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      Potential of Flavonoid-Inspired Phytomedicines against COVID-19

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          Abstract

          Flavonoids are widely used as phytomedicines. Here, we report on flavonoid phytomedicines with potential for development into prophylactics or therapeutics against coronavirus disease 2019 (COVID-19). These flavonoid-based phytomedicines include: caflanone, Equivir, hesperetin, myricetin, and Linebacker. Our in silico studies show that these flavonoid-based molecules can bind with high affinity to the spike protein, helicase, and protease sites on the ACE2 receptor used by the severe acute respiratory syndrome coronavirus 2 to infect cells and cause COVID-19. Meanwhile, in vitro studies show potential of caflanone to inhibit virus entry factors including, ABL-2, cathepsin L, cytokines (IL-1β, IL-6, IL-8, Mip-1α, TNF-α), and PI4Kiiiβ as well as AXL-2, which facilitates mother-to-fetus transmission of coronavirus. The potential for the use of smart drug delivery technologies like nanoparticle drones loaded with these phytomedicines to overcome bioavailability limitations and improve therapeutic efficacy are discussed.

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          Most cited references 18

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          Flavonoid Bioavailability and Attempts for Bioavailability Enhancement

          Flavonoids are a group of phytochemicals that have shown numerous health effects and have therefore been studied extensively. Of the six common food flavonoid classes, flavonols are distributed ubiquitously among different plant foods whereas appreciable amounts of isoflavones are found in leguminous plant-based foods. Flavonoids have shown promising health promoting effects in human cell culture, experimental animal and human clinical studies. They have shown antioxidant, hypocholesterolemic, anti-inflammatory effects as well as ability to modulate cell signaling and gene expression related disease development. Low bioavailability of flavonoids has been a concern as it can limit or even hinder their health effects. Therefore, attempts to improve their bioavailability in order to improve the efficacy of flavonoids are being studied. Further investigations on bioavailability are warranted as it is a determining factor for flavonoid biological activity.
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            Inhibition of Angiotensin-Converting Enzyme Activity by Flavonoids: Structure-Activity Relationship Studies

            Previous studies have demonstrated that certain flavonoids can have an inhibitory effect on angiotensin-converting enzyme (ACE) activity, which plays a key role in the regulation of arterial blood pressure. In the present study, 17 flavonoids belonging to five structural subtypes were evaluated in vitro for their ability to inhibit ACE in order to establish the structural basis of their bioactivity. The ACE inhibitory (ACEI) activity of these 17 flavonoids was determined by fluorimetric method at two concentrations (500 µM and 100 µM). Their inhibitory potencies ranged from 17 to 95% at 500 µM and from 0 to 57% at 100 µM. In both cases, the highest ACEI activity was obtained for luteolin. Following the determination of ACEI activity, the flavonoids with higher ACEI activity (i.e., ACEI >60% at 500 µM) were selected for further IC50 determination. The IC50 values for luteolin, quercetin, rutin, kaempferol, rhoifolin and apigenin K were 23, 43, 64, 178, 183 and 196 µM, respectively. Our results suggest that flavonoids are an excellent source of functional antihypertensive products. Furthermore, our structure-activity relationship studies show that the combination of sub-structures on the flavonoid skeleton that increase ACEI activity is made up of the following elements: (a) the catechol group in the B-ring, (b) the double bond between C2 and C3 at the C-ring, and (c) the cetone group in C4 at the C-ring. Protein-ligand docking studies are used to understand the molecular basis for these results.
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              More than 80 clinical trials launch to test coronavirus treatments

               Amy Maxmen (2020)
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                Author and article information

                Contributors
                Role: Academic Editor
                Journal
                Molecules
                Molecules
                molecules
                Molecules
                MDPI
                1420-3049
                11 June 2020
                June 2020
                : 25
                : 11
                Affiliations
                [1 ]Brigham and Women’s Hospital, Harvard Medical School, Boston, MA 02115, USA
                [2 ]Dana-Farber Cancer Institute, Harvard Medical School, Boston, MA 02115, USA
                [3 ]Northeastern University, Boston, MA 02115, USA; rajivtondak@ 123456gmail.com
                [4 ]R&D Biomedical Materials, Millipore Sigma, Milwaukee, WI 02115, USA
                [5 ]Global Research and Discovery Group Sciences, Winter Haven, FL 33884, USA; d.thompson@ 123456globalrdg.com (D.T.); william.lyerly@ 123456gmail.com (W.L.); rmoore@ 123456phrockwood.com (R.M.)
                [6 ]School of Pharmacy, Concordia University of Wisconsin, Mequon, WI 53097, USA; Terry-Elinor.Reid@ 123456cuw.edu
                [7 ]Vilotos Pharmaceuticals Inc, Baltimore, MD 21202, USA; lowebiotech@ 123456gmail.com (H.L.); ngeh.toyang@ 123456flavocure.com (N.T.)
                [8 ]Flavocure Biotech Inc, Baltimore, MD 21202, USA
                Author notes
                [* ]Correspondence: wngwa@ 123456bwh.harvard.edu
                Article
                molecules-25-02707
                10.3390/molecules25112707
                7321405
                32545268
                © 2020 by the authors.

                Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license ( http://creativecommons.org/licenses/by/4.0/).

                Categories
                Communication

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