Aframomum melegueta secondary metabolites exhibit polypharmacology against SARS-CoV-2 drug targets : in vitro validation of furin inhibition

© 2020 John Wiley & Sons Ltd..

COVID-19 pandemic is currently decimating the world's most advanced technologies and largest economies and making its way to the continent of Africa. Weak medical infrastructure and over-reliance on medical aids may eventually predict worse outcomes in Africa. To reverse this trend, Africa must re-evaluate the only area with strategic advantage; phytotherapy. One of the many plants with previous antiviral potency is against RNA viruses is Aframomum melegueta. In this study, one hundred (100) A. melegueta secondary metabolites have been mined and computational evaluated for inhibition of host furin, and SARS-COV-2 targets including 3C-like proteinase (Mpro /3CLpro ), 2'-O-ribose methyltransferase (nsp16) and surface glycoprotein/ACE2 receptor interface. Silica-gel column partitioning of A. melegueta fruit/seed resulted in 6 fractions tested against furin activity. Diarylheptanoid (Letestuianin A), phenylpropanoid (4-Cinnamoyl-3-hydroxy-spiro[furan-5,2'-(1'H)-indene]-1',2,3'(2'H,5H)-trione), flavonoids (Quercetin, Apigenin and Tectochrysin) have been identified as high-binding compounds to SARS-COV-2 targets in a polypharmacology manner. Di-ethyl-ether (IC50 = 0.03 mg/L), acetone (IC50 = 1.564 mg/L), ethyl-acetate (IC50 = 0.382 mg/L) and methanol (IC50 = 0.438 mg/L) fractions demonstrated the best inhibition in kinetic assay while DEF, ASF and MEF completely inhibited furin-recognition sequence containing Ebola virus-pre-glycoprotein. In conclusion, A. melegueta and its secondary metabolites have potential for addressing the therapeutic needs of African population during the COVID-19 pandemic.

Medienart:

E-Artikel

Erscheinungsjahr:

2021

Erschienen:

2021

Enthalten in:

Zur Gesamtaufnahme - volume:35

Enthalten in:

Phytotherapy research : PTR - 35(2021), 2 vom: 15. Feb., Seite 908-919

Sprache:

Englisch

Beteiligte Personen:

Omotuyi, I Olaposi [VerfasserIn]
Nash, Oyekanmi [VerfasserIn]
Ajiboye, Basiru O [VerfasserIn]
Olumekun, Victor O [VerfasserIn]
Oyinloye, Babatunji E [VerfasserIn]
Osuntokun, Oludare T [VerfasserIn]
Olonisakin, Adebisi [VerfasserIn]
Ajayi, A Olajide [VerfasserIn]
Olusanya, Olasehinde [VerfasserIn]
Akomolafe, Funmilola S [VerfasserIn]
Adelakun, Niyi [VerfasserIn]

Links:

Volltext

Themen:

Aframomum melegueta
COVID-19
Diarylheptanoid
EC 3.4.21.75
Flavonoids
Furin
Journal Article
Phenylpropanoid
Plant Extracts
SARS-COV-2
Validation Study

Anmerkungen:

Date Completed 03.03.2021

Date Revised 07.12.2022

published: Print-Electronic

Citation Status MEDLINE

doi:

10.1002/ptr.6843

funding:

Förderinstitution / Projekttitel:

PPN (Katalog-ID):

NLM315357126