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

Abstract

The outbreak of coronavirus disease-2019, caused by severe acute respiratory syndrome coronavirus-2 (SARS-CoV-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, Polyphenols-rich 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 self-nanoemulsifying formulation, composed of 10% oleic acid, 40% tween 20 and propylene glycol 50%, were 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 form nanoemulsion 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 μg/mL presenting a promising antiviral remedy for SARS-CoV-2, which may be attributed to the possible synergism between the extract components.

PLGA/PEG Nanoparticles Loaded with Cyclodextrin-Peganum harmala Alkaloid Complex and Ascorbic Acid with Promising Antimicrobial Activities

“…HARF is reported to exert its antiviral activity by inhibiting the viral polymerase activity and consequently viral RNA replication [59]. On the other hand, the co-encapsulation of ascorbic acid causes a synergistic antiviral effect against the influenza virus by increasing the generation of interferon (IFN)-α/β [60,61].…”

Naturally Available Flavonoid Aglycones as Potential Antiviral Drug Candidates against SARS-CoV-2

“…However, vaccines are a prophylactic approach and cannot be implemented for treatment, especially in pandemic situations [4]. Furthermore, the search for new therapeutic drugs from safe natural sources is crucial during pandemics [2,[5][6][7][8][9][10][11][12][13]. Several naturally existing bioactive compounds were reported to behave as antiviral agents [14][15][16].…”

Coronavirus Disease (COVID-19) Control between Drug Repurposing and Vaccination: A Comprehensive Overview

“…The dramatic history of fighting COVID-19 has a lot of details including the drug repurposing [43][44][45] of different classes and the introduction of many types of emergency vaccines (Figure 2). Herein, we will discuss the aforementioned issues in a sufficiently detailed manner.…”

“…Several herbal medicines have been assessed for their anti-SARS-CoV-2 activity either as crude extracts or as purified plant-origin components. Several herbal extracts and components could hinder SARS-CoV-2 replication in vitro and relieve COVID-19 symptoms in vivo in experimental and clinical settings such as Echinacea purpurea extract, Cuphea Ignea extract, Pomegranate Peel extract and juice (Punica Granatum), Clove (Syzygium aromaticum L.), and bioactive polyphenolic compounds, namely curcumin, quercetin, and hesperidin [2,45,[247][248][249][250][251][252][253]. However, the main limitation of the herbal medicines is still the inconsistency of the antiviral efficacy between the cell-based in vitro assays and in vivo experimental settings due to the high hydrophilicity and low oral bioavailability of the herbal medicine components [254].…”