• No Need to Wait for Big Pharma’s Anti-Covid Protease-Inhibiting Drug

    Posted September 14, 2021: by Bill Sardi

    Just to steer clear of online censors and trolling bots that detect “misinformation,” and to avoid potential litigation, let’s just report a major manufacturer of vaccines and drugs now announces it will introduce an oral medicine that impedes the replication of COVID-19 coronavirus via enzyme inhibition.  The new drug will augment but not replace vaccines. Online links to the new drug won’t be provided here because the pharmaceutical company doesn’t need any free publicity.  You will realize why after reading the rest of this report.

    The enzyme is protease.  Proteases are enzymes that help to synthesize proteins in the body.  In regard to COVID-19, protease facilitates the replication of viruses.  Inhibit protease, diminish the threat of severe COVID coronavirus infection.

    The drug is specifically intended for non-hospitalized, symptomatic adults who have a confirmed COVID-19 infection and are not believed to be at increased risk for progression to severe illness.  A controlled study is underway.

    Should the public hold their breath for this medicine?  Does this drug supplant vaccination?

    How protease inhibitors work

    Protease inhibitors have a long history of use with a good safety profile.  Protease cuts chains of proteins to produce subunits that allow the virus to replicate. Protease inhibitors interfere with this protein-cutting process.  Protease inhibitors have made history in the battle against HIV.  Furthermore, protease inhibitors work with all variants of a virus.

    Drug targets: obfuscation

    The drug is said to target the main protease enzyme, – Mpro, of COVID-19.  Mpro is intentionally vague and stands for “main protease.”

    Mpro is just a way of hiding the real protease enzyme (3C-like protease, formerly C30 endopeptidase) that facilitates the replication of viruses inside living cells.  Recall from Virology 101 that viruses can’t replicate until they enter the genetic machinery of a living cell.

    Just to confuse everyone, so they won’t put two-and-two together and figure out this drug can be duplicated with vitamin and herbal remedies, alternative names are used for Mpro, such as 3CLpro, 3C-like protease, coronavirus 3C-like protease, Mpro, SARS 3C-like protease, SARS coronavirus 3CL protease, SARS coronavirus main peptidase, SARS coronavirus main protease, (this is the “guess the name of the enzyme” game), SARS-CoV 3CLpro enzyme, SARS-CoV main protease, SARS-CoV Mpro, and severe acute respiratory syndrome coronavirus main protease.

    Papain-like enzyme, (PLpro), is another protein that is crucial in the viral replication process.  PLpro is said to be the Achilles’ heel of COVID-19.

    An alternative pathway for viral entry into cells is TMPRSS2 (trans-membrane protease serine 2) that primes the spike protein on the surface of coronaviruses, thus facilitating the entry of the virus into cells.  A drug trial failed to demonstrate inhibition of this TMPRSS2 pathway.  However, fisetin, a strawberry molecule, was found to inhibit TMPRSS2.

    Natural molecules abound

    A report in Nature magazine notes that pharmacologists assayed over 10,000 compounds, including natural and synthetic drug molecules, and found six that significantly inhibited replication of COVID-19.

    Ebselen, a sulfur-based drug that mimics a natural antioxidant (glutathione peroxidase) prevailed in their screening of molecules to counter Mpro.

    Vitamin E + the trace mineral selenium produces glutathione peroxidase, an internal antioxidant enzyme.

    Ebselen (vitamin E + selenium) inhibits PLpro like it does Mpro.  Ebselen is an extremely safe drug.  Most people who take multivitamins get enough vitamin E and selenium to make glutathione peroxidase.

    Fisetin: the strawberry molecule that clobbers COVID

    A remarkable study conducted by University of Minnesota researchers showed the strawberry molecule fisetin as a protease inhibitor not only was effective against coronavirus-related mortality in lab animals, but it helped to abolish old senescent cells that render older adults vulnerable to viruses.

    In one of their studies, 100% of old mice died within a 2-week period vs. only 36% of fisetin-treated male mice.  Targeting drivers of aging resulted in longer survival of lab animals.

    According to these university-based researchers, writing in Science magazine, even if 95% effectiveness vaccine rate in health populations in borne out in elderly nursing home patients, still at least 1 out of 20 vaccinated elderly people can anticipate becoming ill due to COVID-19 and will need anti-senescent/ anti-COVID medication.  Fisetin may be very valuable for older age adults.  Fisetin is sold as a dietary supplement in health shops and online.

    But there are a couple of things the public ought to know about protease inhibitors that are not being said.

    Non-Rx protease inhibitors

    First, there are many natural non-prescription protease inhibitors, and they are available as dietary supplements without all the cost or impediment of obtaining a doctor’s prescription.

    A class of natural molecules known as polyphenols, found in grapes, berries, tea leaves, cinnamon, are enzyme inhibitors, and they target coronaviruses.

    A number of polyphenols are sold in health shops, such as quercetin (apple peel), resveratrol (grapes and wine), catechin EGCG (from green tea), fisetin (from strawberries).  One would need to eat 37 strawberries to get 50 milligrams of fisetin, so it is more practical to take a concentrated extract.

    Quercetin has been singled out as a candidate molecule that inhibits COVID-19 coronavirus.  In one study influenza-infected mice were given quercetin and animal mortality dropped from 74% to 52% in placebo vs. quercetin-supplemented animals.  Animal studies are criticized because they are not human studies, but it would be unethical to conduct a trial where infected humans would be given an inactive placebo.

    Research studies show polyphenols are metal (iron, copper, etc.) chelators (binders) that inhibit the growth of viruses.  A list of natural iron chelators includes IP6 (inositol hexa-phosphate) derived from rice bran that is a master iron/copper chelator.

    One group of researchers say: “it is surprising that polyphenols have not been tested to combat viral activities,” given their anti-infective properties.

    Potential side effects with high doses

    The second thing consumers should know is that protease inhibitors DO have side effects.  Protease enzyme is needed for wound healing.  Protease inhibitors delay wound healing, which can result in injury to the kidneys.

    Natural non-drug protease inhibitors work more mildly, without side effect, and may be superior to synthetic molecules from a safety standpoint.  With polyphenolic protease inhibitors, modest doses (100-350 milligrams) produce an optimal effect.  More is not better.

    Excessive dosing cannot only impair wound healing, but snuff out the flame of Tumor Necrosis Factor (TNF) which is a necessary part of the immune system.    Over-inhibition of TNF can result in skin rash, anxiety reactions and flu-like symptoms, the latter possibly making it appear the patient has COVID-19!

    Dietary polyphenol intake

    Of interest, in the U.S., mean dietary intake of polyphenols ranges from 250 to 400 milligrams per day.  That compares to Europeans, 167 to 564 milligrams per day, and Japanese 1492 milligrams/day (range 183-4854 milligrams/day).

    Coffee, tea and wine comprise most of the polyphenols consumed around the world, which are concentrated as hot water extracts in tea, or alcohol-extracted polyphenols in wine.  Which is why eating tea leaves or grape juice is not as powerful as an extraction accomplished by heat or alcohol to produce tea and wine. Grape juice is a beverage, wine, consumed in moderation, is medicine.

    Polyphenol pills (wine without the alcohol) may be even better medicinally speaking, but a small amount of alcohol induces relaxation and sociality that can’t be duplicated by any antidepressant drug.

    Dietary and supplemental polyphenol intake, or use of multivitamins (vitamin E + selenium) may explain why some populations are less prone to viral infections or only experience modest symptoms.

    The big news is that the public need not wait for a prescription protease inhibitor.

    Modern medicine drives up the price

    It appears a Big Pharma company’s drug is going to be reimbursed by insurance plans when it could be duplicated with vitamin E + selenium (to produce the antioxidant enzyme glutathione peroxidase), or some polyphenols.  Absurd.

    One can see doctors prescribing this protease-inhibiting drug “off-label,” being used outside of its license, as a preventive instead of treatment, when the local health shop has something less problematic and more economical.

    Of course, doctors and drug companies will say molecules like fisetin, quercetin and resveratrol are unproven, while their patented prescription drug is FDA approved.  Doctors can’t bill insurance for a drug consult if they prescribe fisetin.

    If a molecule like fisetin does undergo a human clinical trial and is successfully shown to quell coronavirus infections, it will be categorically declared a drug and sold at a much higher price.  And so goes the racket we call modern medicine.

    FDA seeks nutraceuticals to be drugs

    The FDA is, once again, after nutraceutical companies to perform needless toxicity studies on their molecules.   That would drive up their price, when dietary supplements are safer than tap water, table salt, aspirin, statin drugs and penicillin.

    The National Health Federation (www.thenhf.com) has a petition demanding the FDA keep its hands off dietary supplements.  The FDA is a front for the drug companies and doesn’t want any competition from nutraceuticals.

    Ironically, properly-used FDA approved drugs are a leading cause of death (2.74 million hospitalizations; 4th leading cause of death;128,000 needless deaths), while the Poison Control Centers of America indicates 48,630 reports to their centers about problems with dietary supplements (most are toddlers getting into mom’s vitamin pills, or intentional or mistaken misuse such as iron pills, with no deaths in 2018!), and don’t report any deaths from dietary supplements years on end.  The conundrum the FDA-approved imprimatur = unsafe; while non-FDA approved = safe.

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