expresspharmaMay 29, 2020
Tag: COVID-19 , Carprofen , Celecoxib , M-pro
A study, published in the International Journal of Molecular Sciences, has found that two anti-inflammatory drugs, one prescribed for humans and another for animals, may inhibit a key enzyme in the replication or reproduction of the novel coronavirus that causes COVID-19.
Researchers from Universitat Rovira in Spain, in this study, used computer techniques to analyse 6,466 drugs authorised by various drug agencies for both human and veterinary use. They assessed whether these drugs could be used to inhibit the main protease of the virus (M-pro) enzyme, which plays an essential role in the replication of the virus.
They found that a human and a veterinary anti-inflammatory drug — Carprofen and Celecoxib — inhibit a key enzyme in the replication and transcription of the virus responsible for COVID-19.
M-pro enzyme is responsible for cutting two polypeptides — generated by the virus itself — and generating a number of proteins that are essential for the reproduction of the virus, the researchers said.
Some of the trials coordinated by the World Health Organization against the COVID-19 pandemic also aim to inhibit M-pro using two antiretrovirals such as Lopinavir and Ritonavir, drugs initially designed to treat HIV, they said.
In the new study, the researchers predicted that seven of the 6,466 drugs analysed may inhibit M-pro.
The results have been shared with the international initiative of scientists, COVID Moonshot, which has selected two of these seven compounds — Carprofen and Celecoxib — in order to test their ability to inhibit M-pro in vitro.
The findings show that at a concentration of 50 micromolar (μM) of Celecoxib or Carprofen, the inhibition of the in vitro activity of M-pro enzyme is 11.90 and 4.0 per cent, respectively.
Both molecules could be used as a starting point for further lead optimisation to obtain even more potent derivatives, informed the researchers.
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