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Targeting SARS-CoV-2 Spike Protein of COVID-19 with Naturally Occurring Phytochemicals: An In Silico Study for Drug Development - Jitendra Subhash Rane, Aroni Chatterjee, Abhijeet Kumar & Shashikant Ray - chemRxiv (8 Apr. 2020):
“Fisetin, quercetin, isorhamnetin, genistein, luteolin, resveratrol and apigenin on the other hand, interact with the S2 domain of spike protein with the binding energies of -8.5, -8.5, -8.3, -8.2, -8.2, -7.9, -7.7 Kcal/mol, respectively. Our study suggested that, these flavonoid and non-flavonoid moieties have significantly high binding affinity for the two main important domains of the spike protein which is responsible for the attachment and internalization of the virus in the host cell and their binding affinities are much higher compared to that of HCQ.”
Natural Compounds as Potential Inhibitors of Novel Coronavirus (COVID-19) Main Protease: An In Silico Study - Amaresh Mishra, Yamini Pathak & Vishwas Tripathi - Research Square (15 Apr. 2020):
“We also investigated the similarity of these compounds, if any, with FDA approved drugs using Swiss similarity. The docking results were found in the order of Amentoflavone (-9.13 kcal/mol), Ritonavir (-8.52 kcal/mol), Lopinavir (-8.5 kcal/mol), Puerarin (-7.97 kcal/mol), Maslinic acid (-7.97 kcal/mol), Piperine (-7.65 kcal/mol), Gallocatechin gallate (-7.59 kcal/mol), Luteolin (-7.58 kcal/mol), Apigenin (-7.42 kcal/mol), Resveratrol (-7.41 kcal/mol), Herbacetin (-7.4 kcal/mol), Daidzein (-7.32 kcal/mol), Rhoifolin (-6.71 kcal/mol), Ganomycin B (-6.46 kcal/mol), Epigallocatechin (-6.13 kcal/mol), and Pectolinarin (-5.88 kcal/mol).”
To learn more about Ingredient #21 (Apigenin) - and the 51 other dietary ingredients identified as exhibiting anti-viral and/or immune-enhancing properties - obtain a copy of the full report of AVD: The Anti-Viral Diet by pressing the button below:
Antiviral Agents of Plant Origin. Antiherpetic Activity of Acacetin - K. Hayashi, T. Hayashl, M. Arisawa & N. Morita - Antiviral Chemistry & Chemotherapy (1993) [Of relevance due to the molecular proximity of Acacetin and Apigenin].
Apigenin Inhibits Enterovirus-71 Infection by Disrupting Viral RNA Association with Trans-Acting Factors - Wei Zhang, Haishi Qiao, Yuanzi Lv, Jingjing Wang, Xiaoqing Chen,Yayi Hou, Renxiang Tan, Erguang Li - PLoS One (16 Oct. 2014):
“Although flavonoids in general share similar structural features, apigenin and kaempferol were among tested compounds with significant activity against EV71 infection. hnRNP proteins function as trans-acting factors regulating EV71 translation. We found that apigenin treatment did not affect EV71-induced nucleocytoplasmic redistribution of hnRNP A1 and A2 proteins. Instead, it prevented EV71 RNA association with hnRNP A1 and A2 proteins. Accordingly, suppression of hnRNP A1 and A2 expression markedly reduced EV71 infection. [...] In addition to identification of apigenin as an antiviral agent against EV71 infection, this study also exemplifies the significance in antiviral agent discovery by targeting host factors essential for viral replication.”
Apigenin Restricts FMDV Infection and Inhibits Viral IRES Driven Translational Activity - Suhong Qian, Wenchun Fan, Ping Qian, Dong Zhang, Yurong Wei, Huanchun Chen, and Xiangmin Li & Curt Hagedorn [Academic Editor] - Viruses (31 Mar. 2015).
“In conclusion, apigenin inhibited FMDV infection by suppressing IRES-driven translational activity. Therefore, apigenin may be a potential small molecular drug to restrict FMDV infection. However, the further research should focus on the use of apigenin in vivo.”
Dietary Apigenin potentiates the Inhibitory Effect of Interferon-α on Cancer Cell Viability through Inhibition of 26S Proteasome-mediated Interferon Receptor Degradation - Sheng Li, Li-juan Yang, Ping Wang, Yu-jiao He, Jun-mei Huang, Han-wei Liu, Xiao-fei Shen & Fei Wang - Food & Nutrition Research (28 Jun. 2016).
Flavonoids: Promising Natural Compounds against Viral Infections - Hovakim Zakaryan, Erik Arabyan, Adrian Oo & Keivan Zandi - Archives of Virology (25 May 2017).
Inhibition of Epstein-Barr Virus Reactivation by the Flavonoid Apigenin - Chung-Chun Wu, Chih-Yeu Fang, Yu-Jhen Cheng, Hui-Yu Hsu, Sheng-Ping Chou, Sheng-Yen Huang, Ching-Hwa Tsai & Jen-Yang Chen - Journal of Biomedical Science (2017):
“Apigenin inhibited expression of the EBV lytic proteins, Zta, Rta, EAD and DNase in epithelial and B cells. It also reduced the number of EBV-reactivating cells detectable by immuno-fluorescence analysis. In addition, apigenin has been found to reduce dramatically the production of EBV virions. Luciferase reporter analysis was performed to determine the mechanism by which apigenin inhibits EBV reactivation: apigenin suppressed the activity of the immediate-early (IE) gene Zta and Rta promoters, suggesting it can block initiation of the EBV lytic cycle.”
The Therapeutic Potential of Apigenin - Bahare Salehi, Alessandro Venditti, Mehdi Sharifi-Rad, Dorota Kręgiel, Javad Sharifi-Rad, Alessandra Durazzo, Massimo Lucarini, Antonello Santini, Eliana B. Souto, Ettore Novellino, Hubert Antolak, Elena Azzini, William N. Setzer & Natália Martins - International Journal of Molecular Science (15 Mar. 2019).
Antiviral Efficacy of Flavonoids against Enterovirus 71 Infection in Vitro and in Newborn Mice - Wenwen Dai, Jinpeng Bi, Fang Li, Shuai Wang, Xinyu Huang, Xiangyu Meng, Bo Sun, Deli Wang, Wei Kong, Chunlai Jiang & Weiheng Su - Viruses (7 Jul. 2019).
A Review on Flavonoid Apigenin: Dietary Intake, ADME, Anti-Microbial Effects, and Interactions with Human Gut Microbiota - Minqian Wang, Jenni Firrman, LinShu Liu & Kit Yam - BioMed Research International (16 Oct 2019):
“Various levels of effectiveness have been reported on apigenin's antibacterial, antifungal, and antiparasitic capability. It has been shown that apigenin or its glycosides are degraded into smaller metabolites by certain gut bacteria which can regulate the human body after absorption. How apigenin contributes to the structural and functional changes in human gut microbiota as well as the bioactivities of apigenin bacterial metabolites are worth further investigation.”
Computational Screening of Known Broad-Spectrum Antiviral Small Organic Molecules for Potential Influenza HA Stem Inhibitors - Shilu Mathew, Asmaa A. Al Thani, Hadi M. Yassine - PLoS One (4 Sep. 2018).
Inhibition of SARS-CoV 3CL Protease by Flavonoids - Seri Jo, Suwon Kim, Dong Hae Shin & Mi-Sun Kim - Journal of Enzyme Inhibition and Medicinal Chemistry (14 Nov. 2019) [Even before SARS-CoV-2 there was research re: Flavonoid inhibition of the SARS-CoV 3CL protease]:
“There were severe panics caused by Severe Acute Respiratory Syndrome (SARS) and Middle-East Respiratory Syndrome-Coronavirus. Therefore, researches targeting these viruses have been required. Coronaviruses (CoVs) have been rising targets of some flavonoids. The antiviral activity of some flavonoids against CoVs is presumed directly caused by inhibiting 3C-like protease (3CLpro). Here, we applied a flavonoid library to systematically probe inhibitory compounds against SARS-CoV 3CLpro. Herbacetin, rhoifolin and pectolinarin were found to efficiently block the enzymatic acti- vity of SARS-CoV 3CLpro.” [Although not included in this study, Apigenin is another relevant candidate for testing in terms of SARS-CoV 3CL protease inhibition.]
Flavonoids as Antiviral Agents for Enterovirus A71 (EV-A71) - Salima Lalani & Chit Laa Poh - Viruses (2020).
Bibliographic Research Information provided courtesy of The Academy of the Third Millennium (A3M) 2020
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Learn how to protect you and your family from viruses more effectively by discovering the 52 'dietary antivirals' to include in your meals, snacks and drinks every day. Boost your immunity and fight diseases the natural way.
An 'Anti-Viral Diet' has been extensively corroborated by science and is gradually being accepted as an integral part of how people may protect themselves against viruses and treat viral illnesses - one other option to make use of alongside vaccines and antiviral medications. However, Food Science does not currently receive even 1% as much financing as pharmaceutical or vaccine-related research. 10% of the profit from sales of the 'AVD' book are being donated towards essential projects in Anti-Viral Dietary Research.
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Edouard d'Araille - Project Lead of Phase 1 of the 'AVD Research Project' - writes about an 'Anti-Viral Diet' that: "Regarding the effects of diet on disease, it is known that healthy, balanced nutrition has greater impact on immunity to viruses than any single vaccine. Science has proven this beyond a shadow of doubt."
'AVD' is a 3-Phase Research Project launched by The Academy of the Third Millennium (A3M). Phase 1 of this scientific inquiry is now complete and a summary of the findings are presented in the volume 'AVD: The Anti-Viral Diet' (2020-2022) available from this website. Information about the progress and purpose of Phases 2 & 3 of this A3M research program will be shared here and at A3M.International.
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