Abstract：
:Knowledge of drug protein-binding and blood cell partitioning may be important for evaluating the pharmacokinetic parameters of zidovudine, particularly because of its intracellular site of action and potential to induce side effects. Equilibrium dialysis studies of zidovudine were performed over 2 h to identify the extent and site of binding. Zidovudine was added to anticoagulated whole blood to study blood cell distribution over a 24 h period at 37 degrees C and at 21 degrees C. Concurrent plasma and whole blood samples were determined at various time-points and blood partitioning was determined by application of a mass balance equation. All samples were analyzed using radioimmunoassay. The free fraction of zidovudine at a concentration of 500 ng/ml (1.7 microM) was 0.77 +/- 0.05 in plasma, 0.78 +/- 0.03 in serum, 0.88 +/- 0.03 in 4 g/dl albumin solution, and 1.0 in 100 mg/dl alpha 1-acid glycoprotein solution. A free fraction of 0.72 +/- 0.10 was observed in plasma from HIV-infected patients with zidovudine concentrations ranging from 16 to 91 ng/ml. Zidovudine equilibration between plasma and blood cells occurred rapidly, being complete within 10 min. After equilibrium was complete, the mean whole blood:plasma ratio was 0.86 +/- 0.02 and 0.80 +/- 0.04 (P = 0.20) and mean blood cell Partitioning ratio, [cell]/[plasma-free], was 0.85 +/- 0.06 and 0.66 +/- 0.14 (P = 0.25) for studies at 37 degrees C and 21 degrees C, respectively. The partitioning ratio was relatively consistent over the study period, suggesting no accumulation in blood cells. These results suggest that zidovudine binds to a small extent primarily to albumin. The free concentration equilibrates readily between blood cells and plasma independent of concentration and without signs of accumulation.
journal_name
Antiviral Resjournal_title
Antiviral researchauthors
Luzier A,Morse GDdoi
10.1016/0166-3542(93)90032-esubject
Has Abstractpub_date
1993-07-01 00:00:00pages
267-80issue
3eissn
0166-3542issn
1872-9096pii
0166-3542(93)90032-Ejournal_volume
21pub_type
杂志文章abstract：:Several pyrophosphate analogues have been studied for their effects on avian myeloblastosis virus reverse transcriptase and on cellular DNA polymerase alpha. Examination of structure-activity relationships for these compounds revealed that two acidic groups connected by a short bridge were necessary, but not sufficien...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/0166-3542(82)90028-6
更新日期：1982-05-01 00:00:00
abstract：:Ebola virus (EBOV), a negative-sense RNA virus in the family Filoviridae, is known to cause severe hemorrhagic fever in humans and other primates. Infection with EBOV causes a high mortality rate and currently there is no FDA-licensed vaccine or therapeutic treatment available. Recently, heat-shock protein 90 (Hsp90),...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2010.04.015
更新日期：2010-08-01 00:00:00
abstract：:The reverse transcriptase (RT) of HIV which has been inhibited by the incorporation of AZT into the primer strand is subject to a deblocking reaction by cellular ATP. This reaction yields unblocked primer plus the dinucleoside tetraphosphate, AZTp(4)A. In the present study, we report that AZTp(4)A is an excellent subs...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/s0166-3542(03)00003-2
更新日期：2003-05-01 00:00:00
abstract：:The aminoadamantanes, amantadine and rimantadine, have been used to prevent and treat influenza A virus infections for many years. Several reports have shown an increased level of resistance to these drugs, particularly among influenza A(H3N2) subtype viruses, during recent years. We observed an increase in amantadine...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2010.08.013
更新日期：2010-11-01 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：: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：:Human T-cell lymphotropic virus type 1 (HTLV-1)-associated adult T-cell leukemia/lymphoma (ATLL) has a poor prognosis owing to its intrinsic resistance to chemotherapy. Although zidovudine (AZT) and alpha interferon (IFN-alpha) give rise to some response and improve the prognosis of ATLL, alternative therapies are nee...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2006.02.003
更新日期：2006-07-01 00:00:00
abstract：:The ability to control plant viral diseases with chemicals has great potential value for agriculture, but few chemicals are available to date due to the difficulty in obtaining effective drugs. IMP dehydrogenase is an enzyme which catalyzes the conversion of inosine 5'-monophosphate to xanthosine 5'-monophosphate in t...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2006.10.007
更新日期：2007-03-01 00:00:00
abstract：:Infections by dengue virus (DENV) are increasing worldwide, with an urgent need for effective anti-DENV agents. We recently identified N-(4-hydroxyphenyl) retinamide (4-HPR), an anti-DENV agent effective against all 4 serotypes of DENV in cell culture, and in a lethal mouse model for DENV infection (Fraser et al., 201...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2016.03.006
更新日期：2016-06-01 00:00:00
abstract：:Infection with the oncogenic γ-herpesviruses Epstein-Barr virus (EBV) and Kaposi's sarcoma-associated herpesvirus (KSHV) cause several severe malignancies in humans. Inhibition of the lytic replication of EBV and KSHV eliminates the reservoir of persistent infection and transmission, consequently preventing the occurr...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2016.12.002
更新日期：2017-02-01 00:00:00
abstract：:Prevention of HIV infection and unintended pregnancies are public health priorities. In sub-Saharan Africa, where HIV prevalence is highest, depot medroxyprogesterone acetate (DMPA) is widely used as contraception. Therefore, understanding potential interactions between DMPA and antiretrovirals is critical. Here, we u...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2020.105001
更新日期：2020-12-29 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：:Rotavirus infection has emerged as an important cause of complications in organ transplantation recipients. Immunosuppressants used to prevent alloreactivity can also interfere with virus infection, but the direct effects of the specific type of immunosuppressants on rotavirus infection are still unclear. Here we prof...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2016.07.017
更新日期：2016-09-01 00:00:00
abstract：:Ampligen, a known immunomodulator and interferon inducer, was used alone and in combination with other antiviral agents to treat ducks congenitally-infected with duck hepatitis B virus. These antiviral agents included the conventional nucleoside analogue ganciclovir and the prokaryotic DNA gyrase B inhibitor coumermyc...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/0166-3542(93)90051-j
更新日期：1993-06-01 00:00:00
abstract：:Stilbenoids including resveratrol contain the basic structural unit of 1,2-diphenylethylene. Naturally occurring stilbenoids have broad structural features due to oligomerization and modifications and some have demonstrated potent biological activities. In an effort to identify bioactive stilbenoids, we screened a gro...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2012.05.001
更新日期：2012-07-01 00:00:00
abstract：:We have previously reported a new class of dendrimers with tryptophan (Trp) residues on the surface that show dual antiviral activities against HIV and enterovirus EV71. The prototype compound of this family is a derivative of pentaerythritol with 12 peripheral Trp groups and trivalent spacer arms. Here a novel series...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2019.06.006
更新日期：2019-08-01 00:00:00
abstract：:Influenza viruses (IV) continue to pose an imminent threat to human welfare. Yearly re-occurring seasonal epidemic outbreaks and pandemics with high mortality can occur. Besides vaccination against a limited number of viral strains only a few antiviral drugs are available, which are losing their effectiveness as more ...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2017.03.024
更新日期：2017-06-01 00:00:00
abstract：:Favipiravir (T-705) is a broad spectrum antiviral which has been approved in Japan for the treatment of severe influenza virus infections. We reported earlier that favipiravir inhibits the in vitro replication of CHIKV and protects against disease progression in CHIKV-infected immunodeficient mice. We here explored wh...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2017.09.016
更新日期：2018-01-01 00:00:00
abstract：:EV71 is a major causative agent of hand, foot and mouth disease (HFMD) and is responsible for large outbreaks in various Asian Pacific countries. In the present study, we generated the recombinant baculovirus (Bac-VP1) encoding VP1 in a novel expression cassette. The transmembrane domain of hemagglutinin of the H3N2 i...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2012.05.017
更新日期：2012-09-01 00:00:00
abstract：:More than 50% of a group of healthy homosexuals in Israel were found to have an activated interferon (IFN) system as evidenced by markedly elevated blood IFN levels, increased in vitro production of IFN by unstimulated peripheral blood mononuclear cells and HuIFN-alpha and HuIFN-gamma production by appropriately stimu...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/0166-3542(85)90027-0
更新日期：1985-08-01 00:00:00
abstract：:Oxyresveratrol, a major compound purified from Artocarpus lakoocha, a Thai traditional medicinal plant, was evaluated for its mechanism of action and therapeutic efficacy on cutaneous herpes simplex virus (HSV) infection in mice. The inhibitory concentrations for 50% HSV-1 plaque formation of oxyresveratrol, three cli...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2008.05.002
更新日期：2008-10-01 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：:Viral hemorrhagic fevers (VHFs) cause thousands of fatalities every year, but the treatment options for their management remain very limited. In particular, the development of therapeutic interventions is restricted by the lack of commercial viability of drugs targeting individual VHF agents. This makes approaches lik...
journal_title：Antiviral research
pub_type： 杂志文章,评审
doi：10.1016/j.antiviral.2019.104569
更新日期：2019-10-01 00:00:00
abstract：:A fatty acid derivative of ganciclovir (GCV), elaidic acid ganciclovir (E-GCV), has been evaluated for its inhibitory activity against laboratory and clinical strains of herpes simplex type 1 (HSV-1) and type 2 (HSV-2), varicella-zoster virus (VZV) and human cytomegalovirus (HCMV) in human embryonic lung fibroblasts. ...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/s0166-3542(00)00070-x
更新日期：2000-03-01 00:00:00
abstract：:Human cytomegalovirus infection can lead to life-threatening clinical manifestations particularly in the immunocompromised host. Current therapy options face severe limitations leading to a continued search for alternative drug candidates. Viral replication is dependent on a balanced interaction between viral and cell...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2013.04.017
更新日期：2013-08-01 00:00:00
abstract：:The K70E mutation in HIV-1 reverse transcriptase was observed in 10% of virologic non-responders of the abacavir/lamivudine/tenofovir arm of ESS30009, alone, or in mixtures with K65R by population sequencing. Clonal analysis of six ESS30009 K70E isolates failed to identify double mutants carrying K65R+K70E. Site-direc...
journal_title：Antiviral research
pub_type： 杂志文章,随机对照试验
doi：10.1016/j.antiviral.2007.03.006
更新日期：2007-09-01 00:00:00
abstract：:Several arenaviruses cause hemorrhagic fever (HF) in humans, and evidence indicates that the worldwide-distributed prototypic arenavirus lymphocytic choriomeningitis virus (LCMV) is a neglected human pathogen of clinical significance. Moreover, arenaviruses pose a biodefense threat. No licensed anti-arenavirus vaccine...
journal_title：Antiviral research
pub_type： 杂志文章,评审
doi：10.1016/j.antiviral.2008.08.002
更新日期：2008-12-01 00:00:00
abstract：:Tea is the second most consumed drink in the world. The beneficial effects of tea have been mostly attributed to its catechin content. Black tea is derived from the leaves of Camellia sinensis plant, and it is rich in theaflavin polyphenols, in particular theaflavin (TF1), theaflavin-3-monogallate (TF2A), theaflavin-3...
journal_title：Antiviral research
pub_type： 杂志文章
doi：10.1016/j.antiviral.2015.03.009
更新日期：2015-06-01 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 Cytomegalovirus Retinitis Retreatment Trial was a multicenter clinical trial designed to evaluate three treatments for the treatment of relapsed CMV retinitis; (1) foscarnet; (2) 'high-dose' ganciclovir, and (3) combination foscarnet and ganciclovir. Two hundred seventy-nine patients were enrolled and randomly ass...
journal_title：Antiviral research
pub_type： 临床试验,杂志文章,随机对照试验
doi：10.1016/0166-3542(95)00921-3
更新日期：1996-01-01 00:00:00
