Hermetica Superfood Encyclopedia
The Short Answer
Astragalin is a kaempferol-3-O-glucoside flavonoid glycoside found in persimmon leaves, rose hips, and Astragalus species that exerts anti-inflammatory effects primarily by suppressing NF-κB signaling and inhibiting cyclooxygenase-mediated prostaglandin synthesis. Research spanning in vitro and animal models suggests it also modulates apoptotic pathways in cancer cells, though human clinical trials remain limited.
CategoryNamed Bioactive Compounds
GroupCompound
Evidence LevelModerate
Primary Keywordastragalin benefits
Synergy Pairings5
Astragalin — botanical close-up
Health Benefits
Origin & History
Natural habitat
Astragalin is a naturally occurring flavonoid (kaempferol 3-O-β-D-glucopyranoside) first isolated from Astragalus sinicus, appearing as a yellow compound. It occurs in various edible plants including green tea seeds, mulberry fruits and leaves, persimmon leaves, and Astragalus membranaceus roots. Extraction methods include methanolic extraction from fern fronds, enzymatic hydrolysis of tea seed extract (yielding >96% purity), and chromatographic separation techniques.
“Astragalin is a bioactive constituent in traditional medicinal plants used in Chinese medicine, including Cuscuta chinensis, Astragalus membranaceus, and Morus alba. While these plants have long traditional use for immune support, isolation and bioactivity studies of astragalin itself are modern developments (post-2010).”Traditional Medicine
Scientific Research
No human clinical trials, RCTs, or meta-analyses for astragalin were identified; all evidence is limited to preclinical studies. Key animal research includes BALB/c nude mice studies showing tumor growth inhibition at 25-75 mg/kg oral doses through upregulation of pro-apoptotic factors and downregulation of anti-apoptotic proteins (Yang et al., 2021, PMID not provided). In vitro studies demonstrated anti-inflammatory effects in RAW 264.7 macrophages (PMID: 21567414).
Preparation & Dosage
Traditional preparation
No clinically studied human dosages available. Preclinical mouse studies used 25-75 mg/kg oral doses (theoretical human equivalent ~2-6 mg/kg, not tested). In vitro anti-inflammatory effects observed at 134-363 µg/mL using >96% pure astragalin prepared via enzymatic hydrolysis. Consult a healthcare provider before starting any new supplement.
Nutritional Profile
Astragalin (kaempferol-3-O-glucoside) is a flavonoid glycoside compound with molecular formula C21H20O11 and molecular weight of 448.38 g/mol. It is not a food ingredient with macronutrient or micronutrient composition in the traditional sense, but rather a discrete bioactive phytochemical. As a pure compound, it contains no meaningful protein, fat, or fiber content. Bioactive compound concentration: when isolated, it is evaluated at 100% purity in research settings, though in natural plant sources (e.g., rose hips, persimmon leaves, green tea, Moringa oleifera) concentrations typically range from 0.1–2.5 mg/g dry weight depending on plant matrix and extraction method. Bioavailability is limited by its glycosidic form; intestinal hydrolysis by beta-glucosidases cleaves the glucose moiety to release the aglycone kaempferol, which is more readily absorbed. Oral bioavailability studies in rodents suggest moderate absorption with peak plasma concentrations reached within 1–2 hours post-administration. The compound undergoes phase II metabolism (glucuronidation and sulfation) in the intestinal wall and liver. Molecular LogP is approximately 1.58, indicating moderate lipophilicity. No clinically established dietary reference intake or recommended daily amount exists. Solubility in water is low (~0.1 mg/mL at 25°C), which may further limit bioavailability in vivo without formulation enhancement.
How It Works
Mechanism of Action
Astragalin suppresses the NF-κB signaling pathway, reducing transcription of pro-inflammatory mediators including inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), and interleukin-6 (IL-6), as demonstrated in LPS-stimulated macrophage models. It also activates intrinsic apoptotic cascades by modulating Bcl-2 family protein ratios, upregulating Bax and cleaved caspase-3 while downregulating anti-apoptotic Bcl-2 expression in colorectal cancer cell lines. Additionally, astragalin inhibits MAPK (ERK1/2 and p38) phosphorylation, further attenuating inflammatory cytokine production.
Clinical Evidence
Current evidence for astragalin is predominantly preclinical. In vitro studies in LPS-stimulated RAW 264.7 macrophages have quantified inhibition of nitric oxide (IC50=363 µg/mL), PGE2 (IC50=134 µg/mL), and IL-6 (IC50=289 µg/mL), establishing a measurable anti-inflammatory potency profile. Mouse xenograft studies using HCT116 colorectal cancer cells demonstrated meaningful tumor growth inhibition at oral doses of 25–75 mg/kg, with dose-dependent responses. No randomized controlled trials in humans have been published as of the latest literature review, meaning all efficacy claims remain preliminary and should not be extrapolated directly to clinical use.
Safety & Interactions
Astragalin has not been evaluated in formal human safety trials, so a comprehensive adverse effect profile is not yet established. Animal studies at doses up to 75 mg/kg oral administration have not reported overt toxicity, but species-to-human dose translation requires caution. Because astragalin inhibits COX-2 and prostaglandin synthesis through pathways similar to NSAIDs, concurrent use with anticoagulants such as warfarin or antiplatelet drugs like aspirin may theoretically potentiate bleeding risk and warrants medical supervision. Pregnant or breastfeeding individuals should avoid supplementation due to a complete absence of safety data in these populations.
Synergy Stack
Hermetica Formulation Heuristic
Frequently Asked Questions
What is astragalin and what foods contain it?
Astragalin is a flavonoid glycoside structurally identified as kaempferol-3-O-glucoside, meaning it consists of the flavonol kaempferol bonded to a glucose molecule. It occurs naturally in persimmon leaves, rose hips (Rosa canina), green tea, Astragalus membranaceus root, and moringa leaves, making dietary exposure possible through whole foods before considering supplemental forms.
How does astragalin reduce inflammation?
Astragalin inhibits the NF-κB transcription factor pathway, preventing the upregulation of iNOS and COX-2 enzymes that produce nitric oxide and prostaglandin E2 (PGE2), two key mediators of acute inflammation. In LPS-stimulated macrophage experiments, it suppressed IL-6 with an IC50 of 289 µg/mL and PGE2 with an IC50 of 134 µg/mL, indicating meaningful potency at these concentrations in cell culture conditions.
What is the evidence for astragalin's anticancer properties?
Astragalin has shown anticancer activity in mouse xenograft models implanted with HCT116 human colorectal cancer cells, where oral doses of 25–75 mg/kg produced dose-dependent tumor growth inhibition. Its proposed mechanism involves activating caspase-3-mediated apoptosis and shifting Bcl-2/Bax protein ratios toward cell death in tumor cells. These results are promising but are limited to animal models; no human oncology trials have been conducted.
What is the recommended dosage of astragalin?
No clinically validated human dosage for isolated astragalin supplements has been established because human trials are lacking. Animal efficacy studies have used oral doses ranging from 25 to 75 mg/kg in mice, which cannot be directly converted to human equivalents without pharmacokinetic data. Consumers taking astragalin-containing supplements should follow manufacturer labeling and consult a healthcare provider, as an evidence-based standard dose does not yet exist.
Does astragalin interact with any medications?
Astragalin's COX-2 inhibitory mechanism suggests a theoretical interaction risk with NSAIDs, anticoagulants like warfarin, and antiplatelet agents such as clopidogrel, potentially enhancing bleeding tendency when combined. It may also theoretically affect cytochrome P450 enzyme activity based on patterns observed with structurally similar kaempferol-based flavonoids, which could alter the metabolism of co-administered drugs. No human pharmacokinetic interaction studies have been published, so these risks remain speculative but prudent to discuss with a physician.
What is the bioavailability of astragalin and does it need to be taken with food?
Astragalin is a flavonoid glycoside with limited oral bioavailability; its absorption may be enhanced when consumed with dietary fats or taken alongside meals. As a plant-derived compound, astragalin undergoes glucuronidation and sulfation in the body, which can reduce circulating levels of the parent compound. Taking astragalin with food may improve its absorption compared to fasting administration, though clinical studies directly examining optimal absorption conditions in humans are limited.
How does astragalin compare to other flavonoids like quercetin or kaempferol for anti-inflammatory effects?
Astragalin is a kaempferol glycoside (kaempferol-3-O-glucoside) that shares a similar aglycone backbone with other kaempferol derivatives but differs structurally from quercetin, which has additional hydroxyl groups on its B-ring. In vitro studies suggest astragalin inhibits inflammatory markers (IL-6, PGE2, nitric oxide) at comparable potency to other flavonoids, though direct head-to-head comparisons in human studies are scarce. The glycoside structure of astragalin may affect its absorption and metabolic fate differently than aglycone forms of kaempferol or quercetin.
What populations might benefit most from astragalin supplementation based on current research?
Preliminary evidence suggests astragalin may be of interest for individuals with chronic inflammatory conditions or colorectal cancer risk, given its NF-κB pathway suppression in cancer models and IL-6 inhibition in macrophage studies. However, current research is limited to in vitro and animal studies, so clinical applicability to specific patient populations has not been established. Until human clinical trials are conducted, astragalin supplementation cannot be recommended for targeted therapeutic use in any particular group.
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