Abstract:
:Several nucleoside reverse transcriptase inhibitors are associated with mitochondrial toxicity resulting from inhibition of DNA polymerase-gamma. This study compared the effects on mitochondrial DNA of apricitabine (previously referred to as AVX754 or SPD754), a novel cytidine analogue under development for the treatment of human immunodeficiency virus (HIV)-1 infection, and other reverse transcriptase inhibitors. Human HepG2 hepatoblastoma were cultured for up to 16 days with test compounds at concentrations of 0.3-300 microM. Mitochondrial DNA replication was assessed by means of a duplex nucleic acid sequence-based amplification technique, which measures the ratio of the number of mitochondrial DNA copies to the number of genomic DNA copies. Apricitabine and tenofovir had no effect on the mitochondrial DNA content. In contrast, alovudine, zalcitabine, didanosine and stavudine markedly reduced mitochondrial DNA content, whereas abacavir, emtricitabine, lamivudine and zidovudine produced slight increases in mitochondrial DNA, which may reflect an adaptive cellular response to mitochondrial dysfunction. These results suggest that apricitabine shows a favorable mitochondrial toxicity profile, which is important for long-term clinical use. Further studies are warranted to define the clinical implications of these findings.
journal_name
Antiviral Resjournal_title
Antiviral researchauthors
de Baar MP,de Rooij ER,Smolders KG,van Schijndel HB,Timmermans EC,Bethell Rdoi
10.1016/j.antiviral.2007.05.004subject
Has Abstractpub_date
2007-10-01 00:00:00pages
68-74issue
1eissn
0166-3542issn
1872-9096pii
S0166-3542(07)00349-Xjournal_volume
76pub_type
杂志文章abstract::Novel L-lyxo-TSAO-T analogs with an inverted configuration at the C-4'-position of the sugar moiety and 5'-deoxy-5'-modified TSAO-T derivatives have been prepared and evaluated for their inhibitory effect on human immunodeficiency virus type 1 (HIV-1) and type 2 (HIV-2) replication in cell culture. None of the compoun...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/s0166-3542(95)00989-2
更新日期:1996-11-01 00:00:00
abstract::Varicella-zoster virus (VZV) replicates in quiescent T cells, neurons, and skin cells. In cultured fibroblasts (HFFs), VZV induces host cyclin expression and cyclin-dependent kinase (CDK) activity without causing cell cycle progression. CDK1/cyclin B1 phosphorylates the major viral transactivator, and the CDK inhibito...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2010.03.007
更新日期:2010-06-01 00:00:00
abstract::The ability to rescue an infectious, recombinant, negative-stranded, RNA virus from a complementary DNA (cDNA) clone, has led to new opportunities for measuring viral replication from a viral expressed reporter gene. In this study, the enhanced green fluorescent protein (EGFP) gene was inserted into the human parainfl...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2009.01.001
更新日期:2009-04-01 00:00:00
abstract::IRES-driven translation plays an essential role in picornavirus infection. However, there are seldom reports of compounds targeting this pathway with effective protection in animal models. Here, we identified emetine, an antiprotozoal drug, which inhibits EV-A71 with an EC50 value of 0.04 μM and a CC50 value of 10 μM ...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2019.104650
更新日期:2020-01-01 00:00:00
abstract:BACKGROUND:By modulating the antiviral immune response via vitamin D receptor, the active form of vitamin D (1,25-dihydroxyvitamin D, calcitriol) could play a central role in protection against respiratory virus infections. This in vitro study tested the hypothesis that respiratory viruses modulate vitamin D receptor e...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2016.11.004
更新日期:2017-01-01 00:00:00
abstract::Human adenoviruses are a common threat to immunocompromised patients, e.g., HIV-positive individuals or solid-organ and, in particular, allogeneic stem cell transplant recipients. Antiviral drugs have a limited effect on adenoviruses, and existing treatment modalities often fail to prevent fatal outcome. Silencing of ...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2012.03.011
更新日期:2012-06-01 00:00:00
abstract::We have analyzed a panel of protein kinase inhibitors (PKIs) and found that some indolocarbazoles (Gö6976, K252a, K252c) proved to be highly effective inhibitors of GCV-sensitive and -resistant human cytomegalovirus (HCMV) strains, but did not show any effect against herpes simplex virus. Antiviral activity was determ...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/s0166-3542(00)00118-2
更新日期:2000-10-01 00:00:00
abstract::The flavivirus nonstructural 4B protein (NS4B) has recently emerged as a valid antiviral target for drug discovery. Here we review (i) the current understanding of the structure and function of DENV NS4B, (ii) the approaches that have been taken to identify NS4B inhibitors, and (iii) the known inhibitors of flavivirus...
journal_title:Antiviral research
pub_type: 杂志文章,评审
doi:10.1016/j.antiviral.2015.03.007
更新日期:2015-06-01 00:00:00
abstract::The internal ribosome entry site (IRES) of hepatitis C virus (HCV) which governs the initiation of protein synthesis from viral RNA represents an ideal target for antisense approaches. Using an original bicistronic plasmid, we first established that sequence and translational activity of HCV IRESs cloned from six pati...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2008.06.011
更新日期:2008-12-01 00:00:00
abstract::Immune evasion by the lethal henipaviruses, Hendra (HeV) and Nipah virus, is mediated by its interferon (IFN) antagonist P gene products, phosphoprotein (P), and the related V and W proteins, which can target the signal transducer and activator of transcription 1 (STAT1) and STAT2 proteins to inhibit IFN/STAT signalin...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2015.09.017
更新日期:2015-12-01 00:00:00
abstract::Respiratory syncytial virus (RSV) is the major cause for respiratory tract disease in infants and young children. Currently, no licensed vaccine or a selective antiviral drug against RSV infections are available. Here, we describe a structure-based drug design approach that led to the synthesis of a novel series of zi...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2015.08.003
更新日期:2015-10-01 00:00:00
abstract::Rabies is a lethal viral infection that can affect almost all mammals, including humans. To better understand the replication of Rabies lyssavirus, we investigated if the viral load in brains naturally infected with rabies influences viral internalization and viral growth kinetics in neuroblastoma cells, and if the vi...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2017.11.003
更新日期:2018-01-01 00:00:00
abstract::The effect of interferon on the replication of herpes simplex virus types 1 and 2 was studied in two murine macrophage-like cell lines which differ in their ability to synthesize interferon. Higher titers of herpes simplex virus type 1 occurred in PU5-1.8 cell cultures where interferon was not produced than in J774A.1...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/0166-3542(86)90010-0
更新日期:1986-05-01 00:00:00
abstract::Emergence of drug-resistant human cytomegalovirus (HCMV) strains is a substantial problem during treatment of HCMV infections in immunocompromised patients. The Z-isomers of 2-hydroxymethylcyclopropylidenemethyl adenine (synadenol) and guanine (synguanol) were previously shown to be potent inhibitors of AD169 and Town...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/s0166-3542(02)00129-8
更新日期:2002-12-01 00:00:00
abstract::Influenza A virus has been responsible for widespread human epidemics because it is readily transmitted from humans to humans by aerosol. Recent events have highlighted the potential of influenza A virus as a bioterrorist weapon: the high virulence of the influenza A virus that infected people in Hong Kong in 1997; an...
journal_title:Antiviral research
pub_type: 杂志文章,评审
doi:10.1016/s0166-3542(02)00207-3
更新日期:2003-01-01 00:00:00
abstract::Current therapies for chronic hepatitis B virus infection (CHB) - nucleos(t)ide analogue reverse transcriptase inhibitors and interferons - result in low rates of functional cure defined as sustained off-therapy seroclearance of hepatitis B surface antigen (HBsAg). One likely reason is the inability of these therapies...
journal_title:Antiviral research
pub_type: 杂志文章,评审
doi:10.1016/j.antiviral.2015.06.019
更新日期:2015-09-01 00:00:00
abstract::The chemically modified DNA, apurinic acid (APA), is cytotoxic for human lymphocytes at concentrations above 100 micrograms/ml. At low concentrations (0.05-1 micrograms/ml) APA acts as an inducer interferon gamma (IFN-gamma) in lymphocytes in vitro; the maximum interferon titer of 50 units/ml was reached at 0.4 microg...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/0166-3542(88)90003-4
更新日期:1988-04-01 00:00:00
abstract::Natural compounds provide a large reservoir of potentially active anti-hepatitis B virus (HBV) agents. We examined the direct effects of protocatechuic aldehyde (PA; derived from the Chinese herb, Salvia miltiorrhiza) on HBV replication in HepG2 2.2.15 cell line and duck hepatitis B virus (DHBV) replication in ducklin...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2006.12.005
更新日期:2007-04-01 00:00:00
abstract::Resveratrol (RV), a polyphenolic natural product present in many plants and fruits, exhibits anti-inflammatory, cardio-protective and anti-proliferative properties. Moreover, RV affects a wide variety of viruses including members of the Herpesviridae family, retroviruses, influenza A virus and polyomavirus by altering...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2012.09.003
更新日期:2012-11-01 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::Due to diverse pathogenic potentials, there is a growing need for anti-HCMV agents. In this study, we show that treatment with DAPT, a γ-secretase inhibitor (GSI), impairs HCMV replication as assessed by a progeny assay based on immunostaining. This effect is not limited to DAPT because other GSIs with different struc...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2020.104867
更新日期:2020-11-01 00:00:00
abstract::Lactoferrin (LF), a member of the transferrin family, is a bi-globular protein secreted in milk, saliva, tears, seminal fluid, endocervix and vaginal secretions. LF is an important player in the defence against pathogenic microorganisms and has also been shown to have activity against several viruses including herpesv...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2004.05.005
更新日期:2004-10-01 00:00:00
abstract::Combinations of anti-HIV agents including one or two reverse transcriptase inhibitors with a protease inhibitor are potent and effective. However, toxicities, costs and the emergence of drug-resistant organisms have compromised their long-term efficacy in people. A next, likely, target for anti-HIV therapy is HIV-1 in...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/s0166-3542(00)00083-8
更新日期:2000-06-01 00:00:00
abstract::Because encapsulation of antiviral drugs in liposomes resulted generally in improved activity against retroviral replication in vivo, the antiviral effects of free-SPC3 and liposome-associated SPC3 were compared in cultured human lymphocytes infected with HIV-1. SPC3 was entrapped in various liposomal formulations, ei...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/s0166-3542(02)00002-5
更新日期:2002-06-01 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::Tiazofurine (2-beta-D-ribofuranosylthiazole-4-carboxamide) was found to inhibit replication of barley stripe mosaic virus (BSMV) in barley and wheat plants. Treatment with this nucleoside analogue delayed and inhibited symptom development and suppressed virus multiplication. The most effective concentration applied tw...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/0166-3542(89)90019-3
更新日期:1989-02-01 00:00:00
abstract::Tiazofurin (2-beta-D-ribofuranosylthiazole-4-carboxamide) was examined for its activity against tomato-spotted wilt virus (TSWV) in tomato plants. Solutions containing 50, 100, 200, 400 and 800 mg/l of the drug were sprayed onto the leaves. The results showed that 100 and 200 mg/l were the most efficient concentration...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/0166-3542(84)90003-2
更新日期:1984-12-01 00:00:00
abstract::Antiviral medication is used for the treatment of severe influenza infections, of which the neuraminidase inhibitors (NAIs) are the most effective drugs, approved so far. Here, we investigated the antiviral efficacy of the peptidomimetic furin inhibitor MI-701 in combination with oseltamivir carboxylate and ribavirin ...
journal_title:Antiviral research
pub_type: 杂志文章
doi:10.1016/j.antiviral.2015.05.006
更新日期:2015-08-01 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::Crimean-Congo hemorrhagic fever (CCHF) is a tick-borne viral disease of humans that affects a wide geographic area of Africa and Eurasia, including Turkey, Iran, Pakistan, Afghanistan and Russia. Since the first detection of CCHF cases in Turkey in 2002, more than 9700 patients have been reported, with an overall mort...
journal_title:Antiviral research
pub_type: 历史文章,杂志文章,评审
doi:10.1016/j.antiviral.2015.12.003
更新日期:2016-02-01 00:00:00