A total of 126 influenza B isolates isolated between 1998 and 2002 from Australasia and the Asia-Pacific region were tested for their sensitivity to the neuraminidase (NA) inhibitor drugs zanamivir and oseltamivir carboxylate using a fluorescence-based enzyme assay. The mean (+/-1 S.D.) 50% inhibitory concentration (IC50) of the influenza B viruses tested was 1.41+/-0.53 nM against zanamivir and 14.91+/-14.31 nM with oseltamivir carboxylate. However, a single type B isolate (B/Perth/211/2001) from an infant who had not been treated with either of the NA inhibitor drugs, showed a nine-fold lower sensitivity to zanamivir and a 14-fold lower sensitivity to oseltamivir carboxylate compared with the mean IC50 of influenza B strains. A decrease in sensitivity to oseltamivir carboxylate and RWJ-270201 was also seen in both: a chemiluminescent assay and a second different fluorescent assay. Sequence analysis of the haemagglutinin HA1 region and the neuraminidase gene of B/Perth/211/2001 revealed no amino acid changes in sites that have previously been reported to confer resistance to either of the NAI drugs. Further investigations are in progress to identify the basis for this reduced sensitivity.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.virusres.2004.02.035 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Edible bird's nest: N- and O-glycan analysis and synergistic anti-avian influenza virus activity with neuraminidase inhibitors.
Antiviral Res
December 2024
Department of Biochemistry, School of Pharmaceutical Sciences, University of Shizuoka, Shizuoka-shi, Shizuoka, 422-8526, Japan.
Article Synopsis
- * Edible bird's nest (EBN), which is swiftlet saliva consumed for health benefits, shows anti-avian viral properties, particularly by inhibiting the receptor-binding hemagglutinin (HA) activity after pancreatin treatment.
- * EBN, rich in specific glycan structures, effectively enhances the action of antiviral drugs oseltamivir and zanamivir, suggesting its potential as a food-derived solution to combat avian viruses and reduce the risk of pandemics.
Occurrence and environmental fate of anti-influenza drugs in a subcatchment of the Yodo River Basin, Japan.
Sci Total Environ
November 2024
Department of Pharmacy, Osaka Medical and Pharmaceutical University, 4-20-1 Nasahara, Takatsuki, Osaka 569-1094, Japan.
Article Synopsis
- * The study evaluated the degradation behaviors of several anti-influenza drugs in urban rivers and a wastewater treatment plant, finding that newer drugs like BALM degrade quickly while older drugs persist in the environment.
- * Ozonation after biological treatment was highly effective (over 90% removal) in eliminating anti-influenza drugs, highlighting its importance in managing pollution and reducing the risk of drug resistance in aquatic settings.
A Novel Prodrug Strategy Based on Reversibly Degradable Guanidine Imides for High Oral Bioavailability and Prolonged Pharmacokinetics of Broad-Spectrum Anti-influenza Agents.
ACS Cent Sci
August 2024
Department of Chemistry, College of Natural Sciences, Seoul National University, Seoul 08826, Republic of Korea.
We present orally administrable prodrugs (s) of guanidino oseltamivir carboxylate () based on guanidine cyclic diimide (GCDI) to treat influenza viruses. By concealing the guanidine group, which significantly limits the intestinal absorption, its prodrugs s demonstrate dramatic improvement of oral bioavailability. The most promising antiviral substance readily forms covalent adducts with serum proteins via a degradable linker after the intestinal absorption.
View Article and Find Full Text PDFAlbumin-Mediated Drug Uptake by Organic Anion Transporter 1/3 Is Real: Implications for the Prediction of Active Renal Secretion Clearance.
Mol Pharm
September 2024
Centre for Applied Pharmacokinetic Research, School of Health Sciences, University of Manchester, Manchester M13 9PL, U.K.
Modulation of the transport-mediated active uptake by human serum albumin (HSA) for highly protein-bound substrates has been reported and improved the -to- extrapolation (IVIVE) of hepatic clearance. However, evidence for the relevance of such a phenomenon in the case of renal transporters is sparse. In this study, transport of renal organic anion transporter 1 or 3 (OAT1/3) substrates into conditionally immortalized proximal tubular epithelial cells transduced with OAT1/3 was measured in the presence and absence of 1 and 4% HSA while keeping the unbound substrate concentration constant (based on measured fraction unbound, ).
View Article and Find Full Text PDFCitrus-derived flavanones as neuraminidase inhibitors: In vitro and in silico study.
Eur J Med Chem
November 2024
School of Food Science and Engineering, South China University of Technology, Guangzhou, 510640, PR China. Electronic address:
Neuraminidase (NA) has been well-studied as a therapeutic target for Influenza. However, resistance to the influenza virus has been observed recently. Out of special interest in the utilization of dietary antivirals from citrus, in vitro inhibition activity against NA and in silico studies including molecular docking, molecular dynamic simulation, and a predictive ADMET study, were performed on five citrus-derived flavanones.
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!