RT info:eu-repo/semantics/article
T1 Antiviral activities of halogenated emodin derivatives against human coronavirus NL63
A1 Horvat, Monika
A1 Avbelj, Martina
A1 Durán Alonso, María Beatriz
A1 Banjanac, Mihailo
A1 Petković, Hrvoje
A1 Iskra, Jernej
K1 COVID-19
K1 COVID-19 (Disease) - Treatment
K1 Antiviral agents
K1 Medical virology
K1 Pharmacology
K1 Emodin
K1 Halogenated emodin
K1 2420 Virología
AB 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.
PB MDPI
SN 1420-3049
YR 2021
FD 2021
LK https://uvadoc.uva.es/handle/10324/59088
UL https://uvadoc.uva.es/handle/10324/59088
LA eng
NO Molecules, 2021, Vol. 26, Nº. 22, 6825
NO Producción Científica
DS UVaDOC
RD 17-jul-2024