Elsevier

Phytomedicine

Volume 85, May 2021, 153311
Phytomedicine

Review
Screening for natural and derived bio-active compounds in preclinical and clinical studies: One of the frontlines of fighting the coronaviruses pandemic

https://doi.org/10.1016/j.phymed.2020.153311Get rights and content
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open access

Abstract

Background

Starting December 2019, mankind faced an unprecedented enemy, the COVID-19 virus. The world convened in international efforts, experiences and technologies in order to fight the emerging pandemic. Isolation, hygiene measure, diagnosis, and treatment are the most efficient ways of prevention and intervention nowadays. The health organizations and global care systems screened the available resources and offered recommendations of approved and proposed medications. However, the search for a specific selective therapy or vaccine against COVID-19 remains a challenge.

Methods

A literature search was performed for the screening of natural and derived bio-active compounds which showed potent antiviral activity against coronaviruses using published articles, patents, clinical trials website (https://clinicaltrials.gov/) and web databases (PubMed, SCI Finder, Science Direct, and Google Scholar).

Results

Through the screening for natural products with antiviral activities against different types of the human coronavirus, extracts of Lycoris radiata (L'Hér.), Gentiana scabra Bunge, Dioscorea batatas Decne., Cassia tora L., Taxillus chinensis (DC.), Cibotium barometz L. and Echinacea purpurea L. showed a promising effect against SARS-CoV. Out of the listed compound Lycorine, emetine dihydrochloride hydrate, pristimerin, harmine, conessine, berbamine, 4`-hydroxychalcone, papaverine, mycophenolic acid, mycophenolate mofetil, monensin sodium, cycloheximide, oligomycin and valinomycin show potent activity against human coronaviruses. Additionally, it is worth noting that some compounds have already moved into clinical trials for their activity against COVID-19 including fingolimod, methylprednisolone, chloroquine, tetrandrine and tocilizumab.

Conclusion

Natural compounds and their derivatives could be used for developing potent therapeutics with significant activity against SARS-COV-2, providing a promising frontline in the fighting against COVID-19.

Keywords

COVID-19
Natural products
Antiviral
Clinical trials
Patent
Protection

Abbreviations

3CLpro
3C-like protease
ACE2
Angiotensin-converting enzyme 2
ARDS
Acute respiratory distress syndrome
CC50
Half maximal cytotoxic concentration
CD13
Human aminopeptidase N receptor
COVID-19
Corona virus disease 2019
DPP4
Dipeptidyl peptidase 4
Nsp3
Non-structural proteins proteases 3
EC50
Half maximal effective concentration
ER
Endoplasmic reticulum
EtOH
Ethanol
EtOAc
Ethyl acetate
FDA
Food and Drug Administration
HCoV-229E
Human coronavirus 229E
HCoV-HKU1
Human coronavirus Hong Kong University 1
HCoV-NL63
Human coronavirus NL63
HCoV-OC43
Human coronavirus OC43
HIV
Human immunodeficiency Virus
IC50
Half maximal inhibitory concentration
IL-6
Interleukin 6
IL-6R
Interleukin-6 receptor
MERS-CoV
Middle East Respiratory Syndrome Coronavirus
MHV-A59
Coronavirus Murine hepatitis virus
N
Unaltered natural product
ND
Natural product derivative
Nsp5
Non-structural proteins proteases 5
ORF1a/b
Nonstructural open‐reading frames
RdRp
RNA dependent RNA polymerase
RNA
Ribonucleic acid
SARS-CoV
Severe acute respiratory syndrome coronavirus
SARS-CoV-2
Severe acute respiratory syndrome coronavirus 2
TEM
Transmission electron microscope

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