Hermetica Superfood Encyclopedia
The Short Answer
Shikonin is a naphthoquinone compound extracted from Lithospermum erythrorhizon root that demonstrates anti-cancer properties through ROS-mediated apoptosis. This bioactive compound also exhibits anti-inflammatory effects by inhibiting key inflammatory markers like TNF-α and IL-1β.
CategoryNamed Bioactive Compounds
GroupCompound
Evidence LevelModerate
Primary Keywordshikonin benefits
Synergy Pairings3
Shikonin (Naphthoquinone) — botanical close-up
Health Benefits
Origin & History
Natural habitat
Shikonin is a natural naphthoquinone compound primarily extracted from the roots of Lithospermum erythrorhizon (purple gromwell), a traditional medicinal herb. It is typically obtained through solvent-based extraction methods from the plant roots, yielding a characteristic red pigment with bioactive properties.
“Shikonin-rich extracts from Lithospermum erythrorhizon roots have been used in Traditional Chinese Medicine for centuries to promote wound healing and treat inflammation. Historical applications include topical use for burns and sores, with traditional antitumor activity noted in modern reviews.”Traditional Medicine
Scientific Research
No human clinical trials, RCTs, or meta-analyses have been conducted with shikonin. Evidence is limited to preclinical studies including in vitro cancer cell lines (PMC10135058, PMC8605926) and a single rat osteoarthritis model (PMC5038895) using 10 mg/kg/day intraperitoneally.
Preparation & Dosage
Traditional preparation
No human dosage data available. Animal studies used 10 mg/kg/day intraperitoneally in rats for 4 days. Consult a healthcare provider before starting any new supplement.
Nutritional Profile
Shikonin is a pure bioactive naphthoquinone compound, not a food ingredient, and therefore has no conventional nutritional profile in terms of macronutrients, vitamins, minerals, or fiber. It is a naturally occurring red pigment and secondary metabolite isolated primarily from the roots of Lithospermum erythrorhizon (purple gromwell) and related Boraginaceae family plants. Key compositional data: Shikonin is a hydroxynaphthoquinone with molecular formula C16H16O5 and molecular weight 288.3 g/mol; it exists as the levorotatory enantiomer (the dextrorotatory form is alkannin). Typical extraction yields from dried Lithospermum root range from 0.5–2.0% by dry weight. Bioactive compound concentration in standardized extracts is generally reported at ≥98% purity in research-grade isolates. It contains no protein, carbohydrates, dietary fiber, or conventional micronutrients. Bioavailability notes: Shikonin demonstrates poor aqueous solubility (lipophilic compound, logP approximately 3.0–3.5), which significantly limits oral bioavailability; nanoparticle formulations and lipid-based delivery systems have been studied to enhance absorption. Plasma half-life in animal models is reported as relatively short (approximately 1–3 hours), necessitating optimized delivery. It is metabolized hepatically and shows high protein binding in plasma. No established dietary reference intake or safe supplemental dose exists for humans.
How It Works
Mechanism of Action
Shikonin induces cancer cell death by generating reactive oxygen species (ROS) that trigger mitochondrial-mediated apoptosis pathways. The compound suppresses inflammatory responses by inhibiting nuclear factor-kappa B (NF-κB) signaling and reducing production of pro-inflammatory cytokines including TNF-α, IL-1β, and cyclooxygenase-2 (COX-2). Shikonin also demonstrates antimicrobial activity by disrupting bacterial cell membrane integrity.
Clinical Evidence
Evidence for shikonin comes primarily from in vitro cell culture studies and animal models, with no human clinical trials currently available. One rat study (n=10) showed reduced osteoarthritis inflammation markers, but this represents extremely limited evidence. Multiple laboratory studies demonstrate anti-cancer effects against leukemia and solid tumor cell lines, but translation to human efficacy remains unproven. The current evidence base is insufficient to establish clinical effectiveness or appropriate dosing protocols.
Safety & Interactions
Safety data for shikonin in humans is extremely limited due to lack of clinical studies. Traditional use suggests potential skin irritation when applied topically, as shikonin is naturally found in plants used for wound healing. No documented drug interactions exist, but theoretical concerns include potential interactions with chemotherapy drugs due to its anti-cancer mechanisms. Pregnancy and breastfeeding safety is unknown, and use should be avoided during these periods.
Synergy Stack
Hermetica Formulation Heuristic
Also Known As
(R)-5,8-dihydroxy-2-(1-hydroxy-4-methyl-3-pentenyl)-1,4-naphthoquinonePurple gromwell extractZicaoLithospermum root extractMurasaki root compoundAlkannin analogRed naphthoquinone
Frequently Asked Questions
What is shikonin extracted from?
Shikonin is extracted from the roots of Lithospermum erythrorhizon, also known as purple gromwell or zicao. This traditional Chinese medicinal plant has been used for centuries, with the red-purple compound shikonin being the primary bioactive naphthoquinone responsible for its therapeutic effects.
How does shikonin kill cancer cells?
Shikonin induces cancer cell death through ROS-dependent apoptosis, generating reactive oxygen species that damage mitochondria and trigger programmed cell death pathways. Studies show effectiveness against leukemia cells and various solid tumors in laboratory settings, though human clinical evidence is lacking.
What inflammatory markers does shikonin reduce?
Shikonin reduces key inflammatory markers including TNF-α, IL-1β, and COX-2 by inhibiting NF-κB signaling pathways. One rat study showed decreased osteoarthritis inflammation, but this represents very preliminary evidence with only 10 animals tested.
Is shikonin safe for human consumption?
Human safety data for shikonin is extremely limited due to absence of clinical trials. While traditional topical use suggests relative safety, internal consumption safety, appropriate dosages, and potential side effects remain unknown and require further research.
What's the difference between shikonin and other naphthoquinones?
Shikonin is specifically an alkylated naphthoquinone with a unique hydroxyl group configuration that distinguishes it from synthetic naphthoquinones. This natural structure provides both antimicrobial and anti-inflammatory properties that differ from other naphthoquinones like vitamin K or synthetic quinones used in chemotherapy.
What is the current strength of clinical evidence for shikonin in humans?
Current evidence for shikonin in humans is extremely limited, with most data coming from in vitro cell studies and animal models rather than clinical trials. While preliminary research suggests potential benefits in cancer cell death and inflammation reduction, these findings have not been validated in human subjects, making it impossible to confirm efficacy or optimal dosing at this time. Any health claims about shikonin should be viewed as preliminary and not yet established as effective for human use.
Who should avoid taking shikonin supplements?
Pregnant and breastfeeding women should avoid shikonin due to insufficient safety data in these populations. Individuals with active cancer undergoing conventional treatment should consult their oncologist before use, as shikonin's mechanisms may interact unpredictably with chemotherapy or radiation. Those with bleeding disorders or taking anticoagulant medications should exercise caution, as some naphthoquinones may affect clotting pathways.
How does shikonin's bioavailability compare to other supplement forms, and what affects its absorption?
Shikonin has poor oral bioavailability due to its lipophilic nature and limited solubility, meaning most ingested amounts may not reach systemic circulation efficiently. Fat-soluble carriers or specialized delivery systems may theoretically improve absorption, but no human pharmacokinetic studies have established optimal formulation strategies. Most commercial shikonin supplements lack standardized bioavailability data, making it unclear which forms provide meaningful blood levels.
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