.
J Infect Chemother
December 2024
Japan Physicians Association, Tokyo, Japan; Ricerca Clinica Co., Fukuoka, Japan.
Introduction: To assess the susceptibility of epidemic influenza viruses to the four most used neuraminidase inhibitors (NAIs) during the 2023-24 influenza season in Japan, we measured the 50% inhibitory concentration (IC) of oseltamivir, peramivir, zanamivir, and laninamivir in virus isolates from the sample of 100 patients.
Methods: Viral isolation was done using specimens obtained before and after treatment, with the type/subtype determined by RT-PCR using type- and subtype-specific primers. IC values were determined by a neuraminidase inhibition assay using a fluorescent substrate.
Pharmacologic background and clinical issue of anti-influenza drugs.
Fukushima J Med Sci
December 2024
Department of Pediatrics, Fukushima Medical University.
Since 2000, rapid antigen detection kits and anti-influenza drugs have been used for the early diagnosis and treatment of influenza in Japan, respectively. The main drugs available in clinical practice are the neuraminidase inhibitors oseltamivir, zanamivir, laninamivir, and peramivir, as well as the cap-dependent endonuclease inhibitor baloxavir marboxil. Antiviral therapy with neuraminidase inhibitors has been practiced for many years, especially in Japan; it can shorten the febrile period and reduce complications.
View Article and Find Full Text PDFAntiviral Activity of (1,9a)-1-[(1,2,3-Triazol-1-yl)methyl]octahydro-1-quinolizines from the Alkaloid Lupinine.
Molecules
December 2024
N.N. Vorozhtsov Novosibirsk Institute of Organic Chemistry, Siberian Branch of the Russian Academy of Sciences, 630090 Novosibirsk, Russia.
Influenza is a disease of significant morbidity and mortality. The number of anti-influenza drugs is small; many of them stimulate the appearance of resistant strains. This article presents the results of assessing the antiviral activity of 1,2,3-triazole-containing derivatives of alkaloid lupinine for their ability to suppress the reproduction of orthomyxoviruses (influenza viruses: A/Vladivostok/2/09 (H1N1) and A/Almaty/8/98 (H3N2)).
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!