article · Phytotherapy Research
Aframomum melegueta, a plant known for antiviral activity against RNA viruses, contains compounds that may target key viral and host mechanisms in SARS-CoV-2 infections. Computational screening of one hundred secondary metabolites assessed their binding to the host enzyme furin, the main protease, the nsp16 methyltransferase, and the ACE2 receptor interface. Several molecules, including the diarylheptanoid letestuianin A, a phenylpropanoid derivative, and flavonoids such as quercetin, apigenin, and tectochrysin, bound strongly across multiple targets. In laboratory testing, fruit and seed extracts were separated into six fractions. Kinetic assays showed strong furin inhibition by diethyl ether, acetone, ethyl acetate, and methanol fractions. Specific fractions also completely inhibited a furin-recognition sequence present in the Ebola virus precursor glycoprotein, indicating multi-target therapeutic potential.
Respiratory viruses such as SARS-CoV-2 place immense burdens on healthcare systems with limited access to imported drugs. Identifying bioactive compounds from locally available botanical sources offers a path toward accessible therapeutic options. Demonstrating that constituents of Aframomum melegueta inhibit both viral targets and the host enzyme furin provides evidence to support further investigation into plant-based antiviral treatments.
This research is at an early laboratory stage, consisting of computational modelling and in vitro biochemical assays. The findings could guide pharmaceutical and nutraceutical developers in isolating bioactive molecules or formulating standardised botanical extracts for antiviral drug discovery. Further cell-based assays, safety evaluations, and clinical trials will be necessary before these extracts or isolated secondary metabolites can be developed into validated therapeutic products.
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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 (M pro /3CL pro ), 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 (IC 50 = 0.03 mg/L), acetone (IC 50 = 1.564 mg/L), ethyl‐acetate (IC 50 = 0.382 mg/L) and methanol (IC 50 = 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.
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DOI: 10.1002/ptr.6843
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