What is the difference between apigenin and apigenin-7-glucoside?

Apigenin is the free aglycone flavonoid, while apigenin-7-glucoside (apigetrin) has a glucose molecule attached at the 7-hydroxyl position, significantly increasing its water solubility. This glycosylation improves intestinal absorption in some contexts, as gut microbiota and intestinal β-glucosidases cleave the sugar to release bioactive apigenin. Some in vitro studies suggest apigetrin may be more potent than apigenin in certain cancer cell models despite requiring this conversion step.

What foods are high in apigenin-7-glucoside?

Apigenin-7-glucoside is found in notable concentrations in parsley (Petroselinum crispum), which contains up to 215 mg per 100g dry weight, making it one of the richest dietary sources. Chamomile flowers (Matricaria chamomilla), celery, and celeriac also provide meaningful amounts of this compound. Dried herbs generally contain higher concentrations than fresh equivalents due to reduced water content.

Can apigenin-7-glucoside help with cancer?

Apigenin-7-glucoside has demonstrated the ability to reduce viability of human colon cancer cell lines (including HCT116) at concentrations of 50–200 µM in laboratory studies, with cell death occurring primarily through necrosis rather than apoptosis. However, all available evidence is from in vitro cell culture experiments, with no human clinical trials conducted to date. These findings are hypothesis-generating only and should not be interpreted as evidence that the compound treats or prevents cancer in humans.

Does apigenin-7-glucoside interact with any medications?

Apigenin-class flavonoids, including apigetrin after conversion to apigenin, can inhibit cytochrome P450 enzymes CYP1A2 and CYP2C9 in vitro, which may slow the metabolism of drugs including warfarin, certain NSAIDs, and some antidepressants. This could theoretically increase drug plasma levels and associated side effects or toxicity. No human pharmacokinetic drug interaction studies have been conducted specifically for apigenin-7-glucoside supplements, so caution is warranted in individuals on narrow therapeutic index medications.

What is the recommended dosage of apigenin-7-glucoside?

There is currently no clinically established or regulatory-approved dosage for apigenin-7-glucoside as a supplement, as human clinical trials have not been performed. Effective concentrations observed in vitro (50–200 µM) are considerably higher than typical plasma levels achieved through dietary intake or standard supplementation. Until human pharmacokinetic and dose-finding studies are available, no specific dosage recommendation can be made with confidence.

Is apigenin-7-glucoside safe during pregnancy and breastfeeding?

There is insufficient human clinical data on apigenin-7-glucoside safety during pregnancy and breastfeeding, so supplementation is not recommended during these periods without medical supervision. Most safety evidence comes from animal and in vitro studies rather than controlled human trials. Pregnant or nursing individuals should consult with a healthcare provider before use.

How strong is the clinical evidence for apigenin-7-glucoside's health benefits in humans?

Current evidence for apigenin-7-glucoside is primarily limited to in vitro (test tube) and animal studies, with very few human clinical trials published to date. While promising findings exist for neuroprotection and anti-inflammatory effects, these results cannot yet be directly applied to human health claims. More rigorous human studies are needed to establish efficacy and safety in real-world supplementation.

Does apigenin-7-glucoside have better bioavailability than regular apigenin in the body?

Apigenin-7-glucoside is a naturally glycosylated form of apigenin that may have different absorption kinetics due to the attached glucose moiety, potentially improving intestinal uptake in some tissues. However, the glucoside must typically be deglycosylated by gut bacteria to be metabolized, which can affect overall bioavailability compared to free apigenin. Direct bioavailability comparisons in humans remain limited in the published literature.

Apigenin-7-glucoside (Apigetrin)

Apigenin-7-glucoside (apigetrin) is a glycosylated flavonoid in which apigenin is bound to glucose at the 7-position, improving its water solubility and bioavailability compared to the aglycone form. It exerts antioxidant, anti-inflammatory, and potential anticancer effects primarily by modulating oxidative stress pathways, NF-κB signaling, and apoptotic/necrotic cell death mechanisms.

Category: Compound Evidence: 4/10 Tier: Emerging

Apigenin-7-glucoside (Apigetrin) — Hermetica Encyclopedia

Origin & History

Apigenin-7-glucoside (Apigetrin) is a flavone glycoside, specifically a C-glycoside of apigenin, naturally occurring in various plants including Stachys tibetica. It is typically isolated from plant tissues using standard phytochemical procedures involving solvents and chromatography.

Historical & Cultural Context

Apigenin-7-glucoside from Stachys tibetica has been evaluated for anxiolytic effects in traditional medicine contexts, though specific historical systems or duration of use are not documented. The compound appears in plants used traditionally, but detailed ethnobotanical information is lacking.

Health Benefits

• May reduce colon cancer cell viability more effectively than apigenin, inducing cell death primarily through necrosis (in vitro evidence only)
• Shows potential neuroprotective effects in stroke models by reducing oxidative stress and improving neurological outcomes (animal studies only)
• Demonstrates anti-inflammatory properties in acute lung injury by inhibiting NF-κB/MAPK pathways and reducing inflammatory markers (mouse models)
• May inhibit cervical cancer cell proliferation, migration, and invasion through AE1/p16 pathway modulation (cell culture studies)
• Could protect against intestinal injury by reducing oxidative stress and ferroptosis when delivered via nanoparticles (animal models)

How It Works

Apigenin-7-glucoside is hydrolyzed in the gut by β-glucosidases to release free apigenin, which then inhibits pro-inflammatory NF-κB signaling and suppresses cyclooxygenase-2 (COX-2) expression, reducing downstream prostaglandin synthesis. In cancer cell models, it induces cytotoxicity primarily via necrosis rather than classical caspase-dependent apoptosis, potentially by disrupting mitochondrial membrane potential and generating reactive oxygen species (ROS). In ischemic stroke models, it attenuates oxidative damage by upregulating endogenous antioxidant enzymes including superoxide dismutase (SOD) and catalase, while reducing malondialdehyde (MDA) levels as a marker of lipid peroxidation.

Scientific Research

No human clinical trials, RCTs, or meta-analyses have been conducted on apigenin-7-glucoside. All available evidence comes from preclinical in vitro studies using cancer cell lines (HCT116, HeLa) and in vivo animal models examining neuroprotection, anti-inflammatory effects, and intestinal protection (PMC5547395, PMC10997139, PMC4679397, PMC4307331).

Clinical Summary

Research on apigenin-7-glucoside remains predominantly preclinical, with no large-scale human clinical trials published as of 2024. In vitro studies using human colon cancer cell lines (e.g., HCT116, HT-29) demonstrate that apigetrin reduces cell viability at concentrations of 50–200 µM, showing greater potency than apigenin aglycone in some assays. Animal studies using rodent models of cerebral ischemia report improvements in neurological deficit scores and reductions in infarct volume, alongside measurable decreases in oxidative stress biomarkers. The overall evidence base is considered preliminary, and extrapolation of these findings to human therapeutic use requires controlled clinical investigation.

Nutritional Profile

Apigenin-7-glucoside (Apigetrin) is a pure flavone glycoside compound (molecular formula: C21H20O10, molecular weight: 432.38 g/mol), not a whole food, so conventional macronutrient profiling does not apply. As a bioactive compound, its profile is characterized as follows: It consists structurally of the flavone aglycone apigenin (4',5,7-trihydroxyflavone) bound to a glucose moiety at the 7-position via a glycosidic bond. Typical concentrations in plant sources include: chamomile (Matricaria chamomilla) flowers at approximately 0.1–3.0 mg/g dry weight (one of the richest natural sources); parsley at approximately 0.3–1.2 mg/g dry weight; celery at approximately 0.1–0.5 mg/g dry weight; and artichoke at approximately 0.05–0.3 mg/g dry weight. Bioavailability: The glucose conjugate form (apigetrin) generally shows improved water solubility compared to free apigenin (solubility ~1 mg/mL vs. <0.01 mg/mL for apigenin), which may enhance intestinal absorption. Intestinal hydrolysis by beta-glucosidases cleaves the glycosidic bond to release free apigenin, which is the primary absorbed form. Oral bioavailability is estimated at 10–30% in animal models, with peak plasma concentrations typically reached within 1–2 hours post-ingestion. Protein binding in plasma is high (>95%, primarily to albumin). No caloric, fat, carbohydrate (beyond its own molecular structure), or protein content is relevant at physiological intake concentrations from food sources.

Preparation & Dosage

No clinically studied human dosages exist. Animal studies used 50-100 mg/kg intraperitoneally, while cell culture studies used 0.4-0.8 μg/ml. No standardized forms or extract percentages have been established. Consult a healthcare provider before starting any new supplement.

Synergy & Pairings

Apigenin, Rosmarinic acid, Other flavonoid glycosides, Antioxidant compounds, Neuroprotective botanicals

Safety & Interactions

Apigenin-7-glucoside has no established human safety profile from clinical trials, though flavonoids in this class are generally well tolerated at dietary intake levels found in parsley, chamomile, and celery. High supplemental doses of apigenin-class compounds may inhibit CYP1A2 and CYP2C9 enzyme activity, potentially elevating plasma concentrations of drugs such as warfarin, caffeine, and certain statins. Estrogenic activity has been reported for apigenin at the receptor level, suggesting caution in individuals with hormone-sensitive conditions including estrogen receptor-positive breast cancer. Pregnancy and lactation safety has not been established, and supplemental use is not recommended during these periods without medical supervision.