5 research outputs found

    Battle Against Coronavirus: Repurposing Old Friends (Food Borne Polyphenols) for New Enemy (COVID-19)

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    In the era of extreme scientific development where the scientific community have reached beyond moon, the entire world today is facing an immense problem due to deadly effect of COVID-19 (coronavirus disease), originated in Wuhan. Coronavirus is having dexterity to target immune compromised people very easily and swiftly get transmitted to healthy individuals from infected ones. Coronavirus infections are spreading very rapidly, and almost all the countries around the world are having corona positive people and asymptomatic carriers. This pandemic has created havoc both to human health and economy in lack of an effective treatment against this disease. Due to time limitations and urgency to find cure for COVID 19 we have undertaken the help of structure assisted drug design approach which mainly involves virtual screening program which identifies the structural leads which can target COVID-19 main protease (Mpro). This protease is the key enzyme of coronavirus which plays crucial role in virus replication and transcription, which can be targeted to retard the growth of virus inside the host. In the present work, the Phenol explorer database (version 3.6) containing 751 different food borne polyphenols were screened against the (Mpro) to identify suitable structural leads with potential to inhibit this protease though High throughput modelling and molecular docking approach. We identified six potential polyphenols belonging to Sanguiin, Theaflavin gallate, Theaflavin digallate, Kaempferol, Punicalagin and Protocatechuic acid chemical classes. All the six polyphenols have much higher docking scores ≥ -9.8 kcal/mol as compared to peptidomimetic inhibitor (N3) of COVID 19 virus Mpro. Pharmacokinetic and Drug likeness predictions of these polyphenols were done using SwissADME web tool where Protocatechuic acid shown fairly good results (1 Lipinski violation). The studies suggest the dietary intake of “black tea” can improve the resistance to fight against COVID 19 virus in early stages of human infection. Importantly though, the enriched subset of six compounds identified from the larger library has to be validated experimentally. </p

    Characterization of IGF2R Molecular Expression in Canine Osteosarcoma as Part of a Novel Comparative Oncology Approach

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    Progress in prognostic factors, treatments, and outcome for both canine and human osteosarcoma (OS) has been minimal over the last three decades. Surface overexpression of the cation independent mannose-6-phosphate/insulin-like growth factor receptor type 2 (IGF2R) has been proven to occur in human OS cells. Subsequently, radioimmunotherapy (RIT) targeting IGF2R has demonstrated promising preliminary results. The main aims of this study were to investigate the expression of IGF2R in spontaneously occurring canine OS cells using immunohistochemistry (IHC) on archived biopsy samples and to assess its prognostic significance. Thirty-four dogs were included in the study. All cases showed that 80–100% of OS cells stained positive for IGF2R. IGF2R overexpression alone was not shown to have prognostic significance using both visual and quantitative methods of IHC staining intensity. This study has established for the first time the consistent expression of IGF2R in spontaneously occurring canine OS. This comparative oncology approach will allow further investigation into RIT as a novel treatment modality; first in canines and then in humans with OS. In addition, further studies should be performed to assess the true prognostic significance of IGF2R overexpression

    Bioactive peptides as functional food ingredients

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    Bioactive Peptides as Functional Food Ingredients, Barberis et al. describe the useful roles of bioactive peptides and tools to improve their nutraceutical impact by reducing limitations, such as low bioavailability due to the gastrointestinal digestion, poor transportability through the membranes, and rapid plasma clearance. Bioactive peptides are protein specific portions of 2 to 20 amino acid residues with desirable biological activities, based on their composition and sequence. Databases report about 3000 peptide sequences with potential activities (antioxidant, anti-hypertensive, antithrombotic, anti-adipogenic, antimicrobial, anti-inflammatory).The bioactive peptides are inactive within parent protein, but can be released during gastrointestinal digestion and the food processing. It is assumed that peptides have high specificity in target tissues; none or little toxicity, neither accumulation in the organism, and easy degradability in the environment. However, their usefulness as nutraceuticals is limited by the low bioavailability due to the gastrointestinal digestion, poor transportability through the membranes and rapid plasma clearance. This Chapter reviews the different technologies for the production of bioactive peptides: extraction from natural sources; production by recombinant DNA technology, production in cell-free expression systems, production in transgenic animals and plants, fermentation, chemical and enzymatic synthesis. Although the size of the molecule will determine the technology most suitable for its production, this Chapter emphasizes in the synthesis, chemical and enzymatic, of bioactive peptides.Finally, chemical and enzymatic strategies are discussed to enhance absorption; effectiveness and bioavailability; study molecular mechanisms of activity and assess the safety of these functional ingredients.Fil: Barberis, Sonia Esther. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - San Luis. Instituto de Física Aplicada "Dr. Jorge Andrés Zgrablich". Universidad Nacional de San Luis. Facultad de Ciencias Físico Matemáticas y Naturales. Instituto de Física Aplicada "Dr. Jorge Andrés Zgrablich"; ArgentinaFil: Origone, Anabella Lucía. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - San Luis. Instituto de Física Aplicada "Dr. Jorge Andrés Zgrablich". Universidad Nacional de San Luis. Facultad de Ciencias Físico Matemáticas y Naturales. Instituto de Física Aplicada "Dr. Jorge Andrés Zgrablich"; ArgentinaFil: Adaro, Mauricio Omar. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - San Luis. Instituto de Física Aplicada "Dr. Jorge Andrés Zgrablich". Universidad Nacional de San Luis. Facultad de Ciencias Físico Matemáticas y Naturales. Instituto de Física Aplicada "Dr. Jorge Andrés Zgrablich"; ArgentinaFil: Bersi, Grisel. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - San Luis. Instituto de Física Aplicada "Dr. Jorge Andrés Zgrablich". Universidad Nacional de San Luis. Facultad de Ciencias Físico Matemáticas y Naturales. Instituto de Física Aplicada "Dr. Jorge Andrés Zgrablich"; Argentin
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