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1.
Future Microbiol ; 16: 119-130, 2021 01.
Article in English | MEDLINE | ID: covidwho-1389070

ABSTRACT

A review of nasal sprays and gargles with antiviral properties suggests that a number of commonly used antiseptics including povidone-iodine, Listerine®, iota-carrageenan and chlorhexidine should be studied in clinical trials to mitigate both the progression and transmission of SARS-CoV-2. Several of these antiseptics have demonstrated the ability to cut the viral load of SARS-CoV-2 by 3-4 log10 in 15-30 s in vitro. In addition, hypertonic saline targets viral replication by increasing hypochlorous acid inside the cell. A number of clinical trials are in process to study these interventions both for prevention of transmission, prophylaxis after exposure, and to diminish progression by reduction of viral load in the early stages of infection.


Subject(s)
Anti-Infective Agents, Local/administration & dosage , Anti-Infective Agents, Local/therapeutic use , COVID-19/prevention & control , SARS-CoV-2/drug effects , COVID-19/transmission , Carrageenan/therapeutic use , Chlorhexidine/therapeutic use , Drug Combinations , Hydrogen Peroxide/therapeutic use , Nasal Sprays , Oils, Volatile/therapeutic use , Povidone-Iodine/therapeutic use , Salicylates/therapeutic use , Terpenes/therapeutic use , Viral Load/drug effects
2.
Fitoterapia ; 152: 104909, 2021 Jul.
Article in English | MEDLINE | ID: covidwho-1203052

ABSTRACT

3-Chymotrypsin-like protease (3CLpro) is a virally encoded main proteinase that is pivotal for the viral replication across a broad spectrum of coronaviruses. This study aims to discover the naturally occurring SARS-CoV-2 3CLpro inhibitors from herbal constituents, as well as to investigate the inhibitory mechanism of the newly identified efficacious SARS-CoV-2 3CLpro inhibitors. Following screening of the inhibitory potentials of eighty herbal products against SARS-CoV-2 3CLpro, Ginkgo biloba leaves extract (GBLE) was found with the most potent SARS-CoV-2 3CLpro inhibition activity (IC50 = 6.68 µg/mL). Inhibition assays demonstrated that the ginkgolic acids (GAs) and the bioflavones isolated from GBLE displayed relatively strong SARS-CoV-2 3CLpro inhibition activities (IC50 < 10 µM). Among all tested constituents, GA C15:0, GA C17:1 and sciadopitysin displayed potent 3CLpro inhibition activities, with IC50 values of less than 2 µM. Further inhibition kinetic studies and docking simulations clearly demonstrated that two GAs and sciadopitysin strongly inhibit SARS-CoV-2 3CLprovia a reversible and mixed inhibition manner. Collectively, this study found that both GBLE and the major constituents in this herbal product exhibit strong SARS-CoV-2 3CLpro inhibition activities, which offer several promising leading compounds for developing novel anti-COVID-19 medications via targeting on 3CLpro.


Subject(s)
Antiviral Agents/pharmacology , COVID-19 , Coronavirus Protease Inhibitors/pharmacology , Ginkgo biloba/chemistry , Plant Extracts/pharmacology , SARS-CoV-2/drug effects , Virus Replication/drug effects , Antiviral Agents/therapeutic use , Biflavonoids/pharmacology , Biflavonoids/therapeutic use , COVID-19/drug therapy , Coronavirus Protease Inhibitors/therapeutic use , Flavones/pharmacology , Flavones/therapeutic use , Humans , Molecular Structure , Phytotherapy , Plant Extracts/therapeutic use , Plant Leaves/chemistry , SARS-CoV-2/enzymology , Salicylates/pharmacology , Salicylates/therapeutic use
3.
Future Microbiol ; 16: 119-130, 2021 01.
Article in English | MEDLINE | ID: covidwho-1034857

ABSTRACT

A review of nasal sprays and gargles with antiviral properties suggests that a number of commonly used antiseptics including povidone-iodine, Listerine®, iota-carrageenan and chlorhexidine should be studied in clinical trials to mitigate both the progression and transmission of SARS-CoV-2. Several of these antiseptics have demonstrated the ability to cut the viral load of SARS-CoV-2 by 3-4 log10 in 15-30 s in vitro. In addition, hypertonic saline targets viral replication by increasing hypochlorous acid inside the cell. A number of clinical trials are in process to study these interventions both for prevention of transmission, prophylaxis after exposure, and to diminish progression by reduction of viral load in the early stages of infection.


Subject(s)
Anti-Infective Agents, Local/administration & dosage , Anti-Infective Agents, Local/therapeutic use , COVID-19/prevention & control , SARS-CoV-2/drug effects , COVID-19/transmission , Carrageenan/therapeutic use , Chlorhexidine/therapeutic use , Drug Combinations , Hydrogen Peroxide/therapeutic use , Nasal Sprays , Oils, Volatile/therapeutic use , Povidone-Iodine/therapeutic use , Salicylates/therapeutic use , Terpenes/therapeutic use , Viral Load/drug effects
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