Antiviral activities of halogenated emodin derivatives against human coronavirus NL63
| Autor: | Monika Horvat, Jernej Iskra, Martina Avbelj, Mihailo Banjanac, Hrvoje Petković, María Beatriz Durán-Alonso |
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| Přispěvatelé: | Slovenian Research Agency, European Commission, Horvat, Monika [0000-0002-2630-9845], Durán Alonso, Beatriz [0000-0001-7784-0591], Iskra, Jernej [0000-0001-6340-3577], Horvat, Monika, Durán Alonso, Beatriz, Iskra, Jernej |
| Jazyk: | angličtina |
| Rok vydání: | 2021 |
| Předmět: |
2420 Virología
Emodin Halogenation Cell Survival Pharmaceutical Science Electrophilic aromatic substitution Pharmacology Anthraquinone Halogenated emodin Article Analytical Chemistry chemistry.chemical_compound QD241-441 udc:547.672 Nitration Drug Discovery Chlorocebus aethiops Animals Humans Physical and Theoretical Chemistry antiviral activities Vero Cells Alanine Organic Chemistry Medical virology COVID-19 Biological activity human coronavirus NL63 COVID-19 (Disease) - Treatment Adenosine Monophosphate halogeniran emodin Coronavirus NL63 Human protivirusna aktivnost Antiviral agents chemistry Chemistry (miscellaneous) Toxicity Vero cell Molecular Medicine Antiviral activities človeški koronavirus NL63 Coronavirus Infections Human coronavirus NL63 |
| Zdroj: | Molecules Volume 26 Issue 22 Digital.CSIC. Repositorio Institucional del CSIC instname Molecules, vol. 26, no. 22, 6825, 2021. Molecules, Vol 26, Iss 6825, p 6825 (2021) |
| ISSN: | 1420-3049 |
| DOI: | 10.3390/molecules26226825 |
| Popis: | Producción Científica 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. Agencia Pública para la Actividad de Investigación de Eslovenia - (Grant P1-0134 and P4–0116) |
| Databáze: | OpenAIRE |
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