Natural antimicrobial peptides as a source of new antiviral agents

2021 ◽  
Vol 102 (9) ◽  
Author(s):  
Hovakim Zakaryan ◽  
Garri Chilingaryan ◽  
Erik Arabyan ◽  
Andre Serobian ◽  
Guangshun Wang

Current antiviral drugs are limited because of their adverse side effects and increased rate of resistance. In recent decades, much scientific effort has been invested in the discovery of new synthetic and natural compounds with promising antiviral properties. Among this new generation of compounds, antimicrobial peptides with antiviral activity have been described and are attracting attention due to their mechanism of action and biological properties. To understand the potential of antiviral peptides (AVPs), we analyse the antiviral activity of well-known AVP families isolated from different natural sources, discuss their physical–chemical properties, and demonstrate how AVP databases can guide us to design synthetic AVPs with better therapeutic properties. All considerations in this sphere of antiviral therapy clearly demonstrate the remarkable contribution that AVPs may make in conquering old as well as newly emerging viruses that plague humanity.

2017 ◽  
Vol 2017 ◽  
pp. 1-11 ◽  
Author(s):  
Daniela Dellosso Cibim ◽  
Miki Taketomi Saito ◽  
Priscila Alves Giovani ◽  
Ana Flávia Sanches Borges ◽  
Vanessa Gallego Arias Pecorari ◽  
...  

The aim of this study was to assess the performance of glass ionomer cement (GIC) added with TiO2nanotubes. TiO2nanotubes [3%, 5%, and 7% (w/w)] were incorporated into GIC’s (Ketac Molar EasyMix™) powder component, whereas unblended powder was used as control. Physical-chemical-biological analysis included energy dispersive spectroscopy (EDS), surface roughness (SR), Knoop hardness (SH), fluoride-releasing analysis, cytotoxicity, cell morphology, and extracellular matrix (ECM) composition. Parametric or nonparametric ANOVA were used for statistical comparisons (α≤0.05). Data analysis revealed that EDS only detected Ti at the 5% and 7% groups and that GIC’s physical-chemical properties were significantly improved by the addition of 5% TiO2as compared to 3% and GIC alone. Furthermore, regardless of TiO2concentration, no significant effect was found on SR, whereas GIC-containing 7% TiO2presented decreased SH values. Fluoride release lasted longer for the 5% and 7% TiO2groups, and cell morphology/spreading and ECM composition were found to be positively affected by TiO2at 5%. In conclusion, in the current study, nanotechnology incorporated in GIC affected ECM composition and was important for the superior microhardness and fluoride release, suggesting its potential for higher stress-bearing site restorations.


Author(s):  
Thongchai Taechowisan ◽  
Tipparat Samsawat ◽  
Chanjira Jaramornburapong ◽  
Weerachai Phutdhawong ◽  
Waya S. Phutdhawong

Aims: The purpose of this study was to synthesis novel amine-geldanamycin hybrids (AGH) and evaluate their biological properties. Study Design: Experimental study. Place and Duration of Study: The study was carried out at the Department of Microbiology and Department of Chemistry, Faculty of Science, Silpakorn University, from December 2019 - November 2020. Methodology: Three new amine-geldanamycin hybrids (AGH); compounds 2 to 4 were synthesised by nucleophilic substitution of geldanamycin (1). The solubility, cytotoxicity, antiviral activity and molecular docking analyses were carried out. Results: The solubility of AGH in water was 1.918-5.571 mM, higher than that of compound 1. Compound 2 exhibited weak cytotoxicity activity against Vero and LLC-MK2 cells, with IC50 values of 229.19 and 330.58 µg/ml, respectively. All compounds inhibited influenza virus propagation in embryonated chicken eggs at the lowest amount of 1.25 µg per egg. They interacted positively with Hsp90, showing a binding free energy (DG) of -112.00 to -116.34 kcal/mol, which indicated lower Hsp90 affinity compared with that of geldanamycin (-133.06 kcal/mol) and 17-dimethylamino ethylamino-17-demethoxygeldanamycin (-136.55 kcal/mol), despite being bound in the similar active site. For the viral absorption, only AGH inhibited hemagglutination at a concentration of 25 µg/ml. Conclusion: The study findings revealed, through molecular docking analysis, that the development of AGH improved the antiviral activity. The AGH inhibited not only influenza virus propagation, but also viral absorption. Therefore, AGH could be considered a new choice for antiviral agents.


Molecules ◽  
2021 ◽  
Vol 26 (16) ◽  
pp. 4777
Author(s):  
Francesca Guzzo ◽  
Rosita Russo ◽  
Cinzia Sanna ◽  
Odeta Celaj ◽  
Alessia Caredda ◽  
...  

Plants are the everlasting source of a wide spectrum of specialized metabolites, characterized by wide variability in term of chemical structures and different biological properties such antiviral activity. In the search for novel antiviral agents against Human Immunodeficiency Virus type 1 (HIV-1) from plants, the phytochemical investigation of Scrophularia trifoliata L. led us to isolate and characterize four flavonols glycosides along with nine iridoid glycosides, two of them, 5 and 13, described for the first time. In the present study, we investigated, for the first time, the contents of a methanol extract of S. trifoliata leaves, in order to explore the potential antiviral activity against HIV-1. The antiviral activity was evaluated in biochemical assays for the inhibition of HIV-1Reverse Transcriptase (RT)-associated Ribonuclease H (RNase H) activity and HIV-1 Integrase (IN). Three isolated flavonoids, rutin, kaempferol-7-O-rhamnosyl-3-O-glucopyranoside, and kaempferol-3-O-glucopyranoside, 8–10, inhibited specifically the HIV-1 IN activity at submicromolar concentration, with the latter being the most potent, showing an IC50 value of 24 nM.


2015 ◽  
Vol 1085 ◽  
pp. 394-399 ◽  
Author(s):  
Lyudmila A. Rasskazova ◽  
Darya Lytkina ◽  
Yelena Shapovalova ◽  
Vladimir V. Botvin ◽  
Maksim A. Pozdnyakov ◽  
...  

A new methodin situfor producing of biocompatible composites based on hydroxyapatite and oligomers of lactic and glycolic acid is described. Their thermo-mechanical, physical-chemical and biological properties are studied as well. The formation of bonds between hydroxyapatite with lactic and glycolic oligomers in composites are confirmed by IR spectroscopy of the samples, including those obtained in the Soxhlet apparatus. The formation of calcium-phosphate layer on the composite's surface containing hydroxyapatite was shown by SBF-investigation. The scaffolds based on lactic acid oligomer do not stimulate formation of a calcium-phosphate layer and they are subjected to destruction by the way of hydrolysis.


Cells ◽  
2021 ◽  
Vol 10 (11) ◽  
pp. 3081
Author(s):  
Francesco Oliva ◽  
Emanuela Marsilio ◽  
Giovanni Asparago ◽  
Antonio Frizziero ◽  
Anna Concetta Berardi ◽  
...  

The physical–chemical, structural, hydrodynamic, and biological properties of hyaluronic acid within tendons are still poorly investigated. Medical history and clinical applications of hyaluronic acid for tendinopathies are still debated. In general, the properties of hyaluronic acid depend on several factors including molecular weight. Several preclinical and clinical experiences show a good efficacy and safety profile of hyaluronic acid, despite the absence of consensus in the literature regarding the classification according to molecular weight. In in vitro and preclinical studies, hyaluronic acid has shown physical–chemical properties, such as biocompatibility, mucoadhesivity, hygroscopicity, and viscoelasticity, useful to contribute to tendon healing. Additionally, in clinical studies, hyaluronic acid has been used with promising results in different tendinopathies. In this narrative review, findings encourage the clinical application of HA in tendinopathies such as rotator cuff, epicondylitis, Achilles, and patellar tendinopathy.


Author(s):  
Vitor Duarte ◽  
Raquel Naves ◽  
Adailton Bortoluzzi ◽  
Eduardo Faria ◽  
Aline da Silva ◽  
...  

Benzimidazole and its derivatives are molecules that have diverse biological properties, therefore we synthesized and studied a new benzimidazole to understand their physical/chemical properties. The compound was obtained through a new synthetic route, using graphite oxide, in the absence of solvent, with crystalline packaging supported by C–H…N and C–H…π interactions. According to the frontier molecular orbitals, the compound is kinetically stable while the molecular electrostatic potential map confirms the site of molecular interactions involving nitrogen atoms and the π-system. This comprehensive study on synthesis, structural description and theoretical calculations can support ongoing studies in pharmaceutical science.


2012 ◽  
Vol 599 ◽  
pp. 32-35
Author(s):  
Zi Chao Zhao ◽  
Zhen Yao Xia ◽  
Ming Yi Li ◽  
Bin Wu ◽  
Wen Nian Xu

Taked an repaired completed slope - Vegetation-Growing Concrete Gunning (VGCG) slope for the experimental plot to measured indicators could evaluate the physical, chemical and biological properties.It showed that there were significantly difference in SBD, PH, SOM, AN. AP. AP and AK in different seasons, but no law. And there were significantly difference in soil enzyme activities except catalase in different seasons. Soil enzyme activities were highest in summer, lowest in winter except catalase. It showed that enzyme activitiy roses at first in the lower from spring to winter in one year. It proved that there were ruleless in seasonal change of the soil physical and chemical properties and there was a certain rule in seasonal change of the soil biological properties of the VGCG slope in one year.


2018 ◽  
Vol 22 (03) ◽  
pp. 96-102 ◽  
Author(s):  
Bayarmaa J ◽  
Purev D

Enzymes are an integral part of the soil and their activity is closely related to the physical, chemical and biological properties of the soil. Human activities, intensive agriculture, changes in ecosystem, environmental pollution have a great influence on the activity of soil enzymes. Depending on the origin soil enzymes are indicators for accessing the condition of the soil for short and long period of time. Almost all anthropogenic and environmental factors affecting the physical and chemical properties of the soil are studied for this purpose, but enzymes in the soil are the most sensitive to these changes. So it is a time to the study of the enzymes in the soil.


1992 ◽  
Vol 32 (7) ◽  
pp. 929 ◽  
Author(s):  
RK Belford ◽  
M Dracup ◽  
D Tennant

The combination of soil physical and chemical properties in duplex soils can depress crop growth and yield, and cause considerable variability in yield within a paddock and from year to year. At an intensively monitored site at East Beverley, Western Australia, the sandy A horizon was found to be nutrient deficient, low in pH, and contained hard layers which impeded root growth. The clayey B horizon had a higher pH, and variable permeability which influenced waterlogging in winter, and root growth and water availability from the subsoil in spring. Growth of wheat and lupin crops reflected response to these stresses. Wheat yields in particular were very variable (0.7-4.2 t/ha in 1988), and as all components of yield were affected, this suggests that the crop in low yielding areas experienced stress throughout the growing season. Lupin yields varied more widely from year to year than wheat yields, but were less variable within a year, possibly because of a more limited exploration of the subsoil by roots. Treatments to overcome the chemical constraints to growth raised yields and reduced variability; wheat and lupin yields were increased by about 25% after application of potassium, and wheat yields increased by about 10% after application of lime. Ripping lowered soil strength in the A horizon, but had little effect on yield, suggesting that the subsoil plays a larger role in determining yield on this soil. Attempts to improve the permeability of the subsoil using gypsum were inconclusive in the year of application. Similar physical and chemical problems have been identified on other duplex soils throughout Australia. Responses to ameliorative treatments have been variable, and there have often been interactions between treatments. Further improvements in yield on these difficult soils requires a better understanding of the interaction of soil physical, chemical and biological properties, and their interactions with crop physiology.


2021 ◽  
Vol 9 (8) ◽  
pp. 1731
Author(s):  
Arianna Calistri ◽  
Anna Luganini ◽  
Barbara Mognetti ◽  
Elizabeth Elder ◽  
Giulia Sibille ◽  
...  

Although coronaviruses (CoVs) have long been predicted to cause zoonotic diseases and pandemics with high probability, the lack of effective anti-pan-CoVs drugs rapidly usable against the emerging SARS-CoV-2 actually prevented a promptly therapeutic intervention for COVID-19. Development of host-targeting antivirals could be an alternative strategy for the control of emerging CoVs infections, as they could be quickly repositioned from one pandemic event to another. To contribute to these pandemic preparedness efforts, here we report on the broad-spectrum CoVs antiviral activity of MEDS433, a new inhibitor of the human dihydroorotate dehydrogenase (hDHODH), a key cellular enzyme of the de novo pyrimidine biosynthesis pathway. MEDS433 inhibited the in vitro replication of hCoV-OC43 and hCoV-229E, as well as of SARS-CoV-2, at low nanomolar range. Notably, the anti-SARS-CoV-2 activity of MEDS433 against SARS-CoV-2 was also observed in kidney organoids generated from human embryonic stem cells. Then, the antiviral activity of MEDS433 was reversed by the addition of exogenous uridine or the product of hDHODH, the orotate, thus confirming hDHODH as the specific target of MEDS433 in hCoVs-infected cells. Taken together, these findings suggest MEDS433 as a potential candidate to develop novel drugs for COVID-19, as well as broad-spectrum antiviral agents exploitable for future CoVs threats.


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