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Keywords = virucidal efficiency

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16 pages, 2036 KB  
Article
Evaluation and Comparison of the UV-LED Action Spectra for Photochemical Disinfection of Coliphages and Human Pathogenic Viruses
by Kazuaki Mawatari, Yushi Onoda, Yasuko Kadomura-Ishikawa, Takahiro Emoto, Momoka Yamaguchi, Nozomi Hirano, Sae Toda, Mina Matsubara, Takashi Uebanso, Toshihiko Aizawa, Shigeharu Yamauchi, Yasuo Fujikawa, Tomotake Tanaka, Xing Li, Eduardo Suarez-Lopez, Richard J. Kuhn, Ernest R. Blatchley and Akira Takahashi
Microorganisms 2025, 13(12), 2798; https://doi.org/10.3390/microorganisms13122798 - 9 Dec 2025
Viewed by 500
Abstract
Ultraviolet (UV) disinfection is a powerful method for inactivating viruses. However, comparative wavelength-dependent sensitivities among human viruses and bacteriophages remain poorly characterized. Here, we evaluated the virucidal efficiencies of UV-light emitting diode (UV-LED) against multiple coliphages (MS2, Qβ, PhiX174, and T1) and mammalian [...] Read more.
Ultraviolet (UV) disinfection is a powerful method for inactivating viruses. However, comparative wavelength-dependent sensitivities among human viruses and bacteriophages remain poorly characterized. Here, we evaluated the virucidal efficiencies of UV-light emitting diode (UV-LED) against multiple coliphages (MS2, Qβ, PhiX174, and T1) and mammalian viruses, including respiratory syncytial virus (RSV) and human metapneumovirus (HMPV). We used a standardized irradiation system equipped with interchangeable UV-LED modules (250–365 nm), a low-pressure mercury lamp (254 nm), and a filtered krypton-chloride excimer lamp (222 nm). All coliphages exhibited wavelength-dependent inactivation with maximal efficiency at 263–270 nm, closely matching the action spectra of RSV and HMPV (r > 0.94, p < 0.001). However, their absolute UV sensitivities were markedly lower: under 254–281 nm irradiation. RSV and HMPV were approximately 21 and 12 times more sensitive than MS2, respectively. In contrast, far-UVC (222 nm) irradiation reduced these differences, indicating simultaneous damage to viral genomes and structural proteins. These results demonstrated that coliphages and human viruses exhibit similar wavelength-dependent sensitivity to UV-LED irradiation but differ in their absolute susceptibility. Therefore, while coliphages can be conservative surrogates for evaluating UV-LED virucidal performance, their applicability to far-UVC assessments should be interpreted with caution. Full article
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14 pages, 2323 KB  
Article
Antiviral Activity of Essential Oils Against Avian Influenza Virus H7N3 In Vitro and In Ovo Models
by Inkar Castellanos-Huerta, Jaime A. Ángel-Isaza, Lucio Bacab-Cab, Kevin Yam-Trujillo, Alejandro Aranda, Sindi Alejandra Velandia-Cruz, Loufrantz Mendez, Victor M. Petrone-Garcia, Guadalupe Ayora-Talavera and Álvaro José Uribe
Viruses 2025, 17(11), 1464; https://doi.org/10.3390/v17111464 - 31 Oct 2025
Viewed by 1121
Abstract
The poultry industry is continually seeking efficient, practical strategies to control infectious diseases. Among these new alternatives are essential oils (EOs), naturally occurring compounds with antimicrobial properties. Their effectiveness has been demonstrated in various studies that focus on their broad antiviral properties. The [...] Read more.
The poultry industry is continually seeking efficient, practical strategies to control infectious diseases. Among these new alternatives are essential oils (EOs), naturally occurring compounds with antimicrobial properties. Their effectiveness has been demonstrated in various studies that focus on their broad antiviral properties. The present experiment evaluated the antiviral efficacy of an EOs formulation against the H7N3 subtype of avian influenza virus (AIV) by directly mixing virus and EOs (virus/EOs mixture) through an in vitro model in cultured Madin-Darby canine kidney cells (MDCKs). The experiment used a focus reduction neutralization test (FRNT) to determine the 50% inhibitory concentration (IC50) by virus/EOs mixture, as well as the application of EOs 24 h before infection, through a viral inhibition test using a chicken embryo (CE) in ovo model. The results demonstrated the antiviral activity of the EOs formulation against the H7N3 in vitro model (IC50 values of 20.4 and 38.3 ppm and selective index (SI) values of 9.4 and 5.1) and in ovo model (decreasing hemagglutination titers to 1 HA unit, 105.28 embryo infectious dose 50% (EID50) per mL, and viral loads to approximately 1011.4 copies/mL) when applied in CE, 24 h before viral infection, representing the lowest replication indicators recorded during the experiment. According to the results, the EOs formulation demonstrated antiviral activity against AIV H7N3 both as a virus/EOs mixture and through application in ovo 24 h before infection. Application 24 h before infection in CE showed a significant effect compared with the virus/EOs mixture, demonstrating an antiviral effect in the ovo infection model. This study demonstrates both the virucidal and antiviral capacity of the compounds in the EOs formulation against AIV H7N3 and their efficacy when applied 24 h before infection in the in ovo model. Full article
(This article belongs to the Special Issue Antiviral Agents to Influenza Virus 2025)
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10 pages, 1565 KB  
Brief Report
Virucidal Potential of 3,3′,4,4′,5,5′-Hexahydroxy-trans-Stilbene Against Respiratory Syncytial Virus
by Zoltán Bánki, Leonie Wolf, Brigitte Müllauer, Daniel Geisler-Moroder, Wegene Borena, Walter Jäger and Thomas Szekeres
Viruses 2025, 17(10), 1287; https://doi.org/10.3390/v17101287 - 23 Sep 2025
Viewed by 602
Abstract
Respiratory syncytial virus (RSV) infections have a significant impact on global health. Despite of recent advancements, the current treatment options for managing severe RSV infections remain primarily limited to supportive care, emphasizing the high priority for the development of effective antiviral therapies. Antiviral [...] Read more.
Respiratory syncytial virus (RSV) infections have a significant impact on global health. Despite of recent advancements, the current treatment options for managing severe RSV infections remain primarily limited to supportive care, emphasizing the high priority for the development of effective antiviral therapies. Antiviral activity of 3,3′,4,4′,5,5′-hexahydroxy-trans-stilbene (HHS), a synthetic polyhydroxyphenol, has previously been demonstrated against SARS-CoV-2. In this study, we provide evidence for a direct virucidal effect of HHS against RSV infection in permissive HEp-2 cells in vitro. HHS, with an IC50 of 3.44 μM, efficiently inhibited HEp-2 cell infection with no sign of toxicity at least up to 25 μM. Interestingly, resveratrol, a polyhydroxyphenol analogue, was less efficient. Mode of action experiments revealed that HHS directly interacts with RSV particles, indicating that its virucidal activity is based on this interaction rather than affecting HEp-2 cells or post-infection processes. Together with previous data, our results suggest a broad antiviral activity of HHS against different respiratory viruses. Further studies are necessary to unveil the exact mechanism and evaluate the potential of HHS in the treatment of severe respiratory virus infections. Full article
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19 pages, 4270 KB  
Article
Viral Inactivation by Light-Emitting Diodes: Action Spectra Reveal Genomic Damage as the Primary Mechanism
by Kazuaki Mawatari, Yasuko Kadomura-Ishikawa, Takahiro Emoto, Yushi Onoda, Kai Ishida, Sae Toda, Takashi Uebanso, Toshihiko Aizawa, Shigeharu Yamauchi, Yasuo Fujikawa, Tomotake Tanaka, Xing Li, Eduardo Suarez-Lopez, Richard J. Kuhn, Ernest R. Blatchley III and Akira Takahashi
Viruses 2025, 17(8), 1065; https://doi.org/10.3390/v17081065 - 30 Jul 2025
Cited by 1 | Viewed by 1755
Abstract
Irradiation with ultraviolet light-emitting diodes (UV-LEDs) represents a promising method for viral inactivation, but a detailed understanding of the wavelength-dependent action spectra remains limited, particularly across different viral components. In this study, we established standardized UV action spectra for infectivity reduction in pathogenic [...] Read more.
Irradiation with ultraviolet light-emitting diodes (UV-LEDs) represents a promising method for viral inactivation, but a detailed understanding of the wavelength-dependent action spectra remains limited, particularly across different viral components. In this study, we established standardized UV action spectra for infectivity reduction in pathogenic viruses using a system equipped with interchangeable LEDs at 13 different peak wavelengths (250–365 nm). The reduction in viral infectivity induced by UV-LED exposure was strongly related to viral genome damage, whereas no significant degradation of viral structural proteins was detected. Peak virucidal efficiency was observed at 267–270 nm across all tested viruses, representing a slight shift from the traditionally expected 260 nm nucleic acid absorption peak. Enveloped RNA viruses, including influenza A virus, respiratory syncytial virus, and coronavirus, exhibited greater UV sensitivity than nonenveloped viruses such as feline calicivirus and adenovirus. These observations indicate that structural characteristics, such as the presence of an envelope and genome organization, influence UV susceptibility. The wavelength-specific action spectra established in this study provide critical data for optimizing UV-LED disinfection systems to achieve efficient viral inactivation while minimizing energy consumption in healthcare, food safety, and environmental sanitation. Full article
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17 pages, 2146 KB  
Article
Synthesis and Antiviral Activity of Nanowire Polymers Activated with Ag, Zn, and Cu Nanoclusters
by Thomas Thomberg, Hanna Bulgarin, Andres Lust, Jaak Nerut, Tavo Romann and Enn Lust
Pharmaceutics 2025, 17(7), 887; https://doi.org/10.3390/pharmaceutics17070887 - 6 Jul 2025
Cited by 1 | Viewed by 929
Abstract
Background/Objectives: Airborne viral diseases pose a health risk, due to which there is a growing interest in developing filter materials capable of capturing fine particles containing virions from the air and that also have a virucidal effect. Nanofiber membranes made of poly(vinylidene fluoride) [...] Read more.
Background/Objectives: Airborne viral diseases pose a health risk, due to which there is a growing interest in developing filter materials capable of capturing fine particles containing virions from the air and that also have a virucidal effect. Nanofiber membranes made of poly(vinylidene fluoride) dissolved in N,N-dimethylacetamide and functionalized with copper, silver, and zinc nanoclusters were fabricated via electrospinning. This study aims to evaluate and compare the virucidal effects of nanofibers functionalized with metal nanoclusters against the human influenza A virus A/WSN/1933 (H1N1) and SARS-CoV-2. Methods: A comprehensive characterization of materials, including X-ray diffraction, scanning electron microscopy, microwave plasma atomic emission spectroscopy, thermogravimetric analysis, contact angle measurements, nitrogen sorption analysis, mercury intrusion porosimetry, filtration efficiency, and virucidal tests, was used to understand the interdependence of the materials’ physical characteristics and biological effects, as well as to determine their suitability for application as antiviral materials in air filtration systems. Results: All the filter materials tested demonstrated very high particle filtration efficiency (≥98.0%). The material embedded with copper nanoclusters showed strong virucidal efficacy against the SARS-CoV-2 alpha variant, achieving an approximately 1000-fold reduction in infectious virions within 12 h. The fibrous nanowire polymer functionalized with zinc nanoclusters was the most effective material against the human influenza A virus strain A/WSN/1933 (H1N1). Conclusions: The materials with Cu nanoclusters can be used with high efficiency to passivate and kill the SARS-CoV-2 alpha variant virions, and Zn nanoclusters modified activated porous membranes for killing human influenza A virus A7WSN/1933 (H1N1) virions. Full article
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17 pages, 2194 KB  
Article
Polysaccharides from Brown Seaweeds (Padina boergesenii and Sargassum euryphyllum) as Promising Inhibitors of SARS-CoV-2: Characterization, Mechanisms, and Therapeutic Potential
by Saly Gheda, Ali M. Karkour, Shimaa El Shafay, Mohamed GabAllah, João Cotas and Leonel Pereira
Macromol 2025, 5(2), 18; https://doi.org/10.3390/macromol5020018 - 10 Apr 2025
Cited by 3 | Viewed by 2671
Abstract
Unexpected mutations in SARS-CoV-2 produce unique variations. While numerous vaccines and antiviral medications are available for SARS-CoV-2, their use in controlling and preventing COVID-19 is restricted in some areas and countries due to accessibility and cost issues. This study investigated polysaccharides produced from [...] Read more.
Unexpected mutations in SARS-CoV-2 produce unique variations. While numerous vaccines and antiviral medications are available for SARS-CoV-2, their use in controlling and preventing COVID-19 is restricted in some areas and countries due to accessibility and cost issues. This study investigated polysaccharides produced from two brown seaweed (Padina boergesenii and Sargassum euryphyllum) for their capacity to inhibit SARS-CoV-2. The seaweed polysaccharides were characterized and identified using ultraviolet and visible (UV/VIS) and Fourier transform infrared attenuated total reflectance (FTIR-ATR) spectra. The polysaccharides inhibited SARS-CoV-2 propagation with inhibitory concentration 50% (IC50) values ranging from 24.2 to 29.3 µg/mL and cytotoxicity concentration 50% (CC50) values for Vero-E6 cells ranging from 587.7 to 396.4 µg/mL for P. boergesenii and S. euryphyllum, respectively. P. boergesenii polysaccharide had a more substantial antiviral potential than S. euryphyllum against SARS-CoV-2 and appeared more promising. At a concentration of 575 µL/mL of P. boergesenii polysaccharide, the virucidal mechanism was found to be the most effective, followed by viral adsorption and replication, with viral inhibition percentages of 68.6% ± 0.8, 57.1% ± 1.4, and 37.2 ± 3, respectively, compared to remdesivir as an antiviral drug. Thus, we concluded that brown seaweed alginate polysaccharides efficiently inhibit SARS-CoV-2 from spreading by preventing viral entry. Finally, P. boergesenii polysaccharide looked promising as a potential therapeutic candidate for the treatment of COVID-19. Full article
(This article belongs to the Special Issue Recent Trends in Carbohydrate-Based Therapeutics)
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13 pages, 1265 KB  
Article
Unveiling the Broad-Spectrum Virucidal Potential of Purified Clinoptilolite-Tuff
by Alisina Sarabi, Stéphane Nizet, Andreas Röhrich and Cornelius Tschegg
Microorganisms 2024, 12(8), 1572; https://doi.org/10.3390/microorganisms12081572 - 1 Aug 2024
Cited by 6 | Viewed by 2160
Abstract
Due to its remarkable surface properties, natural clinoptilolite-tuff interacts with a variety of biochemical, pharmaceutical, chemical, and microbiological entities, including human viruses. In the present work, the virucidal activity of purified clinoptilolite-tuff (PCT) was investigated using a variety of viruses, differing in their [...] Read more.
Due to its remarkable surface properties, natural clinoptilolite-tuff interacts with a variety of biochemical, pharmaceutical, chemical, and microbiological entities, including human viruses. In the present work, the virucidal activity of purified clinoptilolite-tuff (PCT) was investigated using a variety of viruses, differing in their structure and composition. Influenza A virus, Herpes Simplex virus, Rhinovirus, and Parvovirus were chosen to represent enveloped and non-enveloped viruses with RNA and DNA genomes. Beside human viruses, Canine Parvovirus and bacteriophages T4 and MS2 were used to represent animal and bacterial viruses, respectively. The virucidal activity of PCT was quantified by examining the residual viral activity on susceptible cell lines upon incubation with PCT. A wide range of antiviral efficiencies was observed, ranging from up to 99% for Herpes Simplex virus to no activity for Rhinovirus and both bacteriophages. This study reveals that the virucidal potential of PCT is not universal and depends on a complex set of factors including virus structure and medium composition. The environmental and medical implications of this research are discussed for uses such as wastewater treatment or wound healing. Full article
(This article belongs to the Special Issue Antimicrobial Compounds from Alternative Sources 2.0)
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14 pages, 1000 KB  
Article
Efficiency of Virucidal Disinfectants on Wood Surfaces in Animal Husbandry
by Martin J. Oettler, Franz J. Conraths, Uwe Roesler, Sven Reiche, Timo Homeier-Bachmann and Nicolai Denzin
Microorganisms 2024, 12(5), 1019; https://doi.org/10.3390/microorganisms12051019 - 17 May 2024
Cited by 1 | Viewed by 2091
Abstract
The aim of this study was to test the inactivation of viruses on germ carriers of different types of wood using a disinfectant in order to assess the biosafety of wood as a building material in animal husbandry. The laboratory disinfectant efficacy tests [...] Read more.
The aim of this study was to test the inactivation of viruses on germ carriers of different types of wood using a disinfectant in order to assess the biosafety of wood as a building material in animal husbandry. The laboratory disinfectant efficacy tests were based on German testing guidelines and current European standards. Five different types of wood germ carriers, i.e., spruce (Picea abies), pine (Pinus sylvestris), poplar (Populus sp.), beech (Fagus sylvatica) and Douglas fir (Pseudotsuga menziesii), were inoculated with enveloped or non-enveloped viruses and then treated with one of three different disinfectants. The results revealed that intact, fine-sawn timber with a low roughness depth can be effectively inactivated. Peracetic acid proved to be the most effective disinfectant across all tests. Regardless of the pathogen and the type of wood, a concentration of 0.1% of the pure substance at a temperature of 10 °C and an exposure time of one hour can be recommended. At a temperature of −10 °C, a concentration of 0.75% is recommended. The basic chemicals formic acid and glutaraldehyde demonstrated only limited effectiveness overall. The synergistic effects of various wood components on the inactivation of viruses offer potential for further investigation. Disinfectant tests should also be conclusively verified in field trials to ensure that the results from standardised laboratory tests can be transferred to real stable conditions. Full article
(This article belongs to the Special Issue Disinfection and Sterilization of Microorganisms)
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19 pages, 2413 KB  
Article
Remdesivir-Loaded Nanoliposomes Stabilized by Chitosan/Hyaluronic Acid Film with a Potential Application in the Treatment of Coronavirus Infection
by Viktoria Milkova, Neli Vilhelmova-Ilieva, Anna Gyurova, Kamelia Kamburova, Ivaylo Dimitrov, Elina Tsvetanova, Almira Georgieva and Milka Mileva
Neurol. Int. 2023, 15(4), 1320-1338; https://doi.org/10.3390/neurolint15040083 - 30 Oct 2023
Cited by 10 | Viewed by 2602
Abstract
An object of the present study was the development of liposomes loaded with the medicine Veklury® (remdesivir) stabilized by electrostatic adsorption of polysaccharide film formed from chitosans with different physicochemical characteristics and hyaluronic acid. The functionalization of the structures was achieved through [...] Read more.
An object of the present study was the development of liposomes loaded with the medicine Veklury® (remdesivir) stabilized by electrostatic adsorption of polysaccharide film formed from chitosans with different physicochemical characteristics and hyaluronic acid. The functionalization of the structures was achieved through the inclusion of an aptamer (oligonucleotide sequence) with specific affinity to the spike protein of the human coronavirus HCoV-OC43. The hydrodynamic size, electrokinetic potential and stability of the structures were evaluated at each step in the procedure. The encapsulation efficiency and loaded amount of remdesivir (99% and 299 µg/mL) were estimated by UV–vis spectroscopy. Our investigations showed manifestation of promising tendencies for prolonged periods of the drug release and increased effectiveness of its antiviral action. Among all studied versions of the delivery system, the most distinguished and suitable in a model coronavirus therapy are the liposomes formed from chitosan oligosaccharides. The cytotoxicity of the liposomes was determined against the HCT-8 cell line. A cytopathic effect inhibition test was used for the assessment of the antiviral activity of the compounds. The virucidal activity and the effect on the viral adsorption of the samples were reported by the end-point dilution method, and the alteration in viral titer was determined as Δlgs compared to untreated controls. The redox-modulating properties of the nanoparticles were studied in vitro in certain/several/a few chemical model systems. Our investigations showed a manifestation of promising tendencies for a prolonged effect of the drug release and increased effectiveness of its antiviral action. Full article
(This article belongs to the Special Issue COVID-19, Neuroinflammation and Therapeutics)
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23 pages, 2259 KB  
Review
Phenolic Compounds in Salicornia spp. and Their Potential Therapeutic Effects on H1N1, HBV, HCV, and HIV: A Review
by Malthe Fredsgaard, Samba Evelyne Kabemba Kaniki, Io Antonopoulou, Tanmay Chaturvedi and Mette Hedegaard Thomsen
Molecules 2023, 28(14), 5312; https://doi.org/10.3390/molecules28145312 - 10 Jul 2023
Cited by 24 | Viewed by 4258
Abstract
Despite public health risk mitigation measures and regulation efforts by many countries, regions, and sectors, viral outbreaks remind the world of our vulnerability to biological hazards and the importance of mitigation actions. The saltwater-tolerant plants in the Salicornia genus belonging to the Amaranthaceae [...] Read more.
Despite public health risk mitigation measures and regulation efforts by many countries, regions, and sectors, viral outbreaks remind the world of our vulnerability to biological hazards and the importance of mitigation actions. The saltwater-tolerant plants in the Salicornia genus belonging to the Amaranthaceae family are widely recognized and researched as producers of clinically applicable phytochemicals. The plants in the Salicornia genus contain flavonoids, flavonoid glycosides, and hydroxycinnamic acids, including caffeic acid, ferulic acid, chlorogenic acid, apigenin, kaempferol, quercetin, isorhamnetin, myricetin, isoquercitrin, and myricitrin, which have all been shown to support the antiviral, virucidal, and symptom-suppressing activities. Their potential pharmacological usefulness as therapeutic medicine against viral infections has been suggested in many studies, where recent studies suggest these phenolic compounds may have pharmacological potential as therapeutic medicine against viral infections. This study reviews the antiviral effects, the mechanisms of action, and the potential as antiviral agents of the aforementioned phenolic compounds found in Salicornia spp. against an influenza A strain (H1N1), hepatitis B and C (HBV/HCV), and human immunodeficiency virus 1 (HIV-1), as no other literature has described these effects from the Salicornia genus at the time of publication. This review has the potential to have a significant societal impact by proposing the development of new antiviral nutraceuticals and pharmaceuticals derived from phenolic-rich formulations found in the edible Salicornia spp. These formulations could be utilized as a novel strategy by which to combat viral pandemics caused by H1N1, HBV, HCV, and HIV-1. The findings of this review indicate that isoquercitrin, myricetin, and myricitrin from Salicornia spp. have the potential to exhibit high efficiency in inhibiting viral infections. Myricetin exhibits inhibition of H1N1 plaque formation and reverse transcriptase, as well as integrase integration and cleavage. Isoquercitrin shows excellent neuraminidase inhibition. Myricitrin inhibits HIV-1 in infected cells. Extracts of biomass in the Salicornia genus could contribute to the development of more effective and efficient measures against viral infections and, ultimately, improve public health. Full article
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20 pages, 8039 KB  
Article
Antiviral Evaluation of New Synthetic Bioconjugates Based on GA-Hecate: A New Class of Antivirals Targeting Different Steps of Zika Virus Replication
by Paulo Ricardo da Silva Sanches, Ricardo Sanchez Velazquez, Mariana Nogueira Batista, Bruno Moreira Carneiro, Cintia Bittar, Giuditta De Lorenzo, Paula Rahal, Arvind H. Patel and Eduardo Maffud Cilli
Molecules 2023, 28(13), 4884; https://doi.org/10.3390/molecules28134884 - 21 Jun 2023
Cited by 4 | Viewed by 2264
Abstract
Re-emerging arboviruses represent a serious health problem due to their rapid vector-mediated spread, mainly in urban tropical areas. The 2013–2015 Zika virus (ZIKV) outbreak in South and Central America has been associated with cases of microcephaly in newborns and Guillain–Barret syndrome. We previously [...] Read more.
Re-emerging arboviruses represent a serious health problem due to their rapid vector-mediated spread, mainly in urban tropical areas. The 2013–2015 Zika virus (ZIKV) outbreak in South and Central America has been associated with cases of microcephaly in newborns and Guillain–Barret syndrome. We previously showed that the conjugate gallic acid—Hecate (GA-FALALKALKKALKKLKKALKKAL-CONH2)—is an efficient inhibitor of the hepatitis C virus. Here, we show that the Hecate peptide is degraded in human blood serum into three major metabolites. These metabolites conjugated with gallic acid were synthesized and their effect on ZIKV replication in cultured cells was evaluated. The GA-metabolite 5 (GA-FALALKALKKALKKL-COOH) was the most efficient in inhibiting two ZIKV strains of African and Asian lineage at the stage of both virus entry (virucidal and protective) and replication (post-entry). We also demonstrate that GA-metabolite 5 does not affect cell growth after 7 days of continuous treatment. Thus, this study identifies a new synthetic antiviral compound targeting different steps of ZIKV replication in vitro and with the potential for broad reactivity against other flaviviruses. Our work highlights a promising strategy for the development of new antivirals based on peptide metabolism and bioconjugation. Full article
(This article belongs to the Special Issue Peptide and Protein Chemistry: Design, Synthesis, and Applications)
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18 pages, 4601 KB  
Article
Identification of Potential Antiviral Hops Compounds against Chikungunya Virus
by Tsvetelina Mandova, Marielena Vogel Saivish, Leonardo La Serra, Mauricio Lacerda Nogueira and Fernando Batista Da Costa
Int. J. Mol. Sci. 2023, 24(4), 3333; https://doi.org/10.3390/ijms24043333 - 7 Feb 2023
Cited by 5 | Viewed by 3307
Abstract
Chikungunya virus (CHIKV) is an arthropod-borne virus that belongs to the genus Alphavirus (family Togaviridae). CHIKV causes chikungunya fever, which is mostly characterized by fever, arthralgia and, sometimes, a maculopapular rash. The bioactive constituents of hops (Humulus lupulus, Cannabaceae), mainly acylphloroglucinols, [...] Read more.
Chikungunya virus (CHIKV) is an arthropod-borne virus that belongs to the genus Alphavirus (family Togaviridae). CHIKV causes chikungunya fever, which is mostly characterized by fever, arthralgia and, sometimes, a maculopapular rash. The bioactive constituents of hops (Humulus lupulus, Cannabaceae), mainly acylphloroglucinols, known as well as α- and β-acids, exerted distinct activity against CHIKV, without showing cytotoxicity. For fast and efficient isolation and identification of such bioactive constituents, a silica-free countercurrent separation method was applied. The antiviral activity was determined by plaque reduction test and was visually confirmed by a cell-based immunofluorescence assay. All hops compounds demonstrated a promising post-treatment viral inhibition, except the fraction of acylphloroglucinols, in mixture. β-acids fraction of 125 µg/mL expressed the strongest virucidal activity (EC50 = 15.21 µg/mL), in a drug-addition experiment on Vero cells. Hypothesis for mechanism of action were proposed for acylphloroglucinols based on their lipophilicity and chemical structure. Therefore, inhibition of some steps of the protein kinase C (PKC) transduction cascades was also discussed. Full article
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16 pages, 2480 KB  
Article
Antimicrobial and Virucidal Potential of Morpholinium-Based Ionic Liquids
by Jakub Michalski, Julia Sommer, Peter Rossmanith, Anna Syguda, Tomasz Clapa and Patrick Mester
Int. J. Mol. Sci. 2023, 24(2), 1686; https://doi.org/10.3390/ijms24021686 - 14 Jan 2023
Cited by 9 | Viewed by 3784
Abstract
Witnessed by the ongoing spread of antimicrobial resistant bacteria as well as the recent global pandemic of the SARS-CoV-2 virus, the development of new disinfection strategies is of great importance, and novel substance classes as effective antimicrobials and virucides are urgently needed. Ionic [...] Read more.
Witnessed by the ongoing spread of antimicrobial resistant bacteria as well as the recent global pandemic of the SARS-CoV-2 virus, the development of new disinfection strategies is of great importance, and novel substance classes as effective antimicrobials and virucides are urgently needed. Ionic liquids (ILs), low-melting salts, have been already recognized as efficient antimicrobial agents with prospects for antiviral potential. In this study, we examined the antiviral activity of 12 morpholinium based herbicidal ionic liquids with a tripartite test system, including enzyme inhibition tests, virucidal activity determination against five model viruses and activity against five bacterial species. The antimicrobial and enzymatic tests confirmed that the inhibiting activity of ILs corresponds with the number of long alkyl side chains and that [Dec2Mor]+ based ILs are promising candidates as novel antimicrobials. The virucidal tests showed that ILs antiviral activity depends on the type and structure of the virus, revealing enveloped Phi6 phage as highly susceptible to the ILs action, while the non-enveloped phages PRD1 and MS2 proved completely resistant to ionic liquids. Furthermore, a comparison of results obtained for P100 and P001 phages demonstrated for the first time that the susceptibility of viruses to ionic liquids can be dependent on differences in the phage tail structure. Full article
(This article belongs to the Special Issue New Types of Antibacterial Biocides 2.0)
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20 pages, 2095 KB  
Article
Synthesis of Novel 1,3,4-Oxadiazole-Derived α-Aminophosphonates/α-Aminophosphonic Acids and Evaluation of Their In Vitro Antiviral Activity against the Avian Coronavirus Infectious Bronchitis Virus
by Shaima Hkiri, Marwa Mekni-Toujani, Elvan Üstün, Karim Hosni, Abdeljelil Ghram, Soufiane Touil, Ali Samarat and David Sémeril
Pharmaceutics 2023, 15(1), 114; https://doi.org/10.3390/pharmaceutics15010114 - 29 Dec 2022
Cited by 18 | Viewed by 3165
Abstract
An efficient and simple approach has been developed for the synthesis of eight dialkyl/aryl[(5-phenyl-1,3,4-oxadiazol-2-ylamino)(aryl)methyl]phosphonates through the Pudovik-type reaction of dialkyl/arylphosphite with imines, obtained from 5-phenyl-1,3,4-oxadiazol-2-amine and aromatic aldehydes, under microwave irradiation. Five of them were hydrolyzed to lead to the corresponding phosphonic acids. [...] Read more.
An efficient and simple approach has been developed for the synthesis of eight dialkyl/aryl[(5-phenyl-1,3,4-oxadiazol-2-ylamino)(aryl)methyl]phosphonates through the Pudovik-type reaction of dialkyl/arylphosphite with imines, obtained from 5-phenyl-1,3,4-oxadiazol-2-amine and aromatic aldehydes, under microwave irradiation. Five of them were hydrolyzed to lead to the corresponding phosphonic acids. Selected synthesized compounds were screened for their in vitro antiviral activity against the avian bronchitis virus (IBV). In the MTT cytotoxicity assay, the dose-response curve showed that all test compounds were safe in the range concentration of 540–1599 µM. The direct contact of novel synthesized compounds with IBV showed that the diethyl[(5-phenyl-1,3,4-oxadiazol-2-ylamino)(4-trifluoromethoxyphenyl)methyl]phosphonate (5f) (at 33 µM) and the [(5-phenyl-1,3,4-oxadiazol-2-ylamino)(4-trifluoromethylphenyl)methyl] phosphonic acid (6a) (at 1.23 µM) strongly inhibited the IBV infectivity, indicating their high virucidal activity. However, virus titers from IBV-infected Vero cells remained unchanged in response to treatment with the lowest non-cytotoxic concentrations of synthesized compounds suggesting their incapacity to inhibit the virus replication inside the host cell. Lack of antiviral activity might presumably be ascribed to their polarity that hampers their diffusion across the lipophilic cytoplasmic membrane. Therefore, the interactions of 5f and 6a were analyzed against the main coronavirus protease, papain-like protease, and nucleocapsid protein by molecular docking methods. Nevertheless, the novel 1,3,4-oxadiazole-based α-aminophosphonic acids and α-amino-phosphonates hold potential for developing new hygienic virucidal products for domestic, chemical, and medical uses. Full article
(This article belongs to the Special Issue Recent Advances in Antiviral Drug Development)
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17 pages, 668 KB  
Article
Characterization of Planktochlorella nurekis Extracts and Virucidal Activity against a Coronavirus Model, the Murine Coronavirus 3
by Jacqueline Graff Reis, Isabella Dai Prá, William Michelon, Aline Viancelli, David Guillermo Piedrahita Marquez, Caroline Schmitz, Marcelo Maraschin, Sidnei Moura, Izabella Thaís Silva, Geovanna de Oliveira Costa, Tiago Tizziani, Louis P. Sandjo, David Rodríguez-Lázaro and Gislaine Fongaro
Int. J. Environ. Res. Public Health 2022, 19(23), 15823; https://doi.org/10.3390/ijerph192315823 - 28 Nov 2022
Cited by 3 | Viewed by 3052
Abstract
Certain members of the Coronaviridae family have emerged as zoonotic agents and have recently caused severe respiratory diseases in humans and animals, such as SARS, MERS, and, more recently, COVID-19. Antivirals (drugs and antiseptics) capable of controlling viruses at the site of infection [...] Read more.
Certain members of the Coronaviridae family have emerged as zoonotic agents and have recently caused severe respiratory diseases in humans and animals, such as SARS, MERS, and, more recently, COVID-19. Antivirals (drugs and antiseptics) capable of controlling viruses at the site of infection are scarce. Microalgae from the Chlorellaceae family are sources of bioactive compounds with antioxidant, antiviral, and antitumor activity. In the present study, we aimed to evaluate various extracts from Planktochlorella nurekis in vitro against murine coronavirus-3 (MHV-3), which is an essential human coronavirus surrogate for laboratory assays. Methanol, hexane, and dichloromethane extracts of P. nurekis were tested in cells infected with MHV-3, and characterized by UV-vis spectrophotometry, nuclear magnetic resonance (NMR) spectroscopy, ultraperformance liquid chromatography-mass spectrometry (UPLC-MS), and the application of chemometrics through principal component analysis (PCA). All the extracts were highly efficient against MHV-3 (more than a 6 Log unit reduction), regardless of the solvent used or the concentration of the extract, but the dichloromethane extract was the most effective. Chemical characterization by spectrophotometry and NMR, with the aid of statistical analysis, showed that polyphenols, carbohydrates, and isoprene derivatives, such as terpenes and carotenoids have a more significant impact on the virucidal potential. Compounds identified by UPLC-MS were mainly lipids and only found in the dichloromethane extract. These results open new biotechnological possibilities to explore the biomass of P. nurekis; it is a natural extract and shows low cytotoxicity and an excellent antiviral effect, with low production costs, highlighting a promising potential for development and implementation of therapies against coronaviruses, such as SARS-CoV-2. Full article
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