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  1. Article ; Online: Glycyrrhizin

    Bailly, Christian / Vergoten, Gérard

    Pharmacology & Therapeutics

    An alternative drug for the treatment of COVID-19 infection and the associated respiratory syndrome?

    2020  Volume 214, Page(s) 107618

    Keywords Pharmacology (medical) ; Pharmacology ; covid19
    Language English
    Publisher Elsevier BV
    Publishing country us
    Document type Article ; Online
    ZDB-ID 194735-7
    ISSN 1879-016X ; 0163-7258
    ISSN (online) 1879-016X
    ISSN 0163-7258
    DOI 10.1016/j.pharmthera.2020.107618
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  2. Article ; Online: Glycyrrhizin: An alternative drug for the treatment of COVID-19 infection and the associated respiratory syndrome?

    Bailly, Christian / Vergoten, Gérard

    Pharmacology & therapeutics

    2020  Volume 214, Page(s) 107618

    Abstract: Safe and efficient drugs to combat the current COVID-19 pandemic are urgently needed ... rapidly evaluated for the treatment of patients with COVID-19. ... associated Human and animal coronaviruses. GLR is a non-hemolytic saponin and a potent immuno-active ...

    Abstract Safe and efficient drugs to combat the current COVID-19 pandemic are urgently needed. In this context, we have analyzed the anti-coronavirus potential of the natural product glycyrrhizic acid (GLR), a drug used to treat liver diseases (including viral hepatitis) and specific cutaneous inflammation (such as atopic dermatitis) in some countries. The properties of GLR and its primary active metabolite glycyrrhetinic acid are presented and discussed. GLR has shown activities against different viruses, including SARS-associated Human and animal coronaviruses. GLR is a non-hemolytic saponin and a potent immuno-active anti-inflammatory agent which displays both cytoplasmic and membrane effects. At the membrane level, GLR induces cholesterol-dependent disorganization of lipid rafts which are important for the entry of coronavirus into cells. At the intracellular and circulating levels, GLR can trap the high mobility group box 1 protein and thus blocks the alarmin functions of HMGB1. We used molecular docking to characterize further and discuss both the cholesterol- and HMG box-binding functions of GLR. The membrane and cytoplasmic effects of GLR, coupled with its long-established medical use as a relatively safe drug, make GLR a good candidate to be tested against the SARS-CoV-2 coronavirus, alone and in combination with other drugs. The rational supporting combinations with (hydroxy)chloroquine and tenofovir (two drugs active against SARS-CoV-2) is also discussed. Based on this analysis, we conclude that GLR should be further considered and rapidly evaluated for the treatment of patients with COVID-19.
    MeSH term(s) Alarmins/drug effects ; Betacoronavirus ; COVID-19 ; Coronavirus Infections/drug therapy ; Coronavirus Infections/epidemiology ; Drug Therapy, Combination ; Glycyrrhizic Acid/pharmacology ; Glycyrrhizic Acid/therapeutic use ; Humans ; Hydroxychloroquine/therapeutic use ; Membrane Microdomains/drug effects ; Molecular Docking Simulation ; Pandemics ; Pneumonia, Viral/drug therapy ; Pneumonia, Viral/epidemiology ; SARS-CoV-2 ; Tenofovir/therapeutic use
    Chemical Substances Alarmins ; Hydroxychloroquine (4QWG6N8QKH) ; Glycyrrhizic Acid (6FO62043WK) ; Tenofovir (99YXE507IL)
    Keywords covid19
    Language English
    Publishing date 2020-06-24
    Publishing country England
    Document type Journal Article ; Review
    ZDB-ID 194735-7
    ISSN 1879-016X ; 0163-7258
    ISSN (online) 1879-016X
    ISSN 0163-7258
    DOI 10.1016/j.pharmthera.2020.107618
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article: Glycyrrhizin: An alternative drug for the treatment of COVID-19 infection and the associated respiratory syndrome?

    Bailly, Christian / Vergoten, Gérard

    Pharmacol Ther

    Abstract: Safe and efficient drugs to combat the current COVID-19 pandemic are urgently needed ... rapidly evaluated for the treatment of patients with COVID-19. ... associated Human and animal coronaviruses. GLR is a non-hemolytic saponin and a potent immuno-active ...

    Abstract Safe and efficient drugs to combat the current COVID-19 pandemic are urgently needed. In this context, we have analyzed the anti-coronavirus potential of the natural product glycyrrhizic acid (GLR), a drug used to treat liver diseases (including viral hepatitis) and specific cutaneous inflammation (such as atopic dermatitis) in some countries. The properties of GLR and its primary active metabolite glycyrrhetinic acid are presented and discussed. GLR has shown activities against different viruses, including SARS-associated Human and animal coronaviruses. GLR is a non-hemolytic saponin and a potent immuno-active anti-inflammatory agent which displays both cytoplasmic and membrane effects. At the membrane level, GLR induces cholesterol-dependent disorganization of lipid rafts which are important for the entry of coronavirus into cells. At the intracellular and circulating levels, GLR can trap the high mobility group box 1 protein and thus blocks the alarmin functions of HMGB1. We used molecular docking to characterize further and discuss both the cholesterol- and HMG box-binding functions of GLR. The membrane and cytoplasmic effects of GLR, coupled with its long-established medical use as a relatively safe drug, make GLR a good candidate to be tested against the SARS-CoV-2 coronavirus, alone and in combination with other drugs. The rational supporting combinations with (hydroxy)chloroquine and tenofovir (two drugs active against SARS-CoV-2) is also discussed. Based on this analysis, we conclude that GLR should be further considered and rapidly evaluated for the treatment of patients with COVID-19.
    Keywords covid19
    Publisher WHO
    Document type Article
    Note WHO #Covidence: #613022
    Database COVID19

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