Baicalein (Scutellaria Aglycone Flavone · Antiviral · Neuroprotective)
| CAS No. | 491-67-8 |
| Class | Polyphenol · Flavone · Flavonoid |
| Source | Scutellaria baicalensis roots — released from baicalin by gut microbiota hydrolysis. Commercial isolate from direct extraction or baicalin hydrolysis |
| Claim strength | Moderate |
| Buy from Herbuno | Baicalein 98% Powder (Chinese Skullcap) | High-Purity Isolate | Scutellaria baicalensis → |
Relationship to baicalin: Baicalein is the trihydroxy aglycone — the bioavailable form released when gut microbiota cleave baicalin's glucuronide sugar. While baicalin is the most abundant constituent in the intact root extract, baicalein is the form that enters systemic circulation and crosses the blood-brain barrier. Higher membrane permeability: The absence of the charged glucuronide moiety significantly improves baicalein's membrane penetration, giving it higher and more predictable peak plasma concentrations than baicalin at equivalent oral doses. Research spotlight: Baicalein received significant attention during SARS-CoV-2 research as a candidate inhibitor of the viral 3CL protease — a primary drug target for COVID-19 antivirals — and independently in Parkinson's disease research for its ability to inhibit α-synuclein aggregation. CYP interaction note: Baicalein inhibits CYP1A2 and CYP2C9 at high doses — an important consideration for drug interaction labelling.
Evidence for Antiviral Activity, Neuroprotection & 12-LOX Inhibition
Antiviral — direct enzyme inhibition: Documented inhibitor of influenza A/B neuraminidase, HIV-1 reverse transcriptase and integrase, and in vitro SARS-CoV-2 3CL protease (main protease). Claim strength: Moderate (influenza); Emerging (SARS-CoV-2).
Neuroprotection — Parkinson's research: Inhibits α-synuclein aggregation and fibrillation — the pathological protein deposits central to Parkinson's disease. Protects dopaminergic neurons from oxidative stress in preclinical models. Claim strength: Emerging.
12-LOX selective inhibition: Baicalein inhibits 12-lipoxygenase with particular selectivity — more targeted than many anti-inflammatory flavones. 12-LOX converts arachidonic acid to 12-HETE, promoting platelet aggregation and inflammatory skin conditions. This selectivity distinguishes baicalein from most other anti-inflammatory flavones that primarily target COX and 5-LOX pathways. Claim strength: Moderate.
Anxiolytic: Modulates GABA-A receptors and 5-HT1A with more direct and faster CNS access than baicalin due to better membrane permeability. Claim strength: Moderate.
Baicalein 98% Powder (Chinese Skullcap) | High-Purity Isolate | Scutellaria baicalensis →
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Dosage, CYP Interactions & Formulator Specification
Dose range: No established human clinical dose. Emerging supplement range: 50–200 mg/day based on pharmacokinetic modelling from baicalin trials. At 98% purity, a 100 mg capsule delivers 98 mg of baicalein.
CYP interaction — mandatory label consideration: Baicalein inhibits CYP1A2 and CYP2C9 at high supplement doses. May reduce clearance of co-administered drugs metabolised by these enzymes — including warfarin (CYP2C9), theophylline (CYP1A2), and several antiepileptics. Standard precautionary label copy: consult a healthcare professional before use alongside prescription medications, particularly anticoagulants and bronchodilators.
Specification decision: For formulations targeting systemic antiviral, neuroprotective, or anxiolytic effects, baicalein 98% is preferred for consistent plasma concentrations. For traditional Scutellaria botanical profile formulations, standardised extract at 85% baicalin is conventional. Premium formulations frequently include both.
Synergistic pairs: Baicalin (complementary pharmacokinetics), wogonin (complete Scutellaria flavone profile), quercetin (anti-inflammatory synergy), andrographolide (comprehensive antiviral stack).
Frequently Asked Questions — Baicalein
Should I formulate with baicalin or baicalein?
Baicalin (glycoside from standardised extract) provides slower/sustained delivery via microbiota hydrolysis and is more cost-effective. Baicalein (aglycone) achieves higher and more predictable plasma concentrations faster and crosses the blood-brain barrier more efficiently. For antiviral and neuroprotective applications, baicalein is mechanistically preferred. Many premium Scutellaria formulations include both for complementary pharmacokinetic profiles.
Is baicalein relevant for respiratory immune support formulations?
Yes — baicalein's documented influenza neuraminidase inhibition and preliminary SARS-CoV-2 3CL protease inhibition data make it relevant for antiviral respiratory immune support. Position in supplements for supporting healthy respiratory immune function rather than treatment claims.
What does baicalein's 12-LOX selectivity mean for formulators?
12-LOX produces 12-HETE, which promotes platelet aggregation and inflammatory skin conditions including psoriasis and atopic dermatitis. Baicalein's selective 12-LOX inhibition makes it potentially relevant for platelet health and dermatological formulations — distinct positioning from most other anti-inflammatory flavones targeting COX and 5-LOX.
What are the key drug interactions to flag on labels?
Baicalein inhibits CYP1A2 and CYP2C9. This is clinically significant for warfarin (CYP2C9 substrate), theophylline and caffeine (CYP1A2 substrates), and certain antiepileptics. Standard supplement label precaution: consult a healthcare professional before use alongside prescription medications. This is not a prohibition on product development — it is required precautionary label copy.
Claim-strength scale – High = multiple human RCTs; Moderate = limited trials or strong preclinical convergence; Emerging = early-stage lab or animal data.
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