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Título
Antiviral activities of halogenated emodin derivatives against human coronavirus NL63
Autor
Año del Documento
2021
Editorial
MDPI
Descripción
Producción Científica
Documento Fuente
Molecules, 2021, Vol. 26, Nº. 22, 6825
Resumen
The current COVID-19 outbreak has highlighted the need for the development of new vaccines and drugs to combat Severe Acute Respiratory Syndrome-Coronavirus-2 (SARS-CoV-2). Recently, various drugs have been proposed as potentially effective against COVID-19, such as remdesivir, infliximab and imatinib. Natural plants have been used as an alternative source of drugs for thousands of years, and some of them are effective for the treatment of various viral diseases. Emodin (1,3,8-trihydroxy-6-methylanthracene-9,10-dione) is a biologically active anthraquinone with antiviral activity that is found in various plants. We studied the selectivity of electrophilic aromatic substitution reactions on an emodin core (halogenation, nitration and sulfonation), which resulted in a library of emodin derivatives. The main aim of this work was to carry out an initial evaluation of the potential to improve the activity of emodin against human coronavirus NL63 (HCoV-NL63) and also to generate a set of initial SAR guidelines. We have prepared emodin derivatives which displayed significant anti-HCoV-NL63 activity. We observed that halogenation of emodin can improve its antiviral activity. The most active compound in this study was the iodinated emodin analogue E_3I, whose anti-HCoV-NL63 activity was comparable to that of remdesivir. Evaluation of the emodin analogues also revealed some unwanted toxicity to Vero cells. Since new synthetic routes are now available that allow modification of the emodin structure, it is reasonable to expect that analogues with significantly improved anti-HCoV-NL63 activity and lowered toxicity may thus be generated.
Materias (normalizadas)
COVID-19
COVID-19 (Disease) - Treatment
Antiviral agents
Medical virology
Pharmacology
Materias Unesco
2420 Virología
Palabras Clave
Emodin
Halogenated emodin
ISSN
1420-3049
Revisión por pares
SI
Patrocinador
Agencia Pública para la Actividad de Investigación de Eslovenia - (Grant P1-0134 and P4–0116)
Version del Editor
Propietario de los Derechos
© 2021 The authors
Idioma
eng
Tipo de versión
info:eu-repo/semantics/publishedVersion
Derechos
openAccess
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