Antiviral chemistry & chemotherapy · 2016
Derivatives of usnic acid inhibit broad range of influenza viruses and protect mice from lethal influenza infection.
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Shtro A A, Zarubaev V V, Luzina O A, Sokolov D N, Salakhutdinov N F
Аннотация
BACKGROUND: Influenza is a disease of significant morbidity and mortality, the number of anti-influenza drugs is small; many of them stimulate the appearance of resistant strains. In this work, we demonstrate activity of some usnic acid (UA) derivatives against influenza virus in vitro and in vivo.
METHODS: Organic synthesis was used to prepare compounds. Antiviral activity of the compounds in vitro was evaluated by their ability to decrease the virus titer on Madin-Darby Canine Kidney cells. In vivo activity was evaluated by decrease of mortality and index of protection.
RESULTS: Compounds were tested against a broad spectrum of influenza virus strains and showed activity against all used strains. One compound, [5] (valine enamine of UA), also significantly reduced lethality of infected animals and does not give rise to the appearance of resistant strains. Additional studies showed that hepatotoxicity of compound [5] is reduced comparatively to UA.
CONCLUSION: Our results suggest that valine enamine of UA could be a potential candidate for the development of a new anti-influenza therapy.
METHODS: Organic synthesis was used to prepare compounds. Antiviral activity of the compounds in vitro was evaluated by their ability to decrease the virus titer on Madin-Darby Canine Kidney cells. In vivo activity was evaluated by decrease of mortality and index of protection.
RESULTS: Compounds were tested against a broad spectrum of influenza virus strains and showed activity against all used strains. One compound, [5] (valine enamine of UA), also significantly reduced lethality of infected animals and does not give rise to the appearance of resistant strains. Additional studies showed that hepatotoxicity of compound [5] is reduced comparatively to UA.
CONCLUSION: Our results suggest that valine enamine of UA could be a potential candidate for the development of a new anti-influenza therapy.