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1.
Vaccines (Basel) ; 9(11)2021 Nov 12.
Article in English | MEDLINE | ID: covidwho-1512751

ABSTRACT

Respiratory viruses represent a major public health concern, as they are highly mutated, resulting in new strains emerging with high pathogenicity. Currently, the world is suffering from the newly evolving severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). This virus is the cause of coronavirus disease 2019 (COVID-19), a mild-to-severe respiratory tract infection with frequent ability to give rise to fatal pneumonia in humans. The overwhelming outbreak of SARS-CoV-2 continues to unfold all over the world, urging scientists to put an end to this global pandemic through biological and pharmaceutical interventions. Currently, there is no specific treatment option that is capable of COVID-19 pandemic eradication, so several repurposed drugs and newly conditionally approved vaccines are in use and heavily applied to control the COVID-19 pandemic. The emergence of new variants of the virus that partially or totally escape from the immune response elicited by the approved vaccines requires continuous monitoring of the emerging variants to update the content of the developed vaccines or modify them totally to match the new variants. Herein, we discuss the potential therapeutic and prophylactic interventions including repurposed drugs and the newly developed/approved vaccines, highlighting the impact of virus evolution on the immune evasion of the virus from currently licensed vaccines for COVID-19.

2.
Fundam Clin Pharmacol ; 36(1): 160-170, 2022 Feb.
Article in English | MEDLINE | ID: covidwho-1314051

ABSTRACT

BACKGROUND/AIM: SARS-CoV-2 is one of the coronavirus families that emerged at the end of 2019. It infected the respiratory system and caused a pandemic worldwide. Fluoroquinolones (FQs) have been safely used as antibacterial agents for decades. The antiviral activity of FQs was observed. Moreover, substitution on the C-7 position of ciprofloxacin enhanced its antiviral activity. Therefore, this study aims to investigate the antiviral activity of 7-(4-(N-substituted-carbamoyl-methyl)piperazin-1yl)-chalcone in comparison with ciprofloxacin against SARS-CoV-2 main protease (Mpro ). MATERIALS AND METHODS: Vero cells were infected with SARS-CoV-2. After treatment with ciprofloxacin and the chalcone at the concentrations of 1.6, 16, 160 nmol/L for 48 h, SARS-CoV-2 viral load was detected using real-time qPCR, SARS-CoV-2 infectivity was determined using plaque assay, and the main protease enzyme activity was detected using in vitro 3CL-protease inhibition assay. The activity of the chalcone was justified through molecular docking within SARS-CoV-2 Mpro , in comparison with ciprofloxacin. RESULTS: The new chalcone significantly inhibited viral load replication where the EC50 was 3.93 nmol/L, the plaque formation ability of the virus was inhibited to 86.8% ± 2.47. The chalcone exhibited a significant inhibitory effect against SARS-CoV-2 Mpro in vitro in a dose-dependent manner. The docking study into SARS-CoV-2 Mpro active site justified the importance of adding a substitution to the parent drug. Additionally, the assessment of the drug-likeness properties indicated that the chalcone might have acceptable ADMET properties. CONCLUSION: The new chalcone might be useful and has new insights for the inhibition of SARS-CoV-2 Mpro .


Subject(s)
Antiviral Agents/pharmacology , Chalcones , Ciprofloxacin , Coronavirus 3C Proteases/antagonists & inhibitors , SARS-CoV-2/drug effects , Animals , Chalcones/pharmacology , Chlorocebus aethiops , Ciprofloxacin/pharmacology , Molecular Docking Simulation , Molecular Dynamics Simulation , Vero Cells
3.
Nat Prod Res ; 36(11): 2893-2896, 2022 Jun.
Article in English | MEDLINE | ID: covidwho-1240854

ABSTRACT

The ongoing spread of SARS-CoV-2 has created a growing need to develop effective antiviral treatments; therefore, this work was undertaken to delve into the natural metabolites of the Red Sea soft coral Nephthea sp. (family Nephtheidae) as a source of potential anti-COVID-19 agents. Overall, a total of 14 structurally diverse minor constituents were isolated and identified from the petroleum ether fraction of Nephthea sp. The characterised compounds were screened and compared for their inhibitory potential against SARS-CoV-2 main protease (Mpro) using Autodock Vina and MOE software. Interestingly, most compounds were able to bind effectively to the active site of Mpro, of which nephthoside monoacetate (1); an acylated tetraprenyltoluquinol glycoside, exhibited the highest binding capacity in both software with comparable interaction energies to the ligand N3 and moderately acceptable drug-likeness properties, which drew attention to the relevance of marine-derived metabolites from Nephthea sp., particularly compound (1), to develop potential SARS-CoV-2 protease inhibitors.


Subject(s)
Anthozoa , COVID-19 Drug Treatment , Animals , Anthozoa/chemistry , Antiviral Agents/chemistry , Antiviral Agents/pharmacology , Coronavirus 3C Proteases , Molecular Docking Simulation , SARS-CoV-2
4.
Data Brief ; 35: 106851, 2021 Apr.
Article in English | MEDLINE | ID: covidwho-1065011

ABSTRACT

This academic research explicit the data-set of academic difficulties among different age groups of students studying in various schools, colleges or Universities during the COVID-19 induced lockdown. The western part of Uganda comprises 26 districts and the survey was conducted in those regions employing a simple random sampling technique. The dataset is descriptive and an aggregate of 405 students participated in this survey. Among that, 253 students are from rural regions, 59 students are from semi-urban regions and 93 students are from urban regions. This survey was started in April 2020 and data were collected till June 2020. A statistical run was made with the aid of SPSS version 20 software to evaluate the significance level (P-Value<0.05) of each question among the localities.

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