4.5 Article

Delineating a potent antiviral activity of Cuphea ignea extract loaded nano-formulation against SARS-CoV-2: In silico and in vitro studies

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ELSEVIER
DOI: 10.1016/j.jddst.2021.102845

Keywords

Antiviral; Covid-19; Cuphea ignea; Molecular docking; Nanoemulsion; Polyphenols; SARS-CoV-2

Funding

  1. NRC [MP120801]
  2. Egyptian Academy of Scientific Research & Technology (ASRT) within the Ideation Fund program [7303]

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The study found that polyphenol-rich Cuphea ignea extract has the potential to combat SARS-CoV-2, and a self-nanoemulsifying formulation can enhance solubility and enable combined delivery, offering a new direction for antiviral treatment.
The outbreak of coronavirus disease-2019, caused by severe acute respiratory syndrome coronavirus-2 (SARSCoV-2) is a worldwide emerging crisis. Polyphenols are a class of herbal metabolites with a broad-spectrum antiviral activity. However, most polyphenols encounter limited efficacy due to their poor solubility and degradation in neutral and basic environments. Thus, the effectiveness of their pharmaceutical application is critically dependent on the delivery systems to overcome the aforementioned drawbacks. Herein, Polyphenolsrich Cuphea ignea extract was prepared and its constituents were identified and quantified. Molecular docking was conducted for 15 compounds in the extract against SARS-CoV-2 main protease, among which rutin, myricetin-3-O-rhamnoside and rosmarinic acid depicted the most promising antiviral activity. Further, a selfnanoemulsifying formulation, composed of 10% oleic acid, 40% tween 20 and propylene glycol 50%, was prepared to improve the solubility of the extract components and enable its concurrent delivery permitting combined potency. Upon dilution with aqueous phases, the formulation rapidly Formsnanoemulsion of good stability and excellent dissolution profile in acidic pH when compared to the crude extract. It inhibited SARS-CoV-2 completely in vitro at a concentration as low as 5.87 mu g/mL presenting a promising antiviral remedy for SARS-CoV-2, which may be attributed to the possible synergism between the extract components.

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