Abstract:
:Viramidine, the 3-carboxamidine derivative of ribavirin, was effective against a spectrum of influenza A (H1N1, H3N2 and H5N1) and B viruses in vitro, with the 50% effective concentration (EC50) ranging from 2 to 32 microg/ml. The mean 50% cytotoxic concentration (CC50) in the MDCK cells used in these experiments was 760 microg/ml. Ribavirin, run in parallel, had a similar antiviral spectrum, with EC50 values ranging from 0.6 to 5.5 microg/ml; the mean CC50 for ribavirin was 560 microg/ml. Oral gavage administrations of viramidine or ribavirin to mice infected with influenza A/NWS/33 (H1N1), A/Victoria/3/75 (H3N2), B/Hong Kong/5/72 or B/Sichuan/379/99 viruses were highly effective in preventing death, lessening decline in arterial oxygen saturation, inhibition of lung consolidation and reducing lung virus titers. The minimum effective dose of viramidine in these studies ranged from 15 to 31 mg/kg/day, depending upon the virus infection, when administered twice daily for 5 days beginning 4 h pre-virus exposure. The LD50 of the compound was 610 mg/kg/day. Ribavirin's minimum effective dose varied between 18 and 37.5 mg/kg/day with the LD50 determined to be 220 mg/kg/day. Viramidine's efficacy was also seen against an influenza A/NWS/33 (H1N1) virus infection in mice, when the compound was administered in the drinking water, the minimum effective dose being 100 mg/kg/day. Delay of the initiation of either viramidine or ribavirin therapy, using the approximate 1/3 LD50 dose of each, was protective as late as 48 h after exposure to the A/NWS/33 virus. While both compounds appear to have similar efficacy against influenza virus infections, when one considers the lesser toxicity, viramidine may warrant further evaluation as a possible therapy for influenza.
journal_name
Antiviral Resjournal_title
Antiviral researchauthors
Sidwell RW,Bailey KW,Wong MH,Barnard DL,Smee DFdoi
10.1016/j.antiviral.2005.06.003subject
Has Abstractpub_date
2005-10-01 00:00:00pages
10-7issue
1eissn
0166-3542issn
1872-9096pii
S0166-3542(05)00121-Xjournal_volume
68pub_type
杂志文章abstract::Epidermal growth factor receptor (EGFr) has been shown to be induced and activated in cells infected with HPV, suggesting that it may play a physiological role in viral replication or in the formation or maintenance of warts. To investigate this possibility, human foreskin tissue was infected with HPV11 and transplant...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2006.12.004
更新日期:2007-04-01 00:00:00
abstract::The biological evaluation of mononucleotide prodrugs (pronucleotides) of various nucleoside reverse transcriptase inhibitors (NRTIs) such as zidovudine (AZT), zalcitabine (ddC) and lamivudine (3TC) was reported in human T-lymphoid MOLT-4/8 cells which were grown continuously for more than 1 year in a medium containing...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/s0166-3542(01)00205-4
更新日期:2002-02-01 00:00:00
abstract::Despite the importance of Dengue virus (DENV) infection in human health, there is not a fully effective vaccine or antiviral treatment against the infection. Since lipids such as cholesterol are required during DENV infection, its uptake and synthesis are increased in infected cells. Ezetimibe is an FDA-approved drug ...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2018.10.024
更新日期:2018-12-01 00:00:00
abstract::The effects of caps, dinucleotides, oligonucleotides and polynucleotides on influenza virus RNA polymerase activity have been investigated. The results show that both methyl groups in a cap are necessary for optimal stimulation of polymerase activity. Both m7G(5')ppp(5')Am and ApG stimulated the influenza RNA polymera...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/0166-3542(81)90036-x
更新日期:1981-06-01 00:00:00
abstract::Lumpy skin disease is of significant economic impact for the cattle industry in Africa. The disease is currently spreading aggressively in the Near East, posing a threat of incursion to Europe and Asia. Due to cross-protection within the Capripoxvirus genus, sheep pox virus (SPPV) vaccines have been widely used for ca...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2014.06.009
更新日期:2014-09-01 00:00:00
abstract::Novel analogues of the anti-HIV-1 agent TSAO-T, [1-[2',5'-bis-O-(tert- butyldimethylsilyl)-beta-D-ribofuranosyl]thymine]-3'-spiro-5"-(4"-amino- 1",2"-oxathiole-2",2"-dioxide) and its 3-methyl counterpart TSAO-m3T were obtained by modifications at positions 2' or 5' of the sugar moiety. These compounds were evaluated f...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/0166-3542(95)00012-b
更新日期:1995-06-01 00:00:00
abstract::The hepatitis B virus nucleocapsid or core antigen is extremely immunogenic during infection and after immunization. This review summarizes several features of the nucleocapsid which explain this exceptionally high immunogenicity: a unique three-dimensional folding, the presence of a region that interacts with immunog...
journal_title:Antiviral research
pub_type: 杂志文章,评审
doi:10.1016/j.antiviral.2003.08.011
更新日期:2003-10-01 00:00:00
abstract::Synthetic flavans, isoflavans and isoflavenes substituted with chloro, cyano and amidino groups were tested for their in vitro activity against poliovirus type 2, Coxsackie virus B4, echovirus type 6 and enterovirus 71. Plaque-reduction assays showed that substituted 3-(2H)-isoflavenes, carrying a double bond in the o...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/0166-3542(95)00088-4
更新日期:1995-05-01 00:00:00
abstract::The TC-83 vaccine strain of Venezuelan equine encephalitis virus (VEEV) causes encephalitis and death in C3H/HeN mice infected by intranasal (i.n.) instillation. Since TC-83 is exempt as a select agent, this mouse model was used in the evaluation of antiviral therapies. Virus titers in the brains of infected mice peak...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2008.01.007
更新日期:2008-06-01 00:00:00
abstract::Sequences from the gag, pol and rev regions of the RF strain of HIV-1 (HIV-1RF) were chosen as targets for antisense phosphorothioate oligodeoxynucleotides (S-oligos). These sequences were the p18/p24 junction in gag, the active site of HIV protease in pol; a sequence from the first exon of the rev gene and S-oligodeo...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/0166-3542(92)90090-r
更新日期:1992-01-01 00:00:00
abstract::Everolimus is an inhibitor of mammalian target of rapamycin (mTOR) and reduces the risk of cytomegalovirus (CMV) infection in transplant recipients. Everolimus inhibits mTOR complex 1, which regulates factors involved in several crucial cellular functions and is required for CMV replication. However, it is not clear h...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2018.12.004
更新日期:2019-02-01 00:00:00
abstract::The rapid spread of Zika virus (ZIKV) in recent years has highlighted the severe diseases associated with ZIKV infection, such as Guillain-Barré syndrome in adults and microcephaly in newborns; yet no vaccines or antivirals currently exist to prevent or treat ZIKV infection. We and others have previously identified N-...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2017.10.014
更新日期:2017-11-01 00:00:00
abstract::Derivation of the 2-aminobenzylstatine containing HIV-1 proteinase (PR) inhibitor I led to a series of compounds with considerably improved antiviral activity, the most potent derivatives inhibiting HIV-1 with IC50 values below 25 nM. This was achieved by the combination of several structural modifications, most promi...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/0166-3542(94)90005-1
更新日期:1994-12-01 00:00:00
abstract::Pyrosequencing has been successfully used to monitor resistance in influenza A viruses to the first class of anti-influenza drugs, M2 blockers (adamantanes). In contrast to M2 blockers, resistance to neuraminidase (NA) inhibitors (NAIs) is subtype- and drug-specific. Here, we designed a pyrosequencing assay for detect...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2008.08.008
更新日期:2009-01-01 00:00:00
abstract::Herpes simplex virus-1 (HSV-1) infection is known to cause skin blisters, keratitis as well as deadly cases of encephalitis in some situations. Only a few therapeutic modalities are available for this globally prevalent infection. Very recently, a small molecule BX795 was identified as an inhibitor of HSV-1 protein sy...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2020.104814
更新日期:2020-08-01 00:00:00
abstract::Two new influenza virus neuraminidase inhibitors (NAIs), peramivir and laninamivir, were approved in 2010 which resulted to four NAIs that were used during the 2010-2011 influenza season in Japan. This study aims to monitor the susceptibility of influenza virus isolates in 2009-2010 and 2010-2011 influenza seasons in ...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2013.06.003
更新日期:2013-09-01 00:00:00
abstract::Investments in the development of new drugs for orthopoxvirus infections have fostered new avenues of research, provided an improved understanding of orthopoxvirus biology and yielded new therapies that are currently progressing through clinical trials. These broad-based efforts have also resulted in the identificatio...
journal_title:Antiviral research
pub_type: 杂志文章,评审
doi:10.1016/j.antiviral.2012.02.012
更新日期:2012-05-01 00:00:00
abstract::In spite of a decrease in the prevalence and incidence seen in recent years, chronic hepatitis B (CHB) still remains a major healthcare challenge, prevalent mostly in developing but also in developed regions. CHB is associated with significant morbidity and mortality, secondary to the complications of disease progress...
journal_title:Antiviral research
pub_type: 杂志文章,评审
doi:10.1016/j.antiviral.2020.104783
更新日期:2020-05-01 00:00:00
abstract::LY253963, the sodium salt of 1,3,4-thiadiazol-2-ylcyanamide, was evaluated in tissue culture and in cotton rats for toxicity and antiviral efficacy against respiratory syncytial (RSV) and parainfluenza type 3 (PIV3) viruses. The selective index (ratio of the median toxic dose: median efficacious dose) of LY253963 in H...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/0166-3542(90)90005-r
更新日期:1990-10-01 00:00:00
abstract:BACKGROUND:Cyclophilin inhibitors have shown activity against a variety of viruses, including HCV. NIM811, a novel, non-immunosuppressive cyclophilin inhibitor was studied in ascending doses in a randomized, double-blind, placebo-controlled 14-day trial in genotype 1 HCV patients. Doses of 10 up to 600 mg were given or...
journal_title:Antiviral research
pub_type: 杂志文章,随机对照试验
doi:10.1016/j.antiviral.2011.01.003
更新日期:2011-03-01 00:00:00
abstract::Sheep and goat pox continue to be important livestock diseases that pose a major threat to the livestock industry in many regions in Africa and Asia. Currently, several live attenuated vaccines are available and used in endemic countries to control these diseases. One of these is a partially attenuated strain of lumpy...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2015.08.016
更新日期:2015-11-01 00:00:00
abstract::delta 12-Prostaglandin J2 (delta 12-PGJ2), a natural dehydration product of prostaglandin D2 present in human body fluids, was shown to suppress Sendai virus replication in monkey kidney cells, at doses non-toxic to uninfected cells. Dramatic inhibition of virus production could be obtained at doses of delta 12-PGJ2 w...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/0166-3542(92)90072-d
更新日期:1992-08-01 00:00:00
abstract::In a previous study a 15-mer phosphorothioate oligonucleotide (S-ON) derived from the packaging signal in the 5' end of segment 1 (PB2) of influenza A virus (designated 5-15b) proved markedly inhibitory to virus replication. Here we investigated whether analogous inhibitory S-ONs targeting the 5' end of segments 2 (PB...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2011.06.013
更新日期:2011-10-01 00:00:00
abstract::We isolated a ganciclovir (GCV)-resistant human cytomegalovirus (HCMV) from a laboratory strain, AD169, and analysed the mutant. Attempts were also made to identify directly the mutated gene. The 50% inhibitory concentration (IC50) of GCV for the mutant strain was five times higher than that of the wild-type strain. T...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/s0166-3542(98)00051-5
更新日期:1998-12-01 00:00:00
abstract::Human cytomegalovirus (HCMV) infections cause congenital birth defects and disease in immunosuppressed individuals. Antiviral compounds can control infection yet their use is restricted due to concerns of toxicity and the emergence of drug resistant strains. We have evaluated the impact of an RNA Polymerase I (Pol I) ...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2018.02.014
更新日期:2018-05-01 00:00:00
abstract::Site-directed in vitro mutagenesis was used to create analogs of human interferons (IFNs)-alpha 1 and -alpha 4. Analogs were expressed in vitro using SP6 RNA polymerase and a rabbit reticulocyte lysate cell-free protein synthesis system. Amino acid substitutions for the highly conserved residues at positions 33, 121, ...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/0166-3542(89)90066-1
更新日期:1989-08-01 00:00:00
abstract::The antiviral effect of foscarnet (PFA) on the replication of rotavirus, a member of the Reoviridae, was studied. The pyrophosphate analogue is an effective inhibitor of several viral polymerases acting on the enzyme pyrophosphate binding site. Replication of rotavirus in MA104 cells using different u.o.i. was inhibit...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/0166-3542(94)00085-m
更新日期:1995-05-01 00:00:00
abstract::Interleukin (IL)28-B polymorphism has been related to interferon response in the treatment of hepatitis C, but its role in chronic hepatitis B (CHB) therapy is still poorly understood. We aimed to investigate the effect of IL28-B polymorphisms in the treatment with pegylated-interferon (PEG-IFN) of patients with CHB. ...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2013.11.014
更新日期:2014-02-01 00:00:00
abstract::This review describes the procedures for the use of fluorochrome labeled monoclonal antibodies and flow cytometry for the detection and quantification of virus infected cells. The application of this technology for (1) identifying virus infected cells in clinical specimens obtained from human cytomegalovirus (HCMV) an...
journal_title:Antiviral research
pub_type: 杂志文章,评审
doi:10.1016/s0166-3542(99)00039-x
更新日期:1999-08-01 00:00:00
abstract::One of the plant extracts, glycyrrhizin (GL) was investigated for its antiviral action on varicella-zoster virus (VZV) in vitro. When human embryonic fibroblast (HEF) cells were treated with GL after inoculation of virus (post-treatment), the average 50%-inhibitory dose (ID50) for five VZV strains was 0.71 mM, and the...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/0166-3542(87)90025-8
更新日期:1987-02-01 00:00:00