scholarly journals #Nitrosocarbonyls 1: Antiviral Activity ofN-(4-Hydroxycyclohex-2-en-1-yl)quinoline-2-carboxamide against the Influenza A Virus H1N1

2014 ◽  
Vol 2014 ◽  
pp. 1-10 ◽  
Author(s):  
Dalya Al-Saad ◽  
Misal Giuseppe Memeo ◽  
Paolo Quadrelli
Keyword(s):  
Influenza Virus ◽  
Antiviral Activity ◽  
Small Molecules ◽  
Influenza A ◽  
Nucleoside Analogues ◽  
Virus H1n1 ◽  
Antiviral Activities ◽  
Synthetic Approaches ◽  
Carbocyclic Nucleoside

Influenza virus flu A H1N1 still remains a target for its inhibition with small molecules. Fleeting nitrosocarbonyl intermediates are at work in a short-cut synthesis of carbocyclic nucleoside analogues. The strategy of the synthetic approaches is presented along with thein vitroantiviral tests. The nucleoside derivatives were tested for their inhibitory activity against a variety of viruses. Promising antiviral activities were found for specific compounds in the case of flu A H1N1.

scholarly journals Antiviral Activity of Fritillaria thunbergii Extract against Human Influenza Virus H1N1 (PR8) In Vitro, In Ovo and In Vivo

2020 ◽  
Vol 30 (2) ◽  
pp. 172-177 ◽  
Author(s):  
Minjee Kim ◽  
Dinh-Van Nguyen ◽  
Yoonki Heo ◽  
Ki Hoon Park ◽  
Hyun-Dong Paik ◽  
...  
Keyword(s):  
Influenza Virus ◽  
Antiviral Activity ◽  
Virus H1n1 ◽  
Human Influenza ◽  
In Ovo ◽  
Human Influenza Virus

scholarly journals Methylene Blue has a potent antiviral activity against SARS-CoV-2 and H1N1 influenza virus in the absence of UV-activation in vitro

2021 ◽  
Author(s):  
Valeria Cagno1 ◽  
Chiara Medaglia ◽  
Andreas Cerny ◽  
Thomas Cerny ◽  
Arnaud Zwygart ◽  
...  
Keyword(s):  
Methylene Blue ◽  
Influenza Virus ◽  
Antiviral Activity ◽  
Uv Light ◽  
H1n1 Influenza ◽  
European Medicines Agency ◽  
Virus H1n1 ◽  
Therapeutic Activity ◽  
Virucidal Activity

Abstract Methylene blue is an FDA (food and drug administration) and EMA (european medicines agency) approved drug with an excellent safety profile. It displays broad-spectrum virucidal activity in the presence of UV light and has been shown to be effective in inactivating various viruses in blood products prior to transfusions. In addition, its use has been validated for methemoglobinemia and malaria treatment. In this study, we first evaluated the virucidal activity of methylene blue against Influenza Virus H1N1 upon different incubation times and in the presence or absence of light activation, and then against SARS-CoV-2. We further assessed the therapeutic activity of methylene blue by administering it to cells previously infected with SARS-CoV-2. Finally, we examined the effect of co-administration of the drug together with immune serum. Our findings reveal that methylene blue displays virucidal preventive or therapeutic activity against Influenza Virus H1N1 and SARS-CoV-2 at low micromolar concentrations and in the absence of UV activation. We also confirm that MB antiviral activity is based on several mechanisms of action as the degradation of genomic RNA is only observed in the presence of light and after long exposure. Our work supports the interest of testing methylene blue in clinical studies to confirm a preventive or therapeutic efficacy against both Influenza Virus H1N1 and SARS-CoV-2 infections.

Effect of anaferon for children on the life cycle of influenza virus A/H1N1

2018 ◽  
pp. 87-94
Author(s):  
А.Г. Емельянова ◽  
М.В. Никифорова ◽  
Е.С. Дон ◽  
Н.Р. Махмудова ◽  
И.Н. Фалынскова ◽  
...  
Keyword(s):  
Influenza Virus ◽  
Life Cycle ◽  
Antiviral Activity ◽  
Influenza A ◽  
Mdck Cells ◽  
Antiviral Effect ◽  
H1n1 Influenza ◽  
Dose Dependence ◽  
Influenza Virus A

Цель исследования - изучение возможного прямого влияния препарата «Анаферон детский» на жизненный цикл вируса гриппа А в процессе развития инфекции, а также дозозависимости противовирусного эффекта in vitro . Методика. Исследование противовирусной активности препарата «Анаферон детский» in vitro было проведено с использованием культуры клеток MDCK (Madin Darby canine kidney) и эталонных штаммов вируса гриппа A (H1N1) pdm09: A/California/07/09 и А/California/04/09, полученных от ВОЗ. Использовались методы оценки подавления Анафероном детским вирусной репликации (по результатам иммуноферментного анализа по определению экспрессии внутренних белков NP и M1 вируса гриппа А) и его влияние на ультраструктурные особенности морфогенеза вируса гриппа методом электронной микроскопии. В качестве положительного контроля был использован Озельтамивир карбоксилат в концентрации 10 мкМ. Для мониторинга валидности экспериментальной модели в работе использовали клетки, зараженные вирусом без добавления экспериментальных образцов (контроль вируса), а также интактные клетки (клеточный контроль). Результаты. В ходе исследования показан дозозависимый противовирусный эффект препарата «Анаферон детский» для 3 тестируемых разведений - 1/8, 1/12, 1/16. Методом электронной микроскопии показано, что применение препарата «Анаферон детский» при сравнении с контрольным образцом влияло на процесс почкования вирионов. Заключение. Впервые показана дозозависимость противовирусного действия препарата «Анаферон детский», а также подтверждена его эффективность в отношении двух штаммов вируса пандемического гриппа А/H1N1. Документировано, что применение препарата «Анаферон детский» нарушает жизненный цикл вируса гриппа А. Механизмы развития такого эффекта требуют дополнительного изучения, однако можно предположить их связь с ИФН-индуцирующими свойствами препарата «Анаферон детский», так как было показано, что в начале лечения вирусной инфекции препарат вызывает индукцию синтеза белков системы интерферонов. The aim of this study was to evaluate a possible direct effect of Anaferon for Children on the life cycle of influenza A virus during infection development and a dose response of the antiviral effect in vitro. Methods. The in vitro antiviral activity of Anaferon for Children was studied on cultured MDCK cells and reference strains of influenza virus A (H1N1) pdm09: A/California/07/09 and A/California/04/09, both from the WHO. Inhibition of viral replication by Anaferon for Children and its effect on ultrastructural features of the influenza morphogenesis were evaluated using electron microscopy. Results. The study demonstrated a dose dependence of Anaferon for Children antiviral activity for three dilutions - 1/8, 1/12, and 1/16. Anaferon for Children affected the process of virion budding as compared to placebo. Conclusion. The study showed that the anti-influenza action of Anaferon for Children was dose-dependent and confirmed that this drug was effective against two strains of pandemic A/H1N1 influenza. Furthermore, Anaferon for children disrupted one or several stages of the virus life cycle.

Antiviral Effect of Gingyo-San, a Traditional Chinese Herbal Medicine, on Influenza A2Virus Infection in Mice

1999 ◽  
Vol 27 (01) ◽  
pp. 53-62 ◽  
Author(s):  
Makiko Kobayashi ◽  
Stephen M. Davis ◽  
Tokuichiro Utsunomiya ◽  
Richard B. Pollard ◽  
Fujio Suzuki
Keyword(s):  
Influenza Virus ◽  
Influenza A ◽  
Mdck Cells ◽  
Influenza Virus Infection ◽  
Antiviral Agent ◽  
Antiviral Effect ◽  
Traditional Chinese Herbal Medicine ◽  
Antiviral Activities ◽  
The Common

Gingyo-san is a crude drug containing extracts from 7 medicinal plants and fermented soybeans in a specific ratio. It has been used clinically in China as a therapeutic agent for the common cold. In the present study, we examined the antiviral effect of this agent on influenza virus infection in mice. Gingyo-san and its components were administered orally to mice 1 day before, then 1 and 4, days after the inhalation of a mouse-adopted strain of influenza A2(H2N2) virus. After infection with a 10 LD50of the virus, 100% of mice treated with 10 mg/kg of the agent survived as compared with a 0% survival of control mice treated with saline. Also, the mean survival days were ncreased and consolidation scores were decreased in treated mice as compared with those of control mice. Two components contained in the agent, extracts from Glycyrrhizae radix and Arctii fructus, expressed antiviral activities in mice infected with influenza virus. However, in vitro growth of influenza virus in MDCK cells or viability of the virus was not affected by these extracts or Gingyo-san. From these results Gingyo-san was shown to be an antiviral agent in mice infected with a lethal amount of a mouse-adopted strain of influenza A2virus.

scholarly journals Methylene Blue has a potent antiviral activity against SARS-CoV-2 and H1N1 influenza virus in the absence of UV-activation in vitro

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Valeria Cagno ◽  
Chiara Medaglia ◽  
Andreas Cerny ◽  
Thomas Cerny ◽  
Arnaud Charles-Antoine Zwygart ◽  
...  
Keyword(s):  
Methylene Blue ◽  
Influenza Virus ◽  
Antiviral Activity ◽  
Uv Light ◽  
Rna Degradation ◽  
European Medicines Agency ◽  
Virus H1n1 ◽  
Therapeutic Activity ◽  
Virucidal Activity

AbstractMethylene blue is an FDA (Food and Drug Administration) and EMA (European Medicines Agency) approved drug with an excellent safety profile. It displays broad-spectrum virucidal activity in the presence of UV light and has been shown to be effective in inactivating various viruses in blood products prior to transfusions. In addition, its use has been validated for methemoglobinemia and malaria treatment. In this study, we first evaluated the virucidal activity of methylene blue against influenza virus H1N1 upon different incubation times and in the presence or absence of light activation, and then against SARS-CoV-2. We further assessed the therapeutic activity of methylene blue by administering it to cells previously infected with SARS-CoV-2. Finally, we examined the effect of co-administration of the drug together with immune serum. Our findings reveal that methylene blue displays virucidal preventive or therapeutic activity against influenza virus H1N1 and SARS-CoV-2 at low micromolar concentrations and in the absence of UV-activation. We also confirm that MB antiviral activity is based on several mechanisms of action as the extent of genomic RNA degradation is higher in presence of light and after long exposure. Our work supports the interest of testing methylene blue in clinical studies to confirm a preventive and/or therapeutic efficacy against both influenza virus H1N1 and SARS-CoV-2 infections.

scholarly journals In Vitro Antiviral Activity of a Series of Wild Berry Fruit Extracts against Representatives of Picorna-, Orthomyxo- and Paramyxoviridae

2014 ◽  
Vol 9 (1) ◽  
pp. 1934578X1400900 ◽  
Author(s):  
Lubomira Nikolaeva-Glomb ◽  
Luchia Mukova ◽  
Nadya Nikolova ◽  
Ilian Badjakov ◽  
Ivayla Dincheva ◽  
...  
Keyword(s):  
Influenza Virus ◽  
Antiviral Activity ◽  
Influenza A ◽  
Antiviral Effect ◽  
Influenza Virus A ◽  
Methanol Extracts ◽  
Wide Range ◽  
Berry Fruits ◽  
Wild Berries

Wild berry species are known to exhibit a wide range of pharmacological activities. They have long been traditionally applied for their antiseptic, antimicrobial, cardioprotective and antioxidant properties. The aim of the present study is to reveal the potential for selective antiviral activity of total methanol extracts, as well as that of the anthocyanins and the non-anthocyanins from the following wild berries picked in Bulgaria: strawberry ( Fragaria vesca L.) and raspberry ( Rubus idaeus L.) of the Rosaceae plant family, and bilberry ( Vaccinium myrtillis L.) and lingonberry ( Vaccinium vitis-idaea L) of the Ericaceae. The antiviral effect has been tested against viruses that are important human pathogens and for which chemotherapy and/or chemoprophylaxis is indicated, namely poliovirus type 1 (PV-1) and coxsackievirus B1 (CV-B1) from the Picornaviridae virus family, human respiratory syncytial virus A2 (HRSV-A2) from the Paramyxoviridae and influenza virus A/H3N2 of Orthomyxoviridae. Wild berry fruits are freeze-dried and ground, then total methanol extracts are prepared. Further the extracts are fractioned by solid phase extraction and the non-anthocyanin and anthocyanin fractions are eluted. The in vitro antiviral effect is examined by the virus cytopathic effect (CPE) inhibition test. The results reveal that the total extracts of all tested berry fruits inhibit the replication of CV-B1 and influenza A virus. CV-B1 is inhibited to the highest degree by both bilberry and strawberry, as well as by lingonberry total extracts, and influenza A by bilberry and strawberry extracts. Anthocyanin fractions of all wild berries strongly inhibit the replication of influenza virus A/H3N2. Given the obtained results it is concluded that wild berry species are a valuable resource of antiviral substances and the present study should serve as a basis for further detailed research on the matter.

scholarly journals Limonoids Containing a C1–O–C29 Moiety: Isolation, Structural Modification, and Antiviral Activity

Marine Drugs ◽  
2018 ◽  
Vol 16 (11) ◽  
pp. 434 ◽  
Author(s):  
Jing-Ling Ren ◽  
Xiao-Peng Zou ◽  
Wan-Shan Li ◽  
Li Shen ◽  
Jun Wu
Keyword(s):  
Antiviral Activity ◽  
Inhibitory Activity ◽  
Influenza A ◽  
Structural Modification ◽  
X Ray Diffraction ◽  
Ic50 Value ◽  
Immunodeficiency Virus ◽  
Antiviral Activities ◽  
Hiv 1

Five new limonoids named thaigranatins A–E (1–5), containing a C1–O–C29 moiety, were isolated from seeds of the Thai Xylocarpus granatum, collected at the mangrove swamp of Trang Province, together with the known limonoid, granatumin L (6). The structures of these compounds were established by HR-ESIMS and extensive NMR spectroscopic data. The absolute configuration of 1 was unequivocally determined by single-crystal X-ray diffraction analysis, conducted with Cu Kα radiation; whereas that of 2 or 6 was established to be the same as that of 1 by the similarity of their electronic circular dichroism (ECD) spectra. In view of the marked antiviral activity of 6, its structure was modified via hydrolysis with alkaline KOH, esterification with diazomethane and various organic acids, and oximization with hydroxyamine. Finally, 18 derivatives, viz. 7–10, 8a–8i, 9a–9b, and 10a–10c, were obtained. In vitro antiviral activities of these derivatives against human immunodeficiency virus 1 (HIV-1) and influenza A virus (IAV) were evaluated. Most notably, 8i exhibited marked inhibitory activity against HIV-1 with an IC50 value of 15.98 ± 6.87 μM and a CC50 value greater than 100.0 μM; whereas 10b showed significant inhibitory activity against IAV with an IC50 value of 14.02 ± 3.54 μM and a CC50 value greater than 100.0 μM.

scholarly journals Antiviral Activity of the Sesquiterpene Lactones from Centipeda minima against Influenza a Virus in vitro

2018 ◽  
Vol 13 (2) ◽  
pp. 1934578X1801300 ◽  
Author(s):  
Xiaoli Zhang ◽  
Jun He ◽  
Weihuan Huang ◽  
Huibin Huang ◽  
Zeming Zhang ◽  
...  
Keyword(s):  
Influenza Virus ◽  
Antiviral Activity ◽  
Influenza A ◽  
Sesquiterpene Lactones ◽  
Influenza Virus Infection ◽  
Cell Counting ◽  
Mechanistic Study ◽  
Isolation And Identification ◽  
Centipeda Minima

During the course of searching for antiviral agents from Chinese medicinal herbs, we found that the supercritical fluid extract (SFE) of Centipeda minima possessed good in vitro antiviral activity against influenza virus A/Puerto Rico/8/34 H1N1 (PR8). Bioassay-guided isolation and identification led to the isolation from this extract of seven pseudoguaianolides (1-7). These, as well as nine other sesquiterpene lactones (8-16) previously isolated from this herb were all tested for their anti-PR8 activity using both the cytopathogenic effect (CPE) reduction and cell counting kit 8 (CCK8) assays. As a result, eight pseudoguaianolides (1-8) possessing an α,β-unsaturated cyclopentenone moiety showed antiviral activity against PR8 to different extents. Of the active compounds, brevilin A (4) exhibited the strongest anti-PR8 activity, with an IC50 value much lower than that of the positive control ribavirin. Mechanistic study revealed that brevilin A affected the intracellular replication of PR8 via downregulating the expression of viral M2 protein. All these results suggest the potential application of the pseudoguaianolides containing an α,β-unsaturated cyclopentenone moiety (e.g. brevilin A) in the treatment of influenza virus infection.

scholarly journals Synthesis and Antiviral Evaluation of Nucleoside Analogues Bearing One Pyrimidine Moiety and Two D-Ribofuranosyl Residues

Molecules ◽  
2021 ◽  
Vol 26 (12) ◽  
pp. 3678
Author(s):  
Olga V. Andreeva ◽  
Bulat F. Garifullin ◽  
Vladimir V. Zarubaev ◽  
Alexander V. Slita ◽  
Iana L. Yesaulkova ◽  
...  
Keyword(s):  
Influenza Virus ◽  
Antiviral Activity ◽  
Theoretical Calculations ◽  
Nucleoside Analogs ◽  
Coxsackievirus B3 ◽  
Nucleoside Analogues ◽  
Moderate Activity ◽  
Coat Proteins ◽  
Influenza Virus A ◽  
Ic50 Values

A series of 1,2,3-triazolyl nucleoside analogues in which 1,2,3-triazol-4-yl-β-d-ribofuranosyl fragments are attached via polymethylene linkers to both nitrogen atoms of the heterocycle moiety (uracil, 6-methyluracil, thymine, quinazoline-2,4-dione, alloxazine) or to the C-5 and N-3 atoms of the 6-methyluracil moiety was synthesized. All compounds synthesized were evaluated for antiviral activity against influenza virus A/PR/8/34/(H1N1) and coxsackievirus B3. Antiviral assays revealed three compounds, 2i, 5i, 11c, which showed moderate activity against influenza virus A H1N1 with IC50 values of 57.5 µM, 24.3 µM, and 29.2 µM, respectively. In the first two nucleoside analogues, 1,2,3-triazol-4-yl-β-d-ribofuranosyl fragments are attached via butylene linkers to N-1 and N-3 atoms of the heterocycle moiety (6-methyluracil and alloxazine, respectively). In nucleoside analogue 11c, two 1,2,3-triazol-4-yl-2′,3′,5′-tri-O-acetyl-β-d-ribofuranose fragments are attached via propylene linkers to the C-5 and N-3 atoms of the 6-methyluracil moiety. Almost all synthesized 1,2,3-triazolyl nucleoside analogues showed no antiviral activity against the coxsackie B3 virus. Two exceptions are 1,2,3-triazolyl nucleoside analogs 2f and 5f, in which 1,2,3-triazol-4-yl-2′,3′,5′-tri-O-acetyl-β-d-ribofuranose fragments are attached to the C-5 and N-3 atoms of the heterocycle moiety (6-methyluracil and alloxazine respectively). These compounds exhibited high antiviral potency against the coxsackie B3 virus with IC50 values of 12.4 and 11.3 µM, respectively, although both were inactive against influenza virus A H1N1. According to theoretical calculations, the antiviral activity of the 1,2,3-triazolyl nucleoside analogues 2i, 5i, and 11c against the H1N1 (A/PR/8/34) influenza virus can be explained by their influence on the functioning of the polymerase acidic protein (PA) of RNA-dependent RNA polymerase (RdRp). As to the antiviral activity of nucleoside analogs 2f and 5f against coxsackievirus B3, it can be explained by their interaction with the coat proteins VP1 and VP2.

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