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Molecules ; 27(5)2022 Mar 07.
Artículo en Inglés | MEDLINE | ID: covidwho-1732132

RESUMEN

The COVID-19 pandemic has led to the search for new molecules with antiviral activity against SARS-CoV-2. The entry of the virus into the cell is one of the main targets for inhibiting SARS-CoV-2 infection. Natural products are an important source of new therapeutic alternatives against diseases. Pseudotyped viruses allow the study of SARS-CoV-2 viral entry inhibitors, and due to their simplicity, they allow the screening of a large number of antiviral candidates in Biosafety Level 2 facilities. We used pseudotyped HIV-1 with the D614G SARS-CoV-2 spike glycoprotein to test its ability to infect ACE2-expressing HEK 293T cells in the presence of diverse natural products, including 21 plant extracts, 7 essential oils, and 13 compounds from plants and fungi. The 50% cytotoxic concentration (CC50) was evaluated using the resazurin method. From these analyses, we determined the inhibitory activity of the extract of Stachytarpheta cayennensis, which had a half-maximal inhibitory concentration (IC50) of 91.65 µg/mL, a CC50 of 693.5 µg/mL, and a selectivity index (SI) of 7.57, indicating its potential use as an inhibitor of SARS-CoV-2 entry. Moreover, our work indicates the usefulness of the pseudotyped-virus system in the screening of SARS-CoV-2 entry inhibitors.


Asunto(s)
Antivirales/farmacología , Productos Biológicos/química , Internalización del Virus/efectos de los fármacos , Actinobacteria/química , Actinobacteria/metabolismo , Enzima Convertidora de Angiotensina 2/genética , Enzima Convertidora de Angiotensina 2/metabolismo , Antivirales/química , Antivirales/metabolismo , Antivirales/uso terapéutico , Productos Biológicos/metabolismo , Productos Biológicos/farmacología , Productos Biológicos/uso terapéutico , COVID-19/virología , Células HEK293 , Ensayos Analíticos de Alto Rendimiento/métodos , Humanos , Aceites Volátiles/química , Aceites Volátiles/farmacología , Aceites Volátiles/uso terapéutico , Extractos Vegetales/química , Extractos Vegetales/metabolismo , Extractos Vegetales/farmacología , SARS-CoV-2/aislamiento & purificación , SARS-CoV-2/fisiología , Glicoproteína de la Espiga del Coronavirus/antagonistas & inhibidores , Glicoproteína de la Espiga del Coronavirus/metabolismo , Tratamiento Farmacológico de COVID-19
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