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Can Antiviral Activity of Licorice Help Fight COVID-19 Infection?

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Can Antiviral Activity of Licorice Help Fight COVID-19 Infection? biomolecules Review Can Antiviral Activity of Licorice Help Fight COVID-19 Infection? Luisa Diomede 1,* , Marten Beeg 1, Alessio Gamba 2 , Oscar Fumagalli 1, Marco Gobbi 1 and Mario Salmona 1,* 1 Department of Molecular Biochemistry and Pharmacology, Istituto di Ricerche Farmacologiche Mario Negri IRCCS, Via Mario Negri 2, 20156 Milano, Italy; [email protected] (M.B.); [email protected] (O.F.); [email protected] (M.G.) 2 Department of Environmental Health Science, Istituto di Ricerche Farmacologiche Mario Negri IRCCS, Via Mario Negri 2, 20156 Milano, Italy; [email protected] * Correspondence: [email protected] (L.D.); [email protected] (M.S.) Abstract: The phytotherapeutic properties of Glycyrrhiza glabra (licorice) extract are mainly attributed to glycyrrhizin (GR) and glycyrrhetinic acid (GA). Among their possible pharmacological actions, the ability to act against viruses belonging to different families, including SARS coronavirus, is particularly important. With the COVID-19 emergency and the urgent need for compounds to counteract the pandemic, the antiviral properties of GR and GA, as pure substances or as components of licorice extract, attracted attention in the last year and supported the launch of two clinical trials. In silico docking studies reported that GR and GA may directly interact with the key players in viral internalization and replication such as angiotensin-converting enzyme 2 (ACE2), spike protein, the host transmembrane serine protease 2, and 3-chymotrypsin-like cysteine protease. In vitro data indicated that GR can interfere with virus entry by directly interacting with ACE2 and spike, with a nonspecific effect on cell and viral membranes. Additional anti-inflammatory and antioxidant effects of GR cannot be excluded. These multiple activities of GR and licorice extract are critically Citation: Diomede, L.; Beeg, M.; Gamba, A.; Fumagalli, O.; Gobbi, M.; re-assessed in this review, and their possible role against the spread of the SARS-CoV-2 and the Salmona, M. Can Antiviral Activity of features of COVID-19 disease is discussed. Licorice Help Fight COVID-19 Infection? Biomolecules 2021, 11, 855. Keywords: licorice; liquorice; glycyrrhizin; glycyrrhizic acid; glycyrrhetinic acid; enoxolone; virus; https://doi.org/10.3390/biom11060855 SARS-CoV-2; COVID-19 Academic Editor: Koen Vandenbroeck 1. Introduction Received: 31 March 2021 In ancient times, readily available plant extracts were the first sources of “drugs”. Accepted: 2 June 2021 The therapeutic use of Glycyrrhiza glabra (licorice) and its extracts dates back to the dawn Published: 8 June 2021 of time. Scholars of the history of medicine date the first information on its medicinal use to over 4000 years ago [1]. Its use has spread thanks to the ease of agricultural Publisher’s Note: MDPI stays neutral cultivation of its fourteen species in many warm and temperate countries. Therefore, with regard to jurisdictional claims in its therapeutic use has been proposed by many cultures and ethnic groups. The study published maps and institutional affil- of its phytotherapeutic properties reflects the remarkable variety of products with some iations. therapeutic activity present above all in the roots of the plant [2–4]. The pathologies for which these extracts have been used in the past are extremely varied and include disorders of the respiratory, gastrointestinal, cardiovascular, and urinary systems. It was also widely used to treat ocular exenteration and neurodegenerative diseases. Copyright: © 2021 by the authors. Even the toxic effects of these extracts have been duly recorded in tradition. Of interest Licensee MDPI, Basel, Switzerland. is the hypothesis on the death of the philosopher Heraclitus of Ephesus, who had decided This article is an open access article to eat only herbs and roots in the last part of his life. Diogenes Laertius describes his death distributed under the terms and as due to hydropsy because of his vast consumption of licorice roots [5]. conditions of the Creative Commons Only in the last decades, with the development of adequate analytical methods, has it Attribution (CC BY) license (https:// creativecommons.org/licenses/by/ become possible to understand the nature of the molecules present in the extracts. This has 4.0/). had decisive importance in defining the molecules’ therapeutic potential. The knowledge Biomolecules 2021, 11, 855. https://doi.org/10.3390/biom11060855 https://www.mdpi.com/journal/biomolecules Biomolecules 2021, 11, x FOR PEER REVIEW 2 of 20 Biomolecules 2021, 11, 855 2 of 21 has had decisive importance in defining the molecules’ therapeutic potential. The knowledge from the “ancient pharmacopeia” has made it possible to identify plants with potentialfrom therapeutic the “ancient activity pharmacopeia” and describe has thei mader properties it possible in a to modern, identify current plants context. with potential Amongtherapeutic the compounds activity and identified, describe their glycyrrhizic properties acid in or a modern,glycyrrhizin current (GR) context. and its me- tabolites, mainlyAmong glycyrrhetinic the compounds acid identified,(GA) or enoxolone, glycyrrhizic are the acid most or glycyrrhizinimportant [1]. (GR) Their and its possiblemetabolites, pharmacological mainly action glycyrrhetinic includes acidthe pa (GA)rticularly or enoxolone, important are ability the mostto act important against [1]. virusesTheir belonging possible to pharmacologicaldifferent families, action including includes the theSARS particularly coronavirus important [6,7]. With ability the to act COVID-19against emergency viruses belonging and the urgent to different need families,for compounds including to theease SARS the pandemic, coronavirus the [6 an-,7]. With tiviralthe properties COVID-19 of GR emergency and GA, and as pure the urgentsubstances need or for as compounds components to of ease licorice the pandemic, extract, the antiviral properties of GR and GA, as pure substances or as components of licorice extract, have attracted fresh attention over the last year. have attracted fresh attention over the last year. This review critically reassesses these aspects, widely investigated over the last year, This review critically reassesses these aspects, widely investigated over the last year, and examines the possible utility of GR and GA against the spread of the SARS-CoV-2 and examines the possible utility of GR and GA against the spread of the SARS-CoV-2 virus. We have reviewed the antiviral properties of GR and GA, as pure substances or as virus. We have reviewed the antiviral properties of GR and GA, as pure substances or components of licorice, from the year 1947 to the date of the search, which involved the as components of licorice, from the year 1947 to the date of the search, which involved following databases: Embase, Medline, and the Cochrane Library. Title, abstract, and key- the following databases: Embase, Medline, and the Cochrane Library. Title, abstract, and word searches were made using Boolean search operators by extract, on the basis of a keyword searches were made using Boolean search operators by extract, on the basis critical systematic analysis of the literature. To retrieve all the pertinent evidence, the of a critical systematic analysis of the literature. To retrieve all the pertinent evidence, search was done on 28 February 2021 with global geographical coverage and time limits the search was done on 28 February 2021 with global geographical coverage and time on the ProQuest search engine: (“licorice” OR “liquorice” OR “glycyrrhiza glabra” OR limits on the ProQuest search engine: (“licorice” OR “liquorice” OR “glycyrrhiza glabra” “glycyrrhizicOR “glycyrrhizic acid” OR glycyrrhizin acid” OR glycyrrhizin OR “glycyrrhetinic OR “glycyrrhetinic acid” OR “enoxolone”) acid” OR “enoxolone”) AND (an- AND tiviral(antiviral OR virus OROR virus hepatitis). OR hepatitis). A total of A 508 total studies of 508 were studies identified were identified after adjusting after adjustingfor duplicates,for duplicates, and then andanalyzed. then analyzed. After applying After applyinga pre-selected a pre-selected inclusion inclusionand exclusion and exclusioncri- teria basedcriteria on based the authors’ on the authors’own experience, own experience, 84 original 84 articles original were articles deemed were pertinent deemed pertinentfor inclusionfor inclusionin this review. in this review. 2. From2. Traditional From Traditional to Medicinal to Medicinal Use of Use Licorice of Licorice Extract Extract The passageThe passage from empirical from empirical and anecdotal and anecdotal “pharmacology “pharmacology and therapy” and therapy” to the to iden- the identi- tificationfication of each of eachcomponent component of the of mixture the mixture has enabled has enabled us to usre-evaluate to re-evaluate licorice licorice extracts extracts in modernin modern terms termsand give and each give component each component potential potential pharmacological pharmacological dignity. dignity. The iden- The identi- tificationfication in the in extracts the extracts of licorice of licorice roots rootsof molecules of molecules with interesting with interesting biological biological activities activities contributedcontributed to its re-evaluation to its re-evaluation (Table (Table 1). The1). diversity The diversity of molecules of molecules described described in these in these extractsextracts makes makes it challenging it challenging to distinguish to distinguish information
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