BREAKING! The Phytochemical Xanthohumol Extracted From Hops Flowers Is A Potent Broad Spectrum Antiviral Against Most Coronaviruses Including SARS-CoV-2!
: A new study by researchers from Lanzhou University-China, the Pilot National Laboratory for Marine Science and Technology-China, Washington University-USA, the Ocean University of China, Fudan University-China and the Marine Biomedical Research Institute of Qingdao-China has discovered that the phytochemical Xanthohumol extracted from the hops flower is a potent broad spectrum antiviral against most coronaviruses including the SARS-CoV-2 coronavirus!
Typically, most coronaviruses cause diseases in humans and livestock. At present, the SARS-CoV-2 coronavirus is infecting millions of human beings, with high morbidity and mortality worldwide.
The main protease (Mpro) of coronavirus plays a pivotal role in viral replication and transcription, which, in theory, is an attractive drug target for antiviral drug development. It has been extensively discussed whether Xanthohumol is able to help COVID-19 patients.
The study findings show that Xanthohumol, a small molecule in clinical trials from hops (Humulus lupulus), was a potent pan-inhibitor for various coronaviruses by targeting Mpro including the betacoronavirus SARS-CoV-2 (IC50 value of 1.53 μM), and alphacoronavirus PEDV (IC50 value of 7.51 μM).
The phytochemical Xanthohumol inhibited Mpro activities in the enzymatical assays, while pretreatment with Xanthohumol restricted the SARS-CoV-2 and PEDV replication in Vero-E6 cells.
Hence the study findings show proof that Xanthohumol is a potent pan-inhibitor of coronaviruses and an excellent lead compound for further drug development.
The study findings were published in the peer reviewed Internal Journal of Molecular Sciences. https://www.mdpi.com/1422-0067/22/22/12134
The SARS-CoV-2 is a novel coronavirus infecting humans and even domestic and wild animals worldwide.
Not all coronavirus infections cause major symptoms but some like SARS-CoV-2, SARS-CoV, and MERS-CoV can cause serious disease.
As of today, the COVID-19 pandemic has caused more than 253 million infections and 5.08 million deaths worldwide. Coronavirus infections in livestock are zoonotic in origin and could lead to more outbreaks in the future.
Hence it is very critical to screen for effective pan-inhibitors for emerging coronaviruses like SARS-CoV-2.
Initially it was believed that the RNA-dependent RNA polymerase inhibitor, Remdesivir may be an effective treatment option for patients infected with SARS-CoV-2. However, clinical trials of Remdesivir were not very successful and prompted more screening for ideal antiviral agents, specifically pan-inhibitors of coronaviruses.
The big Western pharma entities in collaboration with certain corrupted Western dictators are planning to introduce a couple of toxic antiviral drugs soon that can also generate more drug resistant and worrisome mutations and variants.
Herbs and phytochemicals are the best sources for potential antivirals for coronaviruses not only due to their long-standing safety profiles but also due to their ‘holistic’ approaches. There are already tons of supporting published scientific studies supporting
the use of some of these herbs as prospective candidates to treat COVID-19 and inhibit other coronavirus not only focusing on their antiviral properties but also their anti-inflammatory, immunomodulatory and other properties.
The SARS-CoV-2 belongs to the Coronaviridae family with a unique life cycle and is a positive RNA virus. Immediately after entry into host cells, coronaviruses translate two polyproteins into nonstructural proteins with the help of protease (Mpro
or 3CLpro) and papain-like protease (PLpro). Given the crucial role of the main protease (Mpro
) in the replication and transcription of the virus, targeting Mpro
chemically may help in inhibiting multiple coronaviruses.
The COVID-19 Herbs
study team from China reported the results of their study aimed at finding an effective Mpro inhibitor since Mpro is the best drug target to fight SARS-CoV-2 infection.
It has been known that any natural products obtained from plants and animals have antiviral and antioxidant properties. The study team screened natural products for Mpro
Interestingly the team found that Xanthohumol, a compound extracted from hops plant (Humulus lupulus
) that contributes to bitterness in beer, is a potent inhibitor of Mpro
Various past studies have reported the antiviral, antioxidant, and anti-cancer properties of Xanthohumol.
Also, in-vitro study of Xanthohumol demonstrated that it could suppress Mpro
hydrolase activity at low concentrations.
Although cell-based assays showed that Xanthohumol can decrease cell viability at high concentrations, it could not reduce cell growth.
Plague assays revealed that Mpro
plays an important role in viral RNA replication as it cleaves the viral polyproteins for assembly of the replication machinery.
Hence this encouraged the study team to use Xanthohumol as a Mpro
inhibitor of SARS-CoV-2 and evaluate its efficacy.
The study findings showed that Xanthohumol is a potent Mpro
inhibitor for SARS-CoV-2 and can eliminate the viral genome. These findings were consistent with and supported the results of the plague assay. Overall, Xanthohumol was found to be effective against SARS-CoV-2.
A further study was by the same team to evaluate the efficiency of Xanthohumol against the porcine epidemic diarrhea virus (PEDV) by using PEDV Mpro
in place of SARS-CoV-2 Mpro
Interestingly similar results were obtained for PEDV as well. From the results of the cell-based assay, the study team concluded that Xanthohumol is a potent inhibitor of coronavirus and PEDV Mpro
The study team says that Xanthohumol
should be further developed to effectively treat patients infected by alpha and beta mutants of SARS-CoV-2.
Though the study findings show that Xanthohumol is effective against coronaviruses at lower concentrations, more detailed systematic studies on the use of Xanthohumol are necessary before it can be used for medicinal purposes.
The study team is still trying to understand the underlying mechanism of viral inhibition by Xanthohumol or its role in coronavirus disease 2019 (COVID-19) treatment.
The study team also suggests that the protease inhibiting property of Xanthohumol can also be used in treating other diseases like HIV, HCV, and porcine reproductive and respiratory syndrome virus (PRRSV) through a similar inhibitor mechanism. Increasing numbers of SARS-CoV-2 infections worldwide have facilitated mutation of SARS-CoV-2 and the emergence of many viral variants.
Worryingly, due to their zoonotic origin, coronaviruses may cause more outbreaks in the future, and thus it is necessary to keep screening for potent inhibitors of these viruses.
Future trials focusing on coronavirus infections could provide more information on whether the findings of this study are useful for the development of pan-inhibitors against different coronaviruses.
The study findings conclude that Xanthohumol is a potent inhibitor of Mpro
SARS-CoV-2 as shown in their in vitro and cell-based assays and suggest that it should be further developed clinically.
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