Browsing by Author "Kutkat, Omnia"

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    Delineating a potent antiviral activity of Cuphea ignea extract loaded nano-formulation against SARS-CoV-2: In silico and in vitro studies
    (Elsevier, 9/15/2021) Mahmoud, Dina B; Ismail, Walaa M; Moatasim, Yassmin; Kutkat, Omnia; ElMeshad, Aliaa N; Ezzat, Shahira M; El Deeb, Kadriya S; El-Fishawy, Ahlam M; Gomaa, Mokhtar R; Kandeil, Ahmed; Al-karmalawy, Ahmed A; Ali, Mohamed A; Mostafa, Ahmed
    Journal of Drug Delivery Science and Technology Available online 15 September 2021, 102845 In Press, Journal Pre-proofWhat are Journal Pre-proof articles? Delineating a potent antiviral activity of Cuphea ignea extract loaded nano-formulation against SARS-CoV-2: In silico and in vitro studies Author links open overlay panelDina B.MahmoudaWalaa M.IsmailbYassminMoatasimcOmniaKutkatcAliaa N.ElMeshaddeShahira M.EzzatbfKadriya S.El DeebbAhlam M.El-FishawybMokhtar R.GomaacAhmedKandeilcAhmed A.Al-karmalawygMohamed A.AlicAhmedMostafac a Pharmaceutics Department, National Organization for Drug Control and Research, Giza, Egypt b Department of Pharmacognosy, Faculty of Pharmacy, Cairo University, Kasr-El-Ainy Street, Cairo, 11562, Egypt c Center of Scientific Excellence for Influenza Viruses, National Research Centre, Giza, Egypt d Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Kasr-El-Ainy Street, Cairo, 11562, Egypt e Faculty of Nanotechnology for Postgraduate Studies, Cairo University, El Sheikh Zayed, Giza, 12588, Egypt f Department of Pharmacognosy, Faculty of Pharmacy, October University for Modern Sciences and Arts (MSA), Giza, 12451, Egypt g Department of Pharmaceutical Medicinal Chemistry, Faculty of Pharmacy, Horus University-Egypt, New Damietta, 34518, Egypt Received 7 March 2021, Revised 17 July 2021, Accepted 5 September 2021, Available online 15 September 2021. https://doi.org/10.1016/j.jddst.2021.102845 Get rights and content 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.
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    Drug repurposing of pyrazolotriazine derivatives as potential anti-SARS-CoV-2 agents: in vitro and in silico studies
    (BioMed Central Ltd, 2024-07) Oudah, Khulood H; Najm, Mazin A. A; Barghash, Reham F; Kutkat, Omnia; GabAllah, Mohamed; Albohy, Amgad; Abouzid, Khaled A. M
    The search for new molecules targeting SARS-CoV-2 has been a priority since 2020. The continuous evolution of new mutants increases the need for more research in the area. One way to find new leads is to repurpose existing drugs and molecules against the required target. Here, we present the in vitro and in silico screening of ten previously synthesized and reported compounds as anti-COVID 19 agents. The compounds were screened in vitro against VERO-E6 cells to find their Cytotoxic Concentration (CC50) and their Inhibitory Concentration (IC50). Compounds 1, 2, and 5 revealed a promising anti-SARS-CoV-2 of (IC50 = 2.4, 11.2 and 2.8 µM), respectively while compounds 3 and 7 showed moderate activity of (IC50 = 17.8 and 26.1 µM) compared to Chloroquine which showed an IC50 of 24.9 µM. Among tested compounds, 1 showed the highest selectivity (CC50/IC50) of 192.8. Docking, molecular dynamics and ADME studies were done to investigate potential interactions between compounds and SARS-CoV-2 targets as well as to study the possibility of using them as lead compounds.