Antiviral Chemistry and Chemotherapy最新文献_第3页

Genome analysis of coxsackievirus B1 isolates during the consecutive alternating administration course of triple antiviral combination in newborn mice. 在新生小鼠连续交替服用三联抗病毒药物期间对柯萨奇病毒 B1 分离物进行基因组分析。

Antiviral Chemistry and Chemotherapy Pub Date : 2020-01-01 DOI: 10.1177/2040206620906061

Petar Grozdanov, Marie-Line Joffret, Adelina Stoyanova, Patsy Polston, Emna Achouri, Ivanka Nikolova, Francis Delpeyroux, Angel S Galabov

引用次数: 0

Nucleos(t)ide analogues and Hepatitis B virus-related hepatocellular carcinoma: A literature review. 核苷类似物与乙型肝炎病毒相关的肝细胞癌:文献综述

Antiviral Chemistry and Chemotherapy Pub Date : 2020-01-01 DOI: 10.1177/2040206620921331

Mohamed A Abd El Aziz, Rodolfo Sacco, Antonio Facciorusso

引用次数: 6

Spectrum of antiviral activity of 4-aminopyrimidine N-oxides against a broad panel of tick-borne encephalitis virus strains. 4-氨基嘧啶n -氧化物对多种蜱传脑炎病毒株的抗病毒活性谱。

Antiviral Chemistry and Chemotherapy Pub Date : 2020-01-01 DOI: 10.1177/2040206620943462

Evgenia V Dueva, Ksenia K Tuchynskaya, Liubov I Kozlovskaya, Dmitry I Osolodkin, Kseniya N Sedenkova, Elena B Averina, Vladimir A Palyulin, Galina G Karganova

{"title":"Spectrum of antiviral activity of 4-aminopyrimidine N-oxides against a broad panel of tick-borne encephalitis virus strains.","authors":"Evgenia V Dueva, Ksenia K Tuchynskaya, Liubov I Kozlovskaya, Dmitry I Osolodkin, Kseniya N Sedenkova, Elena B Averina, Vladimir A Palyulin, Galina G Karganova","doi":"10.1177/2040206620943462","DOIUrl":"https://doi.org/10.1177/2040206620943462","url":null,"abstract":"Tick-borne encephalitis is an important human arbovirus neuroinfection spread across the Northern Eurasia. Inhibitors of tick-borne encephalitis virus (TBEV) strain Absettarov, presumably targeting E protein n-octyl-β-d-glucoside (β-OG) pocket, were reported earlier. In this work, these inhibitors were tested in vitro against seven strains representing three main TBEV subtypes. The most potent compound, 2-[(2-methyl-1-oxido-5,6,7,8-tetrahydroquinazolin-4-yl)amino]-phenol, showed EC50 values lower than 22 µM against all the tested strains. Nevertheless, EC50 values for virus samples of certain strains demonstrated a substantial variation, which appeared to be consistent with the presence of E protein not only in infectious virions, but also in non-infectious and immature virus particles, protein aggregates, and membrane complexes.","PeriodicalId":7960,"journal":{"name":"Antiviral Chemistry and Chemotherapy","volume":"28 ","pages":"2040206620943462"},"PeriodicalIF":0.0,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1177/2040206620943462","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"38276273","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 8

Gallium maltolate has in vitro antiviral activity against SARS-CoV-2 and is a potential treatment for COVID-19. 麦芽糖酸镓对SARS-CoV-2具有体外抗病毒活性，是COVID-19的潜在治疗方法。

Antiviral Chemistry and Chemotherapy Pub Date : 2020-01-01 DOI: 10.1177/2040206620983780

Lawrence R Bernstein, Leike Zhang

{"title":"Gallium maltolate has in vitro antiviral activity against SARS-CoV-2 and is a potential treatment for COVID-19.","authors":"Lawrence R Bernstein, Leike Zhang","doi":"10.1177/2040206620983780","DOIUrl":"10.1177/2040206620983780","url":null,"abstract":"Background: Gallium has demonstrated strong anti-inflammatory activity in numerous animal studies, and has also demonstrated direct antiviral activity against the influenza A H1N1 virus and the human immunodeficiency virus (HIV). Gallium maltolate (GaM), a small metal-organic coordination complex, has been tested in several Phase 1 clinical trials, in which no dose-limiting or other serious toxicity was reported, even at high daily oral doses for several months at a time. For these reasons, GaM may be considered a potential candidate to treat coronavirus disease 2019 (COVID-19), which is caused by the SARS-CoV-2 virus and can result in severe, sometimes lethal, inflammatory reactions. In this study, we assessed the ability of GaM to inhibit the replication of SARS-CoV-2 in a culture of Vero E6 cells.Methods: The efficacy of GaM in inhibiting the replication of SARS-CoV-2 was determined in a screening assay using cultured Vero E6 cells. The cytotoxicity of GaM in uninfected cells was determined using the Cell Counting Kit-8 (CCK-8) colorimetric assay.Results: The results showed that GaM inhibits viral replication in a dose-dependent manner, with the concentration that inhibits replication by 50% (EC50) being about 14 µM. No cytotoxicity was observed at concentrations up to at least 200 µM.Conclusion: The in vitro activity of GaM against SARS-CoV-2, together with GaM's known anti-inflammatory activity, provide justification for testing GaM in COVID-19 patients.","PeriodicalId":7960,"journal":{"name":"Antiviral Chemistry and Chemotherapy","volume":"28 ","pages":"2040206620983780"},"PeriodicalIF":0.0,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1177/2040206620983780","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"38742903","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 11

Application of human lymphoid cells for the evaluation of antivirals against human adenovirus type 19: Zalcitabine has superior activity compared to cidofovir. 应用人淋巴样细胞评价抗病毒药物对人腺病毒19型的作用:与西多福韦相比，Zalcitabine具有更强的活性。

Antiviral Chemistry and Chemotherapy Pub Date : 2020-01-01 DOI: 10.1177/2040206620921319

Kohsuke Nakagawara, Hironori Hayashi, Kumi Kawaji, Mina Sasano, Eiichi N Kodama

{"title":"Application of human lymphoid cells for the evaluation of antivirals against human adenovirus type 19: Zalcitabine has superior activity compared to cidofovir.","authors":"Kohsuke Nakagawara, Hironori Hayashi, Kumi Kawaji, Mina Sasano, Eiichi N Kodama","doi":"10.1177/2040206620921319","DOIUrl":"https://doi.org/10.1177/2040206620921319","url":null,"abstract":"Human adenovirus type 19 (HAdV-19) is a major cause of the epidemic keratoconjunctivitis. Outbreaks of keratoconjunctivitis are problematic to human health, especially for infants, the elderly, and immunocompromised individuals. However, the development of anti-HAdV drugs has been hampered by inconvenient screening systems; therefore, development of a simple screening method is highly desirable. In this study, we identified that HAdV-19 can infect a human lymphoid cell line transformed with human T-cell leukemia virus (MT-2 cells). MT-2 cells supported HAdV-19 replication and showed apparent cytopathic effects within five days post-infection. Using a thiazolyl blue tetrazolium bromide (MTT)-based colorimetric assay on MT-2 cells, we were able to detect the anti-HAdV-19 activities of previously reported nucleoside/tide compounds, including (S)-1-(3-hydroxy-2-phosphonylmethoxypropyl)cytosine (cidofovir), 2',3'-dideoxycytidine (zalcitabine) and 3'-deoxy-3'-fluorothymidine (trifluridine). Compared with previous methods, this system represents a more simple and rapid method to screen anti-HAdV-19 agents.","PeriodicalId":7960,"journal":{"name":"Antiviral Chemistry and Chemotherapy","volume":"28 ","pages":"2040206620921319"},"PeriodicalIF":0.0,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1177/2040206620921319","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"37881217","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 2

Targeting viral genome synthesis as broad-spectrum approach against RNA virus infections. 靶向病毒基因组合成作为抗RNA病毒感染的广谱方法。

Antiviral Chemistry and Chemotherapy Pub Date : 2020-01-01 DOI: 10.1177/2040206620976786

Johanna Huchting

{"title":"Targeting viral genome synthesis as broad-spectrum approach against RNA virus infections.","authors":"Johanna Huchting","doi":"10.1177/2040206620976786","DOIUrl":"https://doi.org/10.1177/2040206620976786","url":null,"abstract":"Zoonotic spillover, i.e. pathogen transmission from animal to human, has repeatedly introduced RNA viruses into the human population. In some cases, where these viruses were then efficiently transmitted between humans, they caused large disease outbreaks such as the 1918 flu pandemic or, more recently, outbreaks of Ebola and Coronavirus disease. These examples demonstrate that RNA viruses pose an immense burden on individual and public health with outbreaks threatening the economy and social cohesion within and across borders. And while emerging RNA viruses are introduced more frequently as human activities increasingly disrupt wild-life eco-systems, therapeutic or preventative medicines satisfying the \"one drug-multiple bugs\"-aim are unavailable. As one central aspect of preparedness efforts, this review digs into the development of broadly acting antivirals via targeting viral genome synthesis with host- or virus-directed drugs centering around nucleotides, the genomes' universal building blocks. Following the first strategy, selected examples of host de novo nucleotide synthesis inhibitors are presented that ultimately interfere with viral nucleic acid synthesis, with ribavirin being the most prominent and widely used example. For directly targeting the viral polymerase, nucleoside and nucleotide analogues (NNAs) have long been at the core of antiviral drug development and this review illustrates different molecular strategies by which NNAs inhibit viral infection. Highlighting well-known as well as recent, clinically promising compounds, structural features and mechanistic details that may confer broad-spectrum activity are discussed. The final part addresses limitations of NNAs for clinical development such as low efficacy or mitochondrial toxicity and illustrates strategies to overcome these.","PeriodicalId":7960,"journal":{"name":"Antiviral Chemistry and Chemotherapy","volume":"28 ","pages":"2040206620976786"},"PeriodicalIF":0.0,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1177/2040206620976786","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"38694050","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 19

Virologic failure after 48 weeks of raltegravir-based regimen in low HIV-1 incidence setting. 在HIV-1低发病率环境下，以替地韦为基础的治疗方案48周后出现病毒学失败。

Antiviral Chemistry and Chemotherapy Pub Date : 2020-01-01 DOI: 10.1177/2040206620927908

Wassim Chehadeh, Osama Albaksami, Shaikhah Al-Shammari

{"title":"Virologic failure after 48 weeks of raltegravir-based regimen in low HIV-1 incidence setting.","authors":"Wassim Chehadeh, Osama Albaksami, Shaikhah Al-Shammari","doi":"10.1177/2040206620927908","DOIUrl":"https://doi.org/10.1177/2040206620927908","url":null,"abstract":"Background: With the advent of next generation integrase strand transfer inhibitors, the rates of virologic failure in treated subjects are expected to decrease. In this study, we analyzed the mutation patterns leading to virologic failure before and after starting integrase strand transfer inhibitor-based regimen as first-line or salvage therapy.Methods: Between 2016 and 2019, blood samples were received from 258 patients with HIV-1 infection. Plasma HIV-1 RNA concentrations, and pol gene sequences were determined at baseline, and 16-48 weeks of treatment with integrase strand transfer inhibitor-based regimen. Only patients who did not achieve viral suppression at 48 weeks of integrase strand transfer inhibitor-based treatment were eligible for the current study.Results: Virologic failure was observed in seven patients on raltegravir-based regimen. All patients with virologic failure but one were infected with CRF01_AE virus subtype. Raltegravir based-regimen was offered as first-line therapy for four patients, and as salvage therapy for three patients. M184V mutation associated with high level resistance to lamivudine and emtricitabine was detected in six out of seven patients. Primary mutations (Y143C, N155H, T66I, G118R, E138K) conferring high level resistance to raltegravir were detected in only three patients. Pre-existing polymorphic integrase mutation (T97A) was detected in two patients. Furthermore, two patients reported low adherence to treatment.Conclusions: Emergence of primary mutations in the integrase gene can account for virologic failure in less than half of patients on raltegravir-based regimen. Low adherence to treatment, pre-existing accessory mutations, and resistance to reverse transcriptase inhibitors may have some role in virologic outcome.","PeriodicalId":7960,"journal":{"name":"Antiviral Chemistry and Chemotherapy","volume":"28 ","pages":"2040206620927908"},"PeriodicalIF":0.0,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1177/2040206620927908","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"37959434","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 1

Alkaloids and flavonoids from African phytochemicals as potential inhibitors of SARS-Cov-2 RNA-dependent RNA polymerase: an in silico perspective. 非洲植物化学物质中的生物碱和黄酮类化合物是 SARS-Cov-2 RNA 依赖性 RNA 聚合酶的潜在抑制剂：从硅学角度看问题。

Antiviral Chemistry and Chemotherapy Pub Date : 2020-01-01 DOI: 10.1177/2040206620984076

Oludare M Ogunyemi, Gideon A Gyebi, Abdo A Elfiky, Saheed O Afolabi, Olalekan B Ogunro, Adegbenro P Adegunloye, Ibrahim M Ibrahim

{"title":"Alkaloids and flavonoids from African phytochemicals as potential inhibitors of SARS-Cov-2 RNA-dependent RNA polymerase: an in silico perspective.","authors":"Oludare M Ogunyemi, Gideon A Gyebi, Abdo A Elfiky, Saheed O Afolabi, Olalekan B Ogunro, Adegbenro P Adegunloye, Ibrahim M Ibrahim","doi":"10.1177/2040206620984076","DOIUrl":"10.1177/2040206620984076","url":null,"abstract":"Corona Virus Disease 2019 (COVID-19) is a pandemic caused by Severe Acute Respiratory Syndrome Coronavirus-2 (SARS-CoV-2). Exploiting the potentials of phytocompounds is an integral component of the international response to this pandemic. In this study, a virtual screening through molecular docking analysis was used to screen a total of 226 bioactive compounds from African herbs and medicinal plants for direct interactions with SARS-CoV-2 RNA-dependent RNA polymerase (RdRp). From these, 36 phytocompounds with binding affinities higher than the approved reference drugs (remdesivir and sobosivir), were further docked targeting the active sites of SARS-CoV-2, as well as SARS-CoV and HCV RdRp. A hit list of 7 compounds alongside two positive controls (remdesivir and sofosbuvir) and two negative controls (cinnamaldehyde and Thymoquinone) were further docked into the active site of 8 different conformations of SARS-CoV-2 RdRp gotten from molecular dynamics simulation (MDS) system equilibration. The top docked compounds were further subjected to predictive druglikeness and ADME/tox filtering analyses. Drugable alkaloids (10'-hydroxyusambarensine, cryptospirolepine, strychnopentamine) and flavonoids (usararotenoid A, and 12α-epi-millettosin), were reported to exhibit strong affinity binding and interactions with key amino acid residues in the catalytic site, the divalent-cation-binding site, and the NTP entry channel in the active region of the RdRp enzyme as the positive controls. These phytochemicals, in addition to other promising antivirals such as remdesivir and sofosbuvir, may be exploited towards the development of a cocktail of anti-coronavirus treatments in COVID-19. Experimental studies are recommended to validate these study.","PeriodicalId":7960,"journal":{"name":"Antiviral Chemistry and Chemotherapy","volume":"28 ","pages":"2040206620984076"},"PeriodicalIF":0.0,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://ftp.ncbi.nlm.nih.gov/pub/pmc/oa_pdf/3a/31/10.1177_2040206620984076.PMC7783895.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39107555","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Respiratory syntycial virus: Current treatment strategies and vaccine approaches. 呼吸道合胞病毒:目前的治疗策略和疫苗方法。

Antiviral Chemistry and Chemotherapy Pub Date : 2020-01-01 DOI: 10.1177/2040206620947303

Elena Margret Thornhill, Jessica Salpor, David Verhoeven

引用次数: 11

In vitro anti-adenoviral activities of ethanol extract, fractions, and main phenolic compounds of pomegranate (Punica granatum L.) peel. 石榴皮乙醇提取物、组分及主要酚类化合物体外抗腺病毒活性研究。

Antiviral Chemistry and Chemotherapy Pub Date : 2020-01-01 DOI: 10.1177/2040206620916571

Ali Karimi, Mohammad-Taghi Moradi, Mohammad Rabiei, Somayeh Alidadi

{"title":"In vitro anti-adenoviral activities of ethanol extract, fractions, and main phenolic compounds of pomegranate (Punica granatum L.) peel.","authors":"Ali Karimi, Mohammad-Taghi Moradi, Mohammad Rabiei, Somayeh Alidadi","doi":"10.1177/2040206620916571","DOIUrl":"https://doi.org/10.1177/2040206620916571","url":null,"abstract":"Background Adenovirus causes a number of diseases in human, and can cause serious infection in severely immunosuppressed individuals. Despite the seriousness of adenovirus infection, there is no definitely approved anti-adenoviral therapy. Many studies have shown that compounds derived from medicinal plants have antiviral activity. Therefore, this study evaluated in vitro anti-adenoviral activity of ethanol extract, fractions, and main phenolic compounds of pomegranate peel. Methods The ethanol extract of pomegranate peel was prepared with maceration method and fractionated by consecutive liquid/liquid partition. The cytotoxic and anti-adenovirus activities of the extract, fractions, and main phenolic compounds (ellagic acid, punicalagin and gallic acid) were evaluated on Hep-2 cell line using MTT assay. Inhibitory effect on adsorption and post-adsorption phases of the virus replication cycle was also evaluated. Results Pomegranate peel extract had a desirable effect against adenovirus with IC50 of 5.77 µg/mL and selectivity index of 49.9. Among the fractions and compounds, the n-butanol fraction and gallic acid had the highest anti-adenoviral activity with IC50 of 2.16 µg/mL and 4.67 µM and selectivity indices of 122.5 and 10.5, respectively. The crude extract, n-butanol fraction and gallic acid inhibited the virus replication in post-adsorption phase (p < 0.01). Conclusion Pomegranate peel extract, especially its n-butanol fraction, could serve as a new promising anti-adenovirus agent due to high inhibitory effect against adenovirus replication. The effect of the n-butanol fraction may be related to the synergistic effect or other compounds of this fraction. Further understanding of the bioassay guided isolation of natural compounds of this fraction seems essential.","PeriodicalId":7960,"journal":{"name":"Antiviral Chemistry and Chemotherapy","volume":"28 ","pages":"2040206620916571"},"PeriodicalIF":0.0,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1177/2040206620916571","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"37849778","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 17