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Scutellaria baicalensis extract and baicalein inhibit replication of SARS-CoV-2 and its 3C-like protease in vitro

IThinkImTurningJapanese

Senior Member
Messages
3,492
Location
Japan
My wife tested positive for Covid this last month. She lives and works in a different city than I, so I encouraged her to come home so I could take care of her. I knew that I could help her minimize the illness with some of the things I use, Baicalin being one of them. I knew it was an antiviral.

In the process of trying to prove to her how much it would help I discovered this,
Scutellaria baicalensis extract and baicalein inhibit replication of SARS-CoV-2 and its 3C-like protease in vitro
COVID-19 has become a global pandemic and there is an urgent call for developing drugs against the virus (SARS-CoV-2). The 3C-like protease (3CLpro) of SARS-CoV-2 is a preferred target for broad spectrum anti-coronavirus drug discovery. We studied the anti-SARS-CoV-2 activity of S. baicalensis and its ingredients. We found that the ethanol extract of S. baicalensis and its major component, baicalein, inhibit SARS-CoV-2 3CLpro activity in vitro with IC50's of 8.52 µg/ml and 0.39 µM, respectively. Both of them inhibit the replication of SARS-CoV-2 in Vero cells with EC50's of 0.74 µg/ml and 2.9 µM, respectively. While baicalein is mainly active at the viral post-entry stage, the ethanol extract also inhibits viral entry. We further identified four baicalein analogues from other herbs that inhibit SARS-CoV-2 3CLpro activity at µM concentration. All the active compounds and the S. baicalensis extract also inhibit the SARS-CoV 3CLpro, demonstrating their potential as broad-spectrum anti-coronavirus drugs.


And this,
Inspiration for COVID-19 Treatment: Network Analysis and Experimental Validation of Baicalin for Cytokine Storm
Background: Cytokine storm (CS) is a systemic inflammatory syndrome and a major cause of multi-organ failure and even death in COVID-19 patients. With the increasing number of COVID-19 patients, there is an urgent need to develop effective therapeutic strategies for CS. Baicalin is an anti-inflammatory and antiviral traditional Chinese medicine. In the present study, we aimed to evaluate the therapeutic mechanism of baicalin against CS through network analysis and experimental validation, and to detect key targets of CS that may bind closely to baicalin through molecular docking.

Her fever approached 40C that day, but with Baicalin it was gone in 24 hours. I also dosed her with a gram of vitamin C every 2.5 to 3 hours. I've had Covid before, but apparently not this variant. I got sick as well. My fever broke in 12 hours, but I started the Baicalin much sooner and I'm taking other antivirals.

I'm very impressed with how powerful a tool this is in dealing with this devastating virus.
 

Hip

Senior Member
Messages
17,905
Lots of substances have been demonstrated to have antiviral effects against SARS-CoV-2 in vitro, but that does not mean these substances will necessarily work in vivo, when people actually take them.

With in vitro studies, researchers often use very high concentrations of the substance to demonstrate an antiviral effect in a cell line, but these high concentrations typically cannot be achieved in vivo.


In the case of this study, they found in vitro that the EC50 for baicalein was 2.9 µM. (The EC50 is the concentration of the substance which reduces viral replication by 50%).

Now in order to get a reasonable antiviral effect in vivo, you need to obtain blood or tissue concentrations of the substance that are at least say 5 times the EC50. So to get antiviral effects in the body, you want a blood concentration of at least 5 x 2.9 = 14.5 µM.


However, this pharmacokinetic study (see table 2) found that a single 2800 mg oral dose of pure baicalein in humans led to a peak blood level concentration (Cmax) of 108.17 ng/mL, which is equivalent to 0.4 μM.

That does not even account for the effects of plasma protein binding, which usually lowers the effective (free) blood concentration even further.

So you can see that the blood levels achieve are unfortunately below the EC50.

So in summary: the baicalein levels achieved in the blood are too low for baicalein to have any substantial antiviral effects in the blood.

I've looked at hundreds of in vitro antiviral studies for many different ME/CFS viruses, and unfortunately in nearly all cases, it turns out that the substance is not effective in vivo.



However, this article says skullcap reduces fever, so that might explain why you observed the fever disappearing. Although whether it is beneficial to reduce fever I am not sure, since the body instigates fever as a means of fighting infection.
 
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Violeta

Senior Member
Messages
2,996
My wife tested positive for Covid this last month. She lives and works in a different city than I, so I encouraged her to come home so I could take care of her. I knew that I could help her minimize the illness with some of the things I use, Baicalin being one of them. I knew it was an antiviral.

In the process of trying to prove to her how much it would help I discovered this,
Scutellaria baicalensis extract and baicalein inhibit replication of SARS-CoV-2 and its 3C-like protease in vitro


And this,
Inspiration for COVID-19 Treatment: Network Analysis and Experimental Validation of Baicalin for Cytokine Storm


Her fever approached 40C that day, but with Baicalin it was gone in 24 hours. I also dosed her with a gram of vitamin C every 2.5 to 3 hours. I've had Covid before, but apparently not this variant. I got sick as well. My fever broke in 12 hours, but I started the Baicalin much sooner and I'm taking other antivirals.

I'm very impressed with how powerful a tool this is in dealing with this devastating virus.

I'm going to have to get some and keep it on hand.

In 2020, when news of COVID first broke, I read about andrographis having been used for Sars-CoV-1, and stocked up on that. It really came in handy.

@IThinkImTurningJapanese, did you use tincture, capsules, or tablets?
 

hapl808

Senior Member
Messages
2,137
So in summary: the baicalein levels achieved in the blood are too low for baicalein to have any substantial antiviral effects in the blood.

I've looked at hundreds of in vitro antiviral studies for many different ME/CFS viruses, and unfortunately in nearly all cases, it turns out that the substance is not effective in vivo.

I think one of the issues is that skullcap like many TCM herbs is not made to be used as a monotherapy despite Western medicine's attempt to make it one. And while the antiviral effect alone may not account for its action, skullcap seems to have many effects on immune function, cytokine release, etc.

It's beyond me to figure out exactly what it's doing, but I often take it as part of a number of herbs as I think there's some research that it can also increase absorption of other things.
 

Hip

Senior Member
Messages
17,905
It's worth mentioning that @msf found Chinese skullcap root is a good PEM shielder, at a high dose of 3 to 6 grams, taken two to three times daily.

One in vivo study in chickens observed that baicalin restored the infection-triggered decrease in mitochondrial complex V (also called ATP synthase, or ATPase).

Mitochondrial complex V has been found deficient in ME/CFS. So this perhaps might explain the anti-PEM effect of Chinese skullcap root noted by @msf.


More info in the PEM busters thread.