Compound Monograph

Isovitexin

Phenolics Flavones Natural (plant-derived)

Isovitexin (apigenin-6-C-glucoside, or saponaretin) is a flavone C-glycoside of passionflower, gentian and many cereal grains, with a broad but entirely preclinical antioxidant and anti-inflammatory profile. Its carbon-bonded sugar resists ordinary hydrolysis, yet oral bioavailability stays low and there are no human trials of the isolate.

Sources · 13

Where Does It Come From?

Isovitexin is a naturally occurring flavonoid (flavone c-glycoside), found in Passionflower, Gentian and 11 other sources. It is well tolerated orally (low toxicity).

Also found in
Bamboo leaves Monograph coming soon
Cereal grains Monograph coming soon
Pigeon pea Monograph coming soon

Concentration

Content by Source

Concentrations not reported. No percent-dry-weight or mg/g figures have been published for this compound in its source plants.

Isovitexin at a Glance

Isovitexin is a flavone C-glycoside — specifically apigenin-6-C-glucoside, a molecule of apigenin carrying a single glucose unit joined through a carbon–carbon bond at the 6-position. It is the 6-C positional isomer of vitexin (apigenin-8-C-glucoside), and older literature calls it saponaretin or homovitexin. It occurs widely across the plant kingdom — in passionflower, gentian, cereal grains, bamboo, pigeon pea and many others — usually as one of a set of co-occurring C-glycosylflavones rather than a dominant constituent.

Its preclinical profile is genuinely broad: antioxidant, anti-inflammatory, neuroprotective, anti-atherosclerotic and anticancer effects are each reported in cell and rodent models, with the most substantial single result being protection against lipopolysaccharide-induced acute lung injury through the NF-κB/MAPK and Nrf2/HO-1 pathways 3Reference 3Lv H et al. · 2016Isovitexin exerts anti-inflammatory and anti-oxidant activities on lipopolysaccharide-induced acute lung injury by inhibiting MAPK and NF-κB and activating HO-1/Nrf2 pathwaysView study →. The honest headline is the ceiling on that evidence: it is entirely preclinical. There are no controlled human trials of isolated isovitexin, and where a plant it marks (passionflower) has human-relevant activity, that activity belongs to the whole extract, not the isolate 7Reference 7Grundmann O et al. · 2008Anxiolytic activity of a phytochemically characterized Passiflora incarnata extract is mediated via the GABAergic systemView study →.

The molecule’s structure cuts two ways and supplies the thread that runs through all of it. Its carbon-bonded sugar resists the acid and enzyme hydrolysis that split ordinary O-glycosides — yet its oral bioavailability is low, and, unusually for a C-glycoside, specific gut bacteria can still cleave it all the way to free apigenin 10Reference 10Braune A · 2012Intestinal bacterium Eubacterium cellulosolvens deglycosylates flavonoid C- and O-glucosidesView study →. That tension between stability and delivery is the compound-unique story.

Isovitexin vs. Vitexin, Orientin & the C-Glycosides

Isovitexin is one of a quartet of near-identical flavone C-glycosides that the herbal literature routinely lists together as the “C-glycosylflavones” of a plant such as passionflower or chickweed. The distinctions are small but pharmacologically real, and turn on two axes: the aglycone (apigenin vs. its catechol-bearing cousin luteolin) and the position of C-glycosylation (C-6 vs. C-8).

CompoundAglyconeSugar position
Isovitexin (saponaretin)apigenin (4’-OH B-ring)glucose at C-6
Vitexinapigeninglucose at C-8
Orientinluteolin (3’,4’-diOH B-ring)glucose at C-8
Iso-orientin (homoorientin)luteolinglucose at C-6

Isovitexin and vitexin are positional isomers — apigenin-6-C-glucoside versus apigenin-8-C-glucoside — and are so alike that they are usually isolated and reported together 1,2Reference 1Yan W et al. · 2025Dietary flavonoids vitexin and isovitexin: new insights into their functional roles in human health and disease preventionView study →Reference 2He M et al. · 2016ReviewA review on the pharmacological effects of vitexin and isovitexinView study →. The aglycone axis is the one that matters most for antioxidant chemistry: in the classic head-to-head study of C-glycosylflavones from chickweed, direct radical-scavenging activity was found only for the luteolin-based orientin and iso-orientin — not for the apigenin-based vitexin and isovitexin 6Reference 6Budzianowski J et al. · 1991Studies on antioxidative activity of some C-glycosylflavonesView study →. The extra B-ring hydroxyl of the luteolin core (its catechol) is the usual explanation, and it is why isovitexin is a weak direct antioxidant even though it can still switch on a cell’s endogenous antioxidant defences (see below).

C-Glycoside Stability & Bioavailability

The single most important thing to understand about isovitexin’s pharmacology is what its carbon–carbon bond does — and does not — buy it.

In an ordinary flavonoid O-glycoside, the sugar hangs off an oxygen atom and is readily cleaved: stomach acid, intestinal glycosidases and gut bacteria hydrolyse it, releasing the free aglycone that is often the truly absorbed species. Isovitexin is a C-glycoside — the glucose is bolted directly to the flavone carbon skeleton — so it resists that ordinary hydrolysis and travels largely as the intact glycoside 1,2Reference 1Yan W et al. · 2025Dietary flavonoids vitexin and isovitexin: new insights into their functional roles in human health and disease preventionView study →Reference 2He M et al. · 2016ReviewA review on the pharmacological effects of vitexin and isovitexinView study →. This stability is real and is part of why C-glycosylflavones are robust dietary and pharmacopoeial markers.

The intuitive expectation — that a stable molecule should therefore be well absorbed — does not hold. Isovitexin’s oral bioavailability is low: reviews describe poor gastrointestinal absorption with heavy first-pass metabolism (on the order of ~90% removed in the intestine), and formulation strategies (nanoparticles, encapsulation, cyclodextrin inclusion) are being explored precisely to overcome it 1,2Reference 1Yan W et al. · 2025Dietary flavonoids vitexin and isovitexin: new insights into their functional roles in human health and disease preventionView study →Reference 2He M et al. · 2016ReviewA review on the pharmacological effects of vitexin and isovitexinView study →. Rat pharmacokinetics done intravenously — to sidestep absorption entirely — show a short half-life (~1 h) and rapid distribution into kidney, intestine and liver 9Reference 9Li Y et al. · 2015AnimalPharmacokinetics and tissue distribution study of isovitexin in rats by HPLC-MS/MSView study →.

There is one twist that sets isovitexin apart from the other C-glycosides. Although the C–C bond resists chemical hydrolysis, a specific human gut bacterium, Eubacterium cellulosolvens, can cleave the flavone C-glucosides and deglycosylate isovitexin all the way to free apigenin 10Reference 10Braune A · 2012Intestinal bacterium Eubacterium cellulosolvens deglycosylates flavonoid C- and O-glucosidesView study →. So the practical picture is layered: isovitexin survives the stomach and small intestine largely intact, is poorly absorbed as the parent glycoside, and any aglycone-mediated effect depends on the colonic microbiota rather than on host enzymes. The recurring caution on every C-glycoside page applies here too — the striking in-vitro potencies sit above the exposures an oral dose is likely to achieve, so the mechanistic results should be read as mechanism, not as a delivered human effect.

What It's Used For

Isovitexin’s evidence is a preclinical machine: cell and rodent studies of the isolate, plus umbrella reviews. What matters is which application and the fact that no rung of it is human.

Anti-inflammatory is the strongest signal, and it is the same story in several tissues:isovitexin repeatedly suppresses NF-κB and MAPK signalling while inducing Nrf2/HO-1, cutting pro-inflammatory cytokines, iNOS and COX-2 — shown both in cultured macrophages and in whole animals (acute lung injury, gouty arthritis) 3,14Reference 3Lv H et al. · 2016Isovitexin exerts anti-inflammatory and anti-oxidant activities on lipopolysaccharide-induced acute lung injury by inhibiting MAPK and NF-κB and activating HO-1/Nrf2 pathwaysView study →Reference 14Sun X et al. · 2021AnimalIsovitexin alleviates acute gouty arthritis in rats by inhibiting inflammation via the TLR4/MyD88/NF-κB pathwayView study →.
A weak direct antioxidant that works indirectly:lacking the catechol B-ring of the luteolin glycosides, isovitexin was inactive in a direct radical-scavenging assay 6Reference 6Budzianowski J et al. · 1991Studies on antioxidative activity of some C-glycosylflavonesView study → — yet in cells it lowers ROS by switching on the endogenous Nrf2/HO-1 antioxidant programme 3Reference 3Lv H et al. · 2016Isovitexin exerts anti-inflammatory and anti-oxidant activities on lipopolysaccharide-induced acute lung injury by inhibiting MAPK and NF-κB and activating HO-1/Nrf2 pathwaysView study →. The distinction is the point.
Neuroprotection is a genuine isolate result:isolated isovitexin, at the concentration found in the plant, protected hippocampal tissue against glutamate excitotoxicity — where apigenin did not 4Reference 4Dos Santos KC et al. · 2016AnimalPassiflora actinia hydroalcoholic extract and its major constituent, isovitexin, are neuroprotective against glutamate-induced cell damage in mice hippocampal slicesView study →.
The honest headline:every study here is cell or rodent work on the isolate; there are no human trials of isovitexin, and the one plant it marks with real human data — passionflower — owes its anxiolytic effect to the whole GABAergic extract, not to isovitexin 7Reference 7Grundmann O et al. · 2008Anxiolytic activity of a phytochemically characterized Passiflora incarnata extract is mediated via the GABAergic systemView study →.
The delivery caveat:the C-glycoside resists ordinary hydrolysis but is poorly bioavailable, and only colonic bacteria cleave it to apigenin — so in-vitro potencies overstate what an oral dose can plausibly deliver 1,9,10Reference 1Yan W et al. · 2025Dietary flavonoids vitexin and isovitexin: new insights into their functional roles in human health and disease preventionView study →Reference 9Li Y et al. · 2015AnimalPharmacokinetics and tissue distribution study of isovitexin in rats by HPLC-MS/MSView study →Reference 10Braune A · 2012Intestinal bacterium Eubacterium cellulosolvens deglycosylates flavonoid C- and O-glucosidesView study →.
Evidence by IndicationStrength of support · Beta

Support is an experimental score — weighted by study type (human > animal > in vitro) and volume. A beta, not a validated metric. There is no human evidence for isolated isovitexin, so every score is capped by design — these rank preclinical strength, not clinical proof.

Mechanisms

Target / pathwayEffectRelevant to
NF-κB (IκB / p65 nuclear translocation)suppressed → ↓TNF-α, IL-6, iNOS, COX-2
anti-inflammatory; anti-atherosclerotic
MAPK (p38 / ERK / JNK phosphorylation)inhibited → dampened inflammatory signalling
anti-inflammatory
Nrf2 / HO-1 antioxidant axisinduced → ↑endogenous antioxidant enzymes, ↓ROS
indirect antioxidant; cytoprotection
TLR4 / MyD88suppressed upstream innate-immune signalling
anti-inflammatory (gout)
Endothelial adhesion molecules (ICAM-1, VCAM-1)↓ → reduced leukocyte adhesion
anti-atherosclerotic
miR-34a (tumour-suppressor microRNA)up-regulated → ↑Bax, ↓Bcl-2/Mcl-1, apoptosis
anticancer (preclinical)
Endothelial Ca²⁺ mobilisationmobilises intracellular Ca²⁺ in pulmonary endothelium
vasodilation
Direct radical scavengingweak/absent (no catechol B-ring)
antioxidant (the key contrast with orientin)

The load-bearing point is that isovitexin’s antioxidant action is indirect — it is a poor direct radical scavenger that instead switches on the Nrf2/HO-1 programme — and that its anti-inflammatory NF-κB/MAPK suppression is the most replicated effect. Almost all of it is in-vitro or rodent, on the isolate.

Pharmacokinetics

Isovitexin’s pharmacokinetics are thinly characterised and route-limited, and dominated by two facts. First, as a polar C-glycoside it is poorly absorbed orally with extensive intestinal first-pass metabolism, giving low systemic bioavailability — the reason formulation work (nanoparticles, encapsulation, cyclodextrin inclusion) is being pursued 1,2Reference 1Yan W et al. · 2025Dietary flavonoids vitexin and isovitexin: new insights into their functional roles in human health and disease preventionView study →Reference 2He M et al. · 2016ReviewA review on the pharmacological effects of vitexin and isovitexinView study →. Second, the one dedicated rodent study dosed rats intravenously (2 mg/kg) — deliberately bypassing absorption — and found a short half-life (t½ ≈ 1.05 h) and rapid distribution, with the main tissue depots being kidney, intestine and liver 9Reference 9Li Y et al. · 2015AnimalPharmacokinetics and tissue distribution study of isovitexin in rats by HPLC-MS/MSView study →. Distinctively, although the C-glycoside bond resists ordinary chemical hydrolysis, the gut bacterium Eubacterium cellulosolvens can deglycosylate isovitexin completely to free apigenin 10Reference 10Braune A · 2012Intestinal bacterium Eubacterium cellulosolvens deglycosylates flavonoid C- and O-glucosidesView study → — so unlike a stable systemic marker, its aglycone is generated by the colonic microbiota rather than by host enzymes. No human pharmacokinetic data exist, and there is no validated oral bioavailability figure carried here (see the gaps tracker).

Clinical Trials

There are no clinical trials of isolated isovitexin. The entire evidence base is preclinical (cell and rodent). The nearest human-relevant data belong to whole Passiflora extracts in which isovitexin is only a marker 7Reference 7Grundmann O et al. · 2008Anxiolytic activity of a phytochemically characterized Passiflora incarnata extract is mediated via the GABAergic systemView study →.

CompletedPlannedTerminatedPreclinical
None(isolate)——Anti-inflammatory, neuroprotective, antioxidant, anti-atherosclerotic, anticancer (all cell/rodent)

Last checked: July 2026.

Isolate vs. Plant Studies

The evidence divides cleanly, and mostly favours the isolate — a genuine strength for a mechanism base. The anti-inflammatory work (acute lung injury 3Reference 3Lv H et al. · 2016Isovitexin exerts anti-inflammatory and anti-oxidant activities on lipopolysaccharide-induced acute lung injury by inhibiting MAPK and NF-κB and activating HO-1/Nrf2 pathwaysView study →, gout 14Reference 14Sun X et al. · 2021AnimalIsovitexin alleviates acute gouty arthritis in rats by inhibiting inflammation via the TLR4/MyD88/NF-κB pathwayView study →), the neuroprotective hippocampal-slice experiment 4Reference 4Dos Santos KC et al. · 2016AnimalPassiflora actinia hydroalcoholic extract and its major constituent, isovitexin, are neuroprotective against glutamate-induced cell damage in mice hippocampal slicesView study →, the anticancer spheroid study 8Reference 8Xu C et al. · 2020Isovitexin inhibits stemness and induces apoptosis in hepatocellular carcinoma SK-Hep-1 spheroids by upregulating miR-34a expressionView study → and the anti-atherosclerotic endothelial/smooth-muscle work 5Reference 5Kesavan R et al. · 2016Gentiana lutea exerts anti-atherosclerotic effects by preventing endothelial inflammation and smooth muscle cell migrationView study → all test isovitexin itself. The antioxidant data sit on both sides: the chickweed study isolated the four C-glycosylflavones and compared them head-to-head 6Reference 6Budzianowski J et al. · 1991Studies on antioxidative activity of some C-glycosylflavonesView study →, while the Nrf2/HO-1 induction is isovitexin acting in cells 3Reference 3Lv H et al. · 2016Isovitexin exerts anti-inflammatory and anti-oxidant activities on lipopolysaccharide-induced acute lung injury by inhibiting MAPK and NF-κB and activating HO-1/Nrf2 pathwaysView study →.

The one place a plant isovitexin marks has human-relevant activity is passionflower — and there the effect is explicitly the whole extract’s: an HPLC-characterised Passiflora incarnata extract (isovitexin among its markers) was anxiolytic via the GABAergic system, comparable to diazepam, in mice 7Reference 7Grundmann O et al. · 2008Anxiolytic activity of a phytochemically characterized Passiflora incarnata extract is mediated via the GABAergic systemView study →. That effect cannot be assigned to isovitexin. So the correct framing is: solid isolate mechanism across inflammation, neuroprotection and vascular biology + no human isolate data + a plant-level effect (passionflower) that is not isovitexin’s to claim.

Its Role in Plants

Isovitexin is a flavone C-glycoside built on the general flavonoid pathway. Its flavone core derives from apigenin’s precursors, and the defining C-glycosylation is installed not on the finished flavone but on an intermediate: a 2-hydroxyflavanone (produced by a CYP93-family flavanone 2-hydroxylase) is C-glucosylated by a C-glycosyltransferase (CGT), and dehydration then yields the flavone C-glycoside 15Reference 15Vanegas KG et al. · 2018Indirect and direct routes to C-glycosylated flavones in Saccharomyces cerevisiaeView study →. In engineered-yeast reconstructions the “direct” route — in which certain CGTs glycosylate the finished flavone — tends to favour the 6-C products such as isovitexin, whereas the “indirect” 2-hydroxyflavanone route yields mixtures of the 6-C and 8-C (vitexin) isomers 15Reference 15Vanegas KG et al. · 2018Indirect and direct routes to C-glycosylated flavones in Saccharomyces cerevisiaeView study →.

Functionally, C-glycosylflavones like isovitexin contribute to a plant’s antioxidant and UV-protective flavonoid pool and to stress and defence chemistry. As with any constituent, this plant-biology role does not translate into a human-pharmacology claim.

Prevalence in Nature

Isovitexin is widespread but rarely dominant. It occurs across many plant families, typically as one of a co-occurring set of C-glycosylflavones (isovitexin, vitexin, orientin, iso-orientin). Documented sources include the aerial parts of passionflower (Passiflora incarnata), where the flavonoid C-glycosides are the pharmacopoeial marker fraction 16Reference 16Miroddi M et al. · 2013Clinical trialPassiflora incarnata L.: ethnopharmacology, clinical application, safety and evaluation of clinical trialsView study →, the root and herb of gentian (Gentiana lutea) 5Reference 5Kesavan R et al. · 2016Gentiana lutea exerts anti-atherosclerotic effects by preventing endothelial inflammation and smooth muscle cell migrationView study →, and cereal grains and pulses — millet, wheat, oats, barley, pigeon pea — as well as bamboo leaves and mimosa 1,2Reference 1Yan W et al. · 2025Dietary flavonoids vitexin and isovitexin: new insights into their functional roles in human health and disease preventionView study →Reference 2He M et al. · 2016ReviewA review on the pharmacological effects of vitexin and isovitexinView study →.

Reliable quantitative in-planta figures for isovitexin specifically are sparse in the accessible literature: it is generally reported as a present-and-identified marker rather than quantified in mg/g, and the passionflower total-flavonoid figure is given for the C-glycoside fraction as a whole rather than for isovitexin alone 16Reference 16Miroddi M et al. · 2013Clinical trialPassiflora incarnata L.: ethnopharmacology, clinical application, safety and evaluation of clinical trialsView study →. Those measured-concentration holes are logged in the compound’s gaps tracker to chase on a later pass.

Major Natural Sources

SourcePlant partReported isovitexin content
Passionflower (Passiflora incarnata)aerial partsmarker C-glycoside; not separately quantified here 7,16Reference 7Grundmann O et al. · 2008Anxiolytic activity of a phytochemically characterized Passiflora incarnata extract is mediated via the GABAergic systemView study →Reference 16Miroddi M et al. · 2013Clinical trialPassiflora incarnata L.: ethnopharmacology, clinical application, safety and evaluation of clinical trialsView study →
Gentian (Gentiana lutea)root / herbidentified constituent; not quantified here 5Reference 5Kesavan R et al. · 2016Gentiana lutea exerts anti-atherosclerotic effects by preventing endothelial inflammation and smooth muscle cell migrationView study →
Millet, wheat, oats, barley, pigeon peagrain / seedreported, not quantified here 1,2Reference 1Yan W et al. · 2025Dietary flavonoids vitexin and isovitexin: new insights into their functional roles in human health and disease preventionView study →Reference 2He M et al. · 2016ReviewA review on the pharmacological effects of vitexin and isovitexinView study →
Bamboo leaves, mimosaleafreported, not quantified here 1,2Reference 1Yan W et al. · 2025Dietary flavonoids vitexin and isovitexin: new insights into their functional roles in human health and disease preventionView study →Reference 2He M et al. · 2016ReviewA review on the pharmacological effects of vitexin and isovitexinView study →

These are qualitative occurrence notes, not whole-plant percentages; measured levels shift with species, tissue, processing and method, and the numeric figures are pending (see the gaps tracker).

Discovery & Synthesis

Isovitexin is a long-known apigenin C-glycoside — the 6-C positional isomer of vitexin, historically named saponaretin (and homovitexin) as it was characterised across many species through 20th-century flavonoid chemistry. The precise date and author of its first isolation are not well documented in the accessible literature; it entered pharmacology as one of a cluster of flavone C-glycosides identified together in plants such as passionflower, gentian and the cereals.

Modern synthesis of isovitexin is chiefly of interest for supply and study rather than commerce: because direct chemical C-glycosylation is difficult, recent work reconstructs the biosynthetic route in engineered microbes — expressing a flavanone 2-hydroxylase together with a C-glycosyltransferase in Saccharomyces cerevisiae, where the “direct” glycosylation route favours the 6-C isovitexin isomer 15Reference 15Vanegas KG et al. · 2018Indirect and direct routes to C-glycosylated flavones in Saccharomyces cerevisiaeView study →. There is no large-scale commercial manufacture; research material is obtained by extraction from flavonoid-rich plants or by such biosynthetic routes.

Patents: not yet researched.

Toxicity & Safety

Isovitexin carries a low toxicity flag. It is a constituent of ordinary foods and beverages — cereal grains and pulses, and passionflower/gentian preparations — consumed for generations without a specific safety signal attached to the molecule, and its poor absorption further limits systemic exposure 1,9Reference 1Yan W et al. · 2025Dietary flavonoids vitexin and isovitexin: new insights into their functional roles in human health and disease preventionView study →Reference 9Li Y et al. · 2015AnimalPharmacokinetics and tissue distribution study of isovitexin in rats by HPLC-MS/MSView study →. Preclinically it has an anti-inflammatory, cytoprotective character rather than a toxic one, and an oral rodent study used it as a therapeutic agent (an osteoanabolic effect in ovariectomised mice) without reporting overt toxicity 11Reference 11Pal S et al. · 2022AnimalOral administration of isovitexin, a naturally occurring apigenin derivative showed osteoanabolic effect in ovariectomized mice: a comparative study with teriparatideView study →. No isolate-specific genotoxicity or repeat-dose package is characterised here, and there are no human safety data; the low rating reflects its dietary ubiquity and benign preclinical record, not a formal toxicology dossier.

One mechanistic nuance is worth flagging rather than alarming over: because colonic bacteria can convert isovitexin to apigenin 10Reference 10Braune A · 2012Intestinal bacterium Eubacterium cellulosolvens deglycosylates flavonoid C- and O-glucosidesView study →, any whole-body assessment of exposure has to account for the aglycone, not just the parent glycoside. No adverse consequence of this is documented.

Safety at a Glance
Low / no toxicity
  • Low-toxicity dietary flavonoid. A normal constituent of grains, pulses and herbal preparations, with no specific safety signal and limited systemic absorption 1,9Reference 1Yan W et al. · 2025Dietary flavonoids vitexin and isovitexin: new insights into their functional roles in human health and disease preventionView study →Reference 9Li Y et al. · 2015AnimalPharmacokinetics and tissue distribution study of isovitexin in rats by HPLC-MS/MSView study →.
  • All evidence is preclinical. No human trials of the isolate exist — efficacy and safety in people are simply unknown.
  • Poor bioavailability undercuts potency. In-vitro and rodent effects occur at exposures an oral dose may not reach; do not read the mechanistic results as a delivered human benefit 1,9Reference 1Yan W et al. · 2025Dietary flavonoids vitexin and isovitexin: new insights into their functional roles in human health and disease preventionView study →Reference 9Li Y et al. · 2015AnimalPharmacokinetics and tissue distribution study of isovitexin in rats by HPLC-MS/MSView study →.
  • Marker, not proven active, in passionflower. Its presence does not make isovitexin responsible for a herb’s effect — the passionflower anxiolysis is the whole extract’s 7Reference 7Grundmann O et al. · 2008Anxiolytic activity of a phytochemically characterized Passiflora incarnata extract is mediated via the GABAergic systemView study →.

Dosage

There is no established or recommended human dose for isolated isovitexin. The figures in the literature are preclinical: cell-culture concentrations (typically low micromolar) and rodent doses — for example 100 mg/kg in the rat gout model 14Reference 14Sun X et al. · 2021AnimalIsovitexin alleviates acute gouty arthritis in rats by inhibiting inflammation via the TLR4/MyD88/NF-κB pathwayView study →, an oral regimen in the ovariectomised-mouse bone study 11Reference 11Pal S et al. · 2022AnimalOral administration of isovitexin, a naturally occurring apigenin derivative showed osteoanabolic effect in ovariectomized mice: a comparative study with teriparatideView study →, and the 2 mg/kg intravenous dose used to map its pharmacokinetics 9Reference 9Li Y et al. · 2015AnimalPharmacokinetics and tissue distribution study of isovitexin in rats by HPLC-MS/MSView study →. None is convertible to human self-dosing, and the compound’s low oral bioavailability would in any case complicate translating a rodent dose to an oral human one 1,9Reference 1Yan W et al. · 2025Dietary flavonoids vitexin and isovitexin: new insights into their functional roles in human health and disease preventionView study →Reference 9Li Y et al. · 2015AnimalPharmacokinetics and tissue distribution study of isovitexin in rats by HPLC-MS/MSView study →.

Real human exposure is dietary and indirect — isovitexin arrives as one C-glycosylflavone within grains, pulses, passionflower and gentian products, whose own dosing (as foods or standardised herbal extracts) is decided at the herb/product level, not the molecule level. These are doses studied in research and are not a personal recommendation.

References

  1. Yan W, Cheng J, Xu B (2025). Dietary flavonoids vitexin and isovitexin: new insights into their functional roles in human health and disease prevention. International Journal of Molecular Sciences. https://pubmed.ncbi.nlm.nih.gov/40725244/
  2. He M, Min JW, Kong WL, He XH, Li JX, Peng BW (2016). A review on the pharmacological effects of vitexin and isovitexin. Fitoterapia. https://pubmed.ncbi.nlm.nih.gov/27693342/
  3. Lv H, Yu Z, Zheng Y, Wang L, Qin X, Cheng G, Ci X (2016). Isovitexin exerts anti-inflammatory and anti-oxidant activities on lipopolysaccharide-induced acute lung injury by inhibiting MAPK and NF-κB and activating HO-1/Nrf2 pathways. International Journal of Biological Sciences. https://pubmed.ncbi.nlm.nih.gov/26722219/
  4. Dos Santos KC, Borges TV, Olescowicz G, Ludka FK, de Moraes Santos CA, Molz S (2016). Passiflora actinia hydroalcoholic extract and its major constituent, isovitexin, are neuroprotective against glutamate-induced cell damage in mice hippocampal slices. Journal of Pharmacy and Pharmacology. https://pubmed.ncbi.nlm.nih.gov/26800497/
  5. Kesavan R, Chandel S, Upadhyay S, Bendre R, Ganugula R, Potunuru UR, Giri H, Sahu G, Kumar PU, Reddy GB, Joksic G, Bera AK, Dixit M (2016). Gentiana lutea exerts anti-atherosclerotic effects by preventing endothelial inflammation and smooth muscle cell migration. Nutrition, Metabolism and Cardiovascular Diseases. https://pubmed.ncbi.nlm.nih.gov/26868432/
  6. Budzianowski J, Pakulski G, Robak J (1991). Studies on antioxidative activity of some C-glycosylflavones. Polish Journal of Pharmacology and Pharmacy. https://pubmed.ncbi.nlm.nih.gov/1824129/
  7. Grundmann O, Wang J, McGregor GP, Butterweck V (2008). Anxiolytic activity of a phytochemically characterized Passiflora incarnata extract is mediated via the GABAergic system. Planta Medica. https://pubmed.ncbi.nlm.nih.gov/19006051/
  8. Xu C, Cao X, Cao X, Liu L, Qiu Y, Li X, Zhou L, Ning Y, Ren K, Cao J (2020). Isovitexin inhibits stemness and induces apoptosis in hepatocellular carcinoma SK-Hep-1 spheroids by upregulating miR-34a expression. Anti-Cancer Agents in Medicinal Chemistry. https://pubmed.ncbi.nlm.nih.gov/32329692/
  9. Li Y, Zhang Y, Yang T, Li H, Guo J, Zhao Q, Xie J (2015). Pharmacokinetics and tissue distribution study of isovitexin in rats by HPLC-MS/MS. Journal of Chromatography B. https://pubmed.ncbi.nlm.nih.gov/25902051/
  10. Braune A, Blaut M (2012). Intestinal bacterium Eubacterium cellulosolvens deglycosylates flavonoid C- and O-glucosides. Applied and Environmental Microbiology. https://pubmed.ncbi.nlm.nih.gov/22961906/
  11. Pal S, Sharma S, Porwal K, Riyazuddin M, Kulkarni C, Chattopadhyay S, Sanyal S, Gayen JR, Chattopadhyay N (2022). Oral administration of isovitexin, a naturally occurring apigenin derivative showed osteoanabolic effect in ovariectomized mice: a comparative study with teriparatide. Calcified Tissue International. https://pubmed.ncbi.nlm.nih.gov/35451627/
  12. Guimarães CC, Oliveira DD, Valdevite M, Saltoratto ALF, Pereira SIV, França SC, Pereira AMS, Pereira PS (2015). The glycosylated flavonoids vitexin, isovitexin, and quercetrin isolated from Serjania erecta Radlk (Sapindaceae) leaves protect PC12 cells against amyloid-β25-35 peptide-induced toxicity. Food and Chemical Toxicology. https://pubmed.ncbi.nlm.nih.gov/26385725/
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