Hermetica Superfood Encyclopedia
The Short Answer
Hispidulin is a naturally occurring flavone found in plants such as Salvia and Artemisia species, functioning as a bioactive polyphenol with anti-inflammatory and potential anti-cancer activity. Its primary mechanisms involve suppression of JAK2/STAT3 signaling pathways and inhibition of Th2-driven cytokine release, including IL-4, IL-5, and IL-13.
CategoryNamed Bioactive Compounds
GroupCompound
Evidence LevelModerate
Primary Keywordhispidulin benefits
Synergy Pairings3
Hispidulin — botanical close-up
Health Benefits
Origin & History
Natural habitat
Hispidulin is a bioflavonoid (flavone subclass) found in various medicinal herbs, particularly Clerodendrum inerme and other plants traditionally used for inflammatory conditions. It is typically isolated from plant materials using standard flavonoid extraction techniques, though specific extraction methods are not detailed in available research.
“Hispidulin is found in herbs traditionally used in various medicine systems for treating inflammatory diseases, including asthma. The compound is notably isolated from Clerodendrum inerme, which has been historically used for conditions like intractable motor tics, though specific traditional systems and usage duration are not detailed.”Traditional Medicine
Scientific Research
No human clinical trials, randomized controlled trials, or meta-analyses have been conducted on hispidulin. All available evidence comes from preclinical in vitro cell culture studies and in vivo mouse models, including ovalbumin-induced asthma models and colorectal cancer xenografts.
Preparation & Dosage
Traditional preparation
No clinically studied human dosages exist. Animal studies used 10 mg/kg injected intraperitoneally in mice, while cell culture studies employed 1-100 μM concentrations. Human dosing cannot be extrapolated from these preclinical studies. Consult a healthcare provider before starting any new supplement.
Nutritional Profile
Hispidulin is a naturally occurring flavonoid (4',5,7-trihydroxy-6-methoxyflavone), classified as a polymethoxylated flavone with a molecular weight of 300.26 g/mol. It is not a macronutrient or conventional micronutrient — it contains no caloric value, protein, fat, or fiber. As a bioactive polyphenolic compound, it is found in several medicinal herbs including Salvia officinalis, Cirsium japonicum, and Saussurea involucrata, typically at trace concentrations (0.01–0.5% dry weight depending on plant source). Its primary bioactive mechanisms are mediated through flavone-receptor interactions rather than nutritional provision. Bioavailability is considered moderate-to-low due to its hydrophobic character and susceptibility to hepatic first-pass metabolism; lipid co-administration or nanoparticle encapsulation has been shown in preclinical studies to improve absorption. No established dietary reference intake exists. It exhibits antioxidant activity with an IC50 against DPPH radicals reported around 18–45 μM in vitro, comparable to other methoxylated flavones.
How It Works
Mechanism of Action
Hispidulin inhibits the JAK2/STAT3 and PIM1 signaling axes, reducing transcription of pro-survival and pro-proliferative genes implicated in tumor cell growth and metastasis. In allergic inflammation models, it suppresses Th2 cell differentiation by downregulating GATA-3 expression, thereby reducing secretion of interleukins IL-4, IL-5, and IL-13. Additionally, hispidulin activates intrinsic apoptotic cascades by modulating Bcl-2 family protein ratios, promoting caspase-dependent cell death in cancer cell lines.
Clinical Evidence
The current evidence base for hispidulin consists almost entirely of in vitro cell culture studies and rodent animal models, with no published human clinical trials as of early 2025. In mouse models of allergic airway inflammation, hispidulin reduced eosinophil infiltration and lowered bronchoalveolar IL-5 and IL-13 levels at doses ranging from 10–50 mg/kg. Anti-cancer activity has been demonstrated in cell lines for gastric, ovarian, and hepatocellular carcinoma, with IC50 values typically in the 20–80 µM range, concentrations difficult to achieve clinically through oral supplementation. Overall, evidence strength is preclinical and preliminary; extrapolation to human health outcomes requires significant caution.
Safety & Interactions
No human safety trials have been conducted for isolated hispidulin supplementation, making a formal adverse event profile unavailable. Because hispidulin inhibits CYP450 enzymes in vitro, there is a theoretical risk of interactions with drugs metabolized by CYP3A4 and CYP2C9, including warfarin, statins, and certain chemotherapeutics. Pregnant and breastfeeding individuals should avoid hispidulin supplements due to a complete absence of reproductive safety data. Individuals on immunosuppressants or undergoing cancer treatment should consult a physician before use, given its demonstrated immune-modulating and cytotoxic mechanisms.
Synergy Stack
Hermetica Formulation Heuristic
Also Known As
4',5,7-trihydroxy-6-methoxyflavone6-methoxy-5,7,4'-trihydroxyflavoneHispidulin flavone6-O-methylscutellareinClerodendrum flavoneHSPWild jasmine compound
Frequently Asked Questions
What is hispidulin and what plants does it come from?
Hispidulin is a naturally occurring O-methylated flavone with the chemical formula C16H12O6, found predominantly in medicinal plants including Salvia rosmarinus (rosemary), Artemisia species, and Saussurea involucrata. It belongs to the flavone subclass of polyphenols and is typically extracted from aerial plant parts including leaves and flowers. It is distinct from structurally similar flavones like apigenin by the presence of a methoxy group at the 4'-position.
Can hispidulin help with allergies or asthma?
In mouse models of allergic airway disease, hispidulin reduced hallmark allergy markers by suppressing Th2 cell differentiation via downregulation of the transcription factor GATA-3, leading to measurably lower levels of IL-4, IL-5, and IL-13 in lung tissue. Doses of 10–50 mg/kg administered intraperitoneally reduced eosinophil counts and airway hyperresponsiveness in these models. However, no human clinical data exists, so its efficacy for human allergies or asthma cannot be confirmed.
Does hispidulin have anti-cancer properties?
Hispidulin has demonstrated anti-cancer activity in cell line studies for gastric, ovarian, hepatocellular, and colorectal cancers, primarily by inhibiting the PIM1 kinase and JAK2/STAT3 signaling pathway, which controls tumor cell proliferation and survival. It also promotes apoptosis by shifting Bcl-2/Bax ratios toward pro-apoptotic Bax, activating caspase-3 and caspase-9. These findings are limited to in vitro and rodent models, and hispidulin should not be considered a cancer treatment in humans.
What is the recommended dosage for hispidulin supplements?
There is currently no established human dosage for hispidulin because no clinical trials have been conducted to determine safe or effective doses in people. Animal research has used doses in the range of 10–50 mg/kg body weight administered via injection, which does not translate directly to oral human supplementation. Any commercially available hispidulin supplements lack regulatory validation, and dosage instructions on such products are not supported by clinical evidence.
Does hispidulin interact with any medications?
In vitro studies indicate that hispidulin can inhibit cytochrome P450 enzymes, particularly CYP3A4 and CYP2C9, which are responsible for metabolizing a wide range of drugs including warfarin, certain statins, benzodiazepines, and some chemotherapy agents. Inhibition of these enzymes could theoretically raise plasma levels of co-administered drugs, increasing both efficacy and toxicity risk. No human pharmacokinetic interaction studies have been performed, but caution is warranted for anyone taking medications with a narrow therapeutic index.
What does the current research evidence say about hispidulin's effectiveness in humans?
Most hispidulin research to date has been conducted in cell cultures and animal models, with limited human clinical trials published. While findings on anti-inflammatory and anti-cancer pathways are promising, these results have not yet been consistently replicated in human studies, meaning efficacy claims remain largely preliminary. More rigorous human trials are needed to establish whether animal study findings translate to meaningful health benefits in people.
Are there natural food sources where I can obtain hispidulin?
Hispidulin is a flavone compound found naturally in certain plants, though dietary food sources are not abundant or well-characterized in common foods. Most hispidulin research focuses on isolated plant extracts or synthesized forms used in supplement studies rather than whole-food consumption. If you're interested in obtaining hispidulin through diet, consulting the specific plant sources it's derived from would be more practical than relying on standard food sources.
Who might benefit most from hispidulin supplementation based on current research?
Based on preliminary evidence, individuals interested in immune support—particularly those with allergic conditions or inflammatory responses—represent the primary theoretical target population, though human evidence is insufficient to make strong recommendations. People concerned with vascular health markers related to inflammation might also be interested, given hispidulin's observed effects on inflammatory pathways in animal studies. However, without robust clinical trials, it remains unclear which populations would experience measurable health benefits from supplementation.
Explore the Full Encyclopedia
7,400+ ingredients researched, verified, and formulated for optimal synergy.
Browse IngredientsThese statements have not been evaluated by the Food and Drug Administration. This content is for informational purposes only and is not intended to diagnose, treat, cure, or prevent any disease.
hermetica-encyclopedia-canary-zzqv9k4w hispidulin curated by Hermetica Superfoods at ingredients.hermeticasuperfoods.com and licensed CC BY-NC-SA 4.0 (non-commercial share-alike, attribution required)
