Tanshinone IIA (Danshen Diterpene Quinone · Cardiovascular · STAT3 Inhibitor · Anti-inflammatory)

Compound	Tanshinone IIA (Tan IIA)
Chemical class	Terpenoid — Diterpene Quinone (Abietane-type diterpenoid phenanthrenequinone)
CAS	568-72-9
Primary source	Salvia miltiorrhiza (Danshen / Red Sage, dried root)
Key applications	Cardiovascular (anti-thrombotic, cardioprotective); anti-inflammatory; STAT3 inhibitor; anticancer research
Claim strength	Moderate
Typical form	Danshen extract standardised to tanshinones 5–10%; tanshinone IIA isolate
Buy from Herbuno	Tanshinones 10% Powder (Danshen Extract) | Standardized Salvia miltiorrhiza → Tanshinones 5% Powder (Danshen Extract) | Standardized Salvia miltiorrhiza →

Name origin: Tanshinone — from Tan Shen (Chinese: 佌勒, red sage root, the TCM name for Salvia miltiorrhiza) + -one (ketone suffix). The Roman numeral II refers to its position in the original chromatographic isolation sequence; “A” distinguishes it from Tanshinone IIB (a minor isomer). Tanshinone IIA is an abietane-type diterpene quinone — its distinctive orange-red colour accounts for Danshen root’s deep red colouration. It is the most abundant and pharmacologically active of the lipophilic tanshinones in Danshen alongside cryptotanshinone and tanshinone I. Traditional use: Danshen (Salvia miltiorrhiza) is one of the most frequently prescribed herbs in Traditional Chinese Medicine — used for over 2,000 years primarily for cardiovascular conditions (heart disease, angina, stroke recovery), as a blood-activating and stasis-resolving herb. The TCM indication directly predicts tanshinone IIA’s modern cardiovascular pharmacology. Pharmacology: Multiple mechanisms: (1) anti-thrombotic via inhibition of TXA2 synthesis and PAF; (2) calcium channel blocking in cardiac and vascular smooth muscle (vasodilation); (3) antioxidant (quinone redox cycling scavenges ROS); (4) STAT3 inhibitor (anticancer); (5) anti-fibrotic in cardiac remodelling. Danshen is used clinically in China as a standard cardiovascular therapy — IV Danshen injection (sodium tanshinone IIA sulfonate, a water-soluble derivative) is a licensed cardiac drug in China for angina, MI, and stroke recovery. Commercial source: Danshen extract standardised to 5% and 10% tanshinones is available from Herbuno.

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Evidence for Tanshinone IIA Applications

Cardiovascular — Chinese clinical use: Sodium tanshinone IIA sulfonate (the water-soluble IV form) has been used in Chinese hospitals for decades for coronary artery disease and acute MI, with multiple Chinese RCTs showing benefit in cardiac function, infarct size reduction, and endothelial function. These are primarily single-centre Chinese trials with methodological limitations by Western standards; no large Western-standard RCT has been conducted. The preclinical cardiovascular pharmacology is extensive and mechanistically consistent. Claim strength: Moderate (Chinese clinical evidence; preclinical strong).

Anti-inflammatory and neuroprotective: Tanshinone IIA inhibits NF-κB and STAT3 signalling, reduces microglial activation in neuroinflammation models, and is neuroprotective in stroke and Alzheimer’s animal models. Claim strength: Moderate (animal; limited human).

Anticancer — STAT3 inhibition: Tanshinone IIA is one of the most studied natural STAT3 inhibitors — directly binding the SH2 domain of STAT3 and preventing dimerisation. STAT3 is constitutively active in many cancers (breast, prostate, leukaemia, gastric). Multiple cancer cell line and animal xenograft studies confirm antiproliferative activity. No clinical oncology trials have been completed. Claim strength: Emerging (preclinical; promising mechanism).

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Dosage & Formulator Specification

For cardiovascular and anti-inflammatory supplement applications: 200–500 mg/day Danshen extract standardised to 5–10% tanshinones (delivering 10–50 mg tanshinone IIA/day). Tanshinone IIA has poor water solubility (highly lipophilic; logP ~4.7) — specify oil-soluble Danshen extract or lipid-based delivery format. Note: Danshen is a potent CYP3A4 and P-gp inhibitor — significant drug interactions with warfarin (Danshen dramatically increases warfarin plasma levels, causing bleeding risk) and digoxin are well-documented. Include anticoagulant and cardiac medication interaction advisory in any Danshen formulation. Contraindicated with warfarin without medical supervision.

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Frequently Asked Questions — Tanshinone IIA

Why does Danshen interact so strongly with warfarin?
The interaction is multiplex: (1) tanshinones inhibit CYP2C9 (the primary warfarin-metabolising enzyme), increasing warfarin plasma levels; (2) danshensu and salvianolic acids (water-soluble Danshen constituents) inhibit CYP3A4 and CYP1A2, further reducing warfarin clearance; (3) Danshen has independent anticoagulant and antiplatelet effects (TXA2 inhibition), compounding warfarin’s anticoagulant action. The cumulative effect can double or triple INR, causing dangerous bleeding. This is one of the most clinically significant botanical-drug interactions documented — Danshen is contraindicated with warfarin without INR monitoring and dose adjustment.

Is sodium tanshinone IIA sulfonate the same as tanshinone IIA?
The sodium sulfonate is a synthetic water-soluble derivative of tanshinone IIA — it carries a sulfonate group added to improve aqueous solubility for IV administration. After IV injection, the sulfonate is partially cleaved to release tanshinone IIA. The oral supplement form uses lipophilic tanshinone IIA directly in oil-based extracts. The Chinese IV formulation has a different pharmacokinetic profile (immediate systemic delivery) compared to oral Danshen extract (first-pass metabolism, variable absorption). Clinical data from Chinese IV tanshinone IIA sulfonate does not directly apply to oral Danshen supplement predictions.

How does Danshen relate to other Salvia species?
Salvia miltiorrhiza (Danshen, red sage) should not be confused with Salvia officinalis (culinary sage) or Salvia rosmarinus (rosemary, also a Salvia). Danshen is specifically characterised by its tanshinone content — lipophilic diterpene quinones absent from culinary Salvia species. Common sage contains rosmarinic acid, carnosic acid, and ursolic acid — different active classes. The Salvia genus has undergone significant taxonomic revision; Rosmarinus has been merged into Salvia, making nomenclature in this genus particularly important for botanical specification.

Can tanshinone IIA be used for acne?
Topical tanshinone IIA has been investigated for acne — it demonstrates antimicrobial activity against Cutibacterium acnes (formerly Propionibacterium acnes), anti-sebum production effects (via 5α-reductase inhibition), and anti-inflammatory (IL-1β reduction) in sebaceous gland models. Several small clinical studies of topical Danshen/tanshinone formulations for acne have shown encouraging results. This is a legitimate emerging application for tanshinone IIA in cosmetic and dermo-cosmetic formulations.

Related compounds: Carnosic Acid, Curcumin, Boswellic Acid, Andrographolide

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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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