Compound Monograph

Isoorientin

Phenolics Flavones Natural (plant-derived)

Isoorientin (luteolin-6-C-glucoside, homoorientin) is the 6-C isomer of orientin — a flavone C-glycoside of chickweed, passionflower, passion-fruit and bamboo leaf. Its standout preclinical thread is Nrf2-driven hepatoprotection, alongside antioxidant, anti-inflammatory and neuroprotective activity, but its oral bioavailability is low (~9% in rats) and there are no human trials of the isolate.

Sources · 12

Where Does It Come From?

Isoorientin is a naturally occurring flavonoid (flavone c-glycoside), found in Chickweed, Passionflower, Passion fruit and 9 other sources. It is well tolerated orally (low toxicity).

Also found in
Bamboo leaves Monograph coming soon
Cecropia Monograph coming soon
Millet Monograph coming soon
Sasa borealis Monograph coming soon

Concentration

Content by Source

Reported concentrations across the plants that contain isoorientin — the bar marks the typical level, the line shows the reported range.

Typical level Reported range mg/g
Bamboo (Phyllostachys / Bambusa spp.) leaves 1–2.78 [13]

Literature figures for varying plant parts and preparations. Read them as a comparative guide, not exact assays.

Isoorientin at a Glance

Isoorientin is a flavone C-glycoside — specifically luteolin-6-C-glucoside (also called homoorientin), a molecule of luteolin carrying a single glucose unit joined through a carbon–carbon bond at the 6-position. It is the positional isomer of orientin (luteolin-8-C-glucoside), and the two travel together as a pair in the plants they mark: the aerial parts of chickweed and passionflower, passion-fruit (Passiflora edulis), bamboo leaf, Cecropia and millet 1,2Reference 1Ziqubu K et al. · 2020Isoorientin: a dietary flavone with the potential to ameliorate diverse metabolic complicationsView study →Reference 2Budzianowski J et al. · 1991Studies on antioxidative activity of some C-glycosylflavonesView study →.

Its preclinical profile is real and centres on one recurring mechanism — activation of the Nrf2 antioxidant pathway. The standout isoorientin thread, and the one that most distinguishes it from orientin, is hepatoprotection: in mice, isoorientin blunts acetaminophen (paracetamol) liver injury by switching on Nrf2, and the effect disappears in Nrf2-knockout animals 3,4Reference 3Lim JH et al. · 2007Isoorientin induces Nrf2 pathway-driven antioxidant response through phosphatidylinositol 3-kinase signalingView study →Reference 4Fan X et al. · 2018Isoorientin ameliorates APAP-induced hepatotoxicity via activation of Nrf2 antioxidative pathway: the involvement of AMPK/Akt/GSK3βView study →. Around that core sit antioxidant, anti-inflammatory, anti-nociceptive and neuroprotective effects, each shown in cell and rodent models 2,6,7,10Reference 2Budzianowski J et al. · 1991Studies on antioxidative activity of some C-glycosylflavonesView study →Reference 6Anilkumar K et al. · 2017Evaluation of anti-inflammatory properties of isoorientin isolated from tubers of Pueraria tuberosaView study →Reference 7Küpeli E et al. · 2004AnimalEvaluation of in vivo biological activity profile of isoorientinView study →Reference 10Kim B et al. · 2021Isoorientin inhibits amyloid β25-35-induced neuronal inflammation in BV2 cells by blocking the NF-κB signaling pathwayView study →. The honest headline is the same ceiling that caps every C-glycosylflavone here: the evidence is entirely preclinical. There are no controlled human trials of isolated isoorientin, and where a plant it marks (passionflower, Cecropia) has human-relevant activity, that activity belongs to the whole extract, not the isolate 1,8Reference 1Ziqubu K et al. · 2020Isoorientin: a dietary flavone with the potential to ameliorate diverse metabolic complicationsView study →Reference 8Andrade-Cetto A · 2001AnimalHypoglycemic effect of Cecropia obtusifolia on streptozotocin diabetic ratsView study →.

The molecule’s defining structural feature cuts two ways, exactly as for orientin. Its carbon-bonded sugar resists hydrolysis, so isoorientin survives the gut largely intact — yet its oral bioavailability is low, measured at roughly 9% in rats, held down by poor aqueous solubility and extensive first-pass metabolism 9Reference 9Shi P et al. · 2015AnimalMetabolism and plasma pharmacokinetics of isoorientin, a natural active ingredient, in Sprague-Dawley male rats after oral and intravenous administrationView study →. That tension between chemical stability and poor delivery is the compound-unique thread that runs through all of it.

Isoorientin vs. Orientin & the C-Glycosides

Isoorientin is easy to confuse with three near-identical siblings, and the herbal literature routinely lists them together as the “flavone C-glycosides” of a plant. The distinctions are small but real, and this molecule completes the quartet:

CompoundAglyconeSugar position
Isoorientin (homoorientin)luteolin (3’,4’-diOH B-ring)glucose at C-6
Orientinluteolinglucose at C-8
Isovitexinapigenin (4’-OH B-ring)glucose at C-6
Vitexinapigeninglucose at C-8

Two axes separate them: the aglycone (luteolin, with its catechol B-ring, versus apigenin, with a single hydroxyl) and the position of C-glycosylation (C-6 versus C-8). Isoorientin and orientin are the two luteolin glycosides — the “iso”/6-C prefix marks the sugar at C-6 — and this pair carried the antioxidant activity in the classic chickweed study, while the apigenin-based vitexin and isovitexin did not 2Reference 2Budzianowski J et al. · 1991Studies on antioxidative activity of some C-glycosylflavonesView study →. The extra B-ring hydroxyl of the luteolin core (the catechol) is the usual explanation: it makes isoorientin and orientin better radical scavengers than their apigenin twins.

The 6-C-versus-8-C distinction is not merely academic — it falls out of biosynthesis. When the C-glycosyltransferase acts directly on the finished flavone, it produces almost exclusively the 6-C-glucosides (isoorientin and isovitexin); the indirect route (via a 2-hydroxyflavanone intermediate), especially with 3’-hydroxylation, shifts the balance toward the 8-C-glucoside orientin 12Reference 12Vanegas KG et al. · 2018Indirect and direct routes to C-glycosylated flavones in Saccharomyces cerevisiaeView study →. So isoorientin is, in a real sense, the “direct-route” luteolin C-glycoside.

C-Glycoside Stability & Bioavailability

The single most important thing to understand about isoorientin’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. Isoorientin is a C-glycoside — the glucose is bolted directly to the flavone carbon skeleton — so it resists that hydrolysis and travels largely as the intact glycoside. This stability is real and is part of why C-glycosylflavones are robust dietary markers.

The intuitive expectation — that a stable molecule should therefore be well absorbed — does not hold. Isoorientin’s pharmacokinetics have been mapped once, in rats dosed both orally and intravenously, and the headline is a low oral bioavailability of about 9% (8.98 ± 1.07%) 9Reference 9Shi P et al. · 2015AnimalMetabolism and plasma pharmacokinetics of isoorientin, a natural active ingredient, in Sprague-Dawley male rats after oral and intravenous administrationView study →. The study attributes that poor systemic exposure to the compound’s low aqueous solubility and extensive first-pass metabolism, and it fits the broader picture of C-glycosides being poorly absorbed in mammals: after an oral gavage dose, only about 6% of the dose was recovered in urine versus ~45% in faeces over 72 hours — most of it never crossed the gut wall 9Reference 9Shi P et al. · 2015AnimalMetabolism and plasma pharmacokinetics of isoorientin, a natural active ingredient, in Sprague-Dawley male rats after oral and intravenous administrationView study →. The practical reading is a caution that recurs on every C-glycoside page: the striking in-vitro potencies sit above the concentrations an oral dose is likely to achieve in plasma, so the mechanistic results should be read as mechanism, not as a delivered human effect.

What It's Used For

Isoorientin’s evidence is a preclinical machine: cell and rodent studies of the isolate, plus umbrella reviews. The split that matters is which organ (the liver is the standout) and the fact that no rung of it is human.

Hepatoprotection is the real signal, and it is Nrf2 at root:in mice, isoorientin protects the liver against acetaminophen (paracetamol) toxicity — lowering ALT/AST, malondialdehyde and mortality — by activating Nrf2 via the AMPK/Akt/GSK3β axis and shielding mitochondria (↓JNK, ↓Bax translocation, ↓cytochrome-c/AIF release); the benefit is abolished in Nrf2-knockout animals 3,4Reference 3Lim JH et al. · 2007Isoorientin induces Nrf2 pathway-driven antioxidant response through phosphatidylinositol 3-kinase signalingView study →Reference 4Fan X et al. · 2018Isoorientin ameliorates APAP-induced hepatotoxicity via activation of Nrf2 antioxidative pathway: the involvement of AMPK/Akt/GSK3βView study →.
A coherent antioxidant core:the same Nrf2/PI3K activation that protects liver cells 3Reference 3Lim JH et al. · 2007Isoorientin induces Nrf2 pathway-driven antioxidant response through phosphatidylinositol 3-kinase signalingView study → also underlies protection of the kidney against cisplatin toxicity (SIRT1/SIRT6/Nrf2 → ↑HO-1/NQO1, ↓NOX4) 5Reference 5Fan X et al. · 2020Isoorientin attenuates cisplatin-induced nephrotoxicity through the inhibition of oxidative stress and apoptosis via activating the SIRT1/SIRT6/Nrf-2 pathwayView study → and the neuronal work below — one antioxidant/anti-apoptotic story told in several organs.
Genuine isolate anti-inflammatory data:isoorientin is a selective COX-2 inhibitor and, uniquely among these C-glycosides, has in-vivo isolate anti-inflammatory and anti-nociceptive activity (carrageenan paw-oedema and writhing tests, 15–30 mg/kg) 6,7Reference 6Anilkumar K et al. · 2017Evaluation of anti-inflammatory properties of isoorientin isolated from tubers of Pueraria tuberosaView study →Reference 7Küpeli E et al. · 2004AnimalEvaluation of in vivo biological activity profile of isoorientinView study →.
The honest headline:every study here is cell or rodent work; there are no human trials of isoorientin, its oral bioavailability is ~9% in rats 9Reference 9Shi P et al. · 2015AnimalMetabolism and plasma pharmacokinetics of isoorientin, a natural active ingredient, in Sprague-Dawley male rats after oral and intravenous administrationView study →, and the plants it marks with human-relevant data (passionflower, Cecropia) owe those effects to the whole extract, not the isolate 1,8Reference 1Ziqubu K et al. · 2020Isoorientin: a dietary flavone with the potential to ameliorate diverse metabolic complicationsView study →Reference 8Andrade-Cetto A · 2001AnimalHypoglycemic effect of Cecropia obtusifolia on streptozotocin diabetic ratsView 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 isoorientin, so every score is capped by design — these rank preclinical strength, not clinical proof.

Mechanisms

Target / pathwayEffectRelevant to
Nrf2 / ARE (via AMPK/Akt/GSK3β and PI3K)activates the master antioxidant programme → ↑NQO1, HO-1, SOD, glutathione
hepatoprotection; antioxidant; nephroprotection
ROS + antioxidant enzymes (SOD, catalase, GPx, GST)scavenges radicals; restores endogenous antioxidant enzymes
antioxidant; organ protection
Mitochondrial apoptotic pathway (Bcl-2 ↑, Bax ↓, cytochrome-c ↓, AIF ↓, caspase-3/9 ↓)anti-apoptotic — blocks the intrinsic cell-death cascade
hepatoprotection; neuroprotection
NF-κB (IκB phosphorylation, p65 translocation)suppressed → ↓TNF-α, IL-6, iNOS, COX-2
anti-inflammatory; neuroprotection
Cyclooxygenase-2 (COX-2)selective reversible inhibition (IC₅₀ ≈ 39 µM)
anti-inflammatory
SIRT1 / SIRT6up-regulated → Nrf2 activation, ↓NOX4
nephroprotection (cisplatin)
Endothelial Ca²⁺ mobilisation 11Reference 11Trettel CDS et al. · 2021The mechanisms of calcium mobilization by procyanidins, flavonols and flavonoids from Cecropia glaziovii Snethl in pulmonary endothelial cell cultures endorse its popular use as vasodilator phytomedicineView study →mobilises intracellular Ca²⁺ in pulmonary endothelium
vasodilation (Cecropia)

The load-bearing point is that these are mostly one story told in several organs: an Nrf2-driven antioxidant / anti-apoptotic core, with AMPK/Akt/GSK3β, PI3K, NF-κB and SIRT1/6 as the tissue-specific arms. Almost all of it is in-vitro or rodent, on the isolate.

Pharmacokinetics

Isoorientin’s pharmacokinetics are thinly characterised but, unusually for this class, include an oral figure. A single rat study dosed the compound both intravenously (5, 10, 15 mg/kg) and orally by gavage (150 mg/kg) and measured an oral bioavailability of 8.98 ± 1.07% — low, and attributed to the molecule’s low aqueous solubility and extensive first-pass metabolism 9Reference 9Shi P et al. · 2015AnimalMetabolism and plasma pharmacokinetics of isoorientin, a natural active ingredient, in Sprague-Dawley male rats after oral and intravenous administrationView study →. Mass balance underlines the absorption problem: over 72 hours, roughly 6% of an oral dose appeared in urine versus ~45% in faeces, i.e. most of the compound passed through unabsorbed 9Reference 9Shi P et al. · 2015AnimalMetabolism and plasma pharmacokinetics of isoorientin, a natural active ingredient, in Sprague-Dawley male rats after oral and intravenous administrationView study →. As a polar C-glycoside, isoorientin is hydrophilic and, like orientin, is not appreciably hydrolysed to free luteolin in the gut, so — unlike an O-glycoside — the aglycone is not the absorbed species. There is no human pharmacokinetic data, no repeat-dose or tissue-distribution profile beyond the excretion balance, and no direct blood–brain-barrier measurement (its isomer orientin penetrates the brain poorly) 9Reference 9Shi P et al. · 2015AnimalMetabolism and plasma pharmacokinetics of isoorientin, a natural active ingredient, in Sprague-Dawley male rats after oral and intravenous administrationView study →.

Clinical Trials

There are no clinical trials of isolated isoorientin. The entire evidence base is preclinical (cell and rodent). The nearest human-relevant data belong to whole plant extracts (passionflower, Cecropia) in which isoorientin is only a marker or co-constituent 1,8Reference 1Ziqubu K et al. · 2020Isoorientin: a dietary flavone with the potential to ameliorate diverse metabolic complicationsView study →Reference 8Andrade-Cetto A · 2001AnimalHypoglycemic effect of Cecropia obtusifolia on streptozotocin diabetic ratsView study →.

CompletedPlannedTerminatedPreclinical
None(isolate)——Hepatoprotection, antioxidant/Nrf2, anti-inflammatory, neuroprotection (all cell/rodent)

Last checked: July 2026.

Isolate vs. Plant Studies

The evidence divides cleanly. The mechanistic and protective work is the isolated molecule — the APAP-hepatotoxicity study 4Reference 4Fan X et al. · 2018Isoorientin ameliorates APAP-induced hepatotoxicity via activation of Nrf2 antioxidative pathway: the involvement of AMPK/Akt/GSK3βView study →, the HepG2 Nrf2/PI3K work 3Reference 3Lim JH et al. · 2007Isoorientin induces Nrf2 pathway-driven antioxidant response through phosphatidylinositol 3-kinase signalingView study →, the cisplatin-nephrotoxicity experiments 5Reference 5Fan X et al. · 2020Isoorientin attenuates cisplatin-induced nephrotoxicity through the inhibition of oxidative stress and apoptosis via activating the SIRT1/SIRT6/Nrf-2 pathwayView study →, the COX-2 and carrageenan anti-inflammatory data 6Reference 6Anilkumar K et al. · 2017Evaluation of anti-inflammatory properties of isoorientin isolated from tubers of Pueraria tuberosaView study →, the writhing/oedema profile 7Reference 7Küpeli E et al. · 2004AnimalEvaluation of in vivo biological activity profile of isoorientinView study → and the BV2 neuroinflammation study 10Reference 10Kim B et al. · 2021Isoorientin inhibits amyloid β25-35-induced neuronal inflammation in BV2 cells by blocking the NF-κB signaling pathwayView study → all test isoorientin itself, which is a genuine strength for a mechanism base and a step ahead of orientin’s mostly cell-and-tissue record.

The places a plant isoorientin marks have human-relevant activity, the effect is explicitly the whole extract’s: an aqueous Cecropia extract (isoorientin + chlorogenic acid) is hypoglycaemic in diabetic rats 8Reference 8Andrade-Cetto A · 2001AnimalHypoglycemic effect of Cecropia obtusifolia on streptozotocin diabetic ratsView study →, and passionflower owes its anxiolytic reputation to its whole GABAergic flavonoid–alkaloid complex, in which isoorientin is one HPLC marker among vitexin, isovitexin and orientin. Neither effect can be assigned to isoorientin alone. So the correct framing is: solid isolate mechanism in liver, kidney, immune and neural cells + no human isolate data + plant-level effects (Cecropia, passionflower) that are not isoorientin’s to claim.

Its Role in Plants

Isoorientin is a flavone C-glycoside built on the general flavonoid pathway. The flavone core comes from luteolin’s precursors, and the defining C-glycosylation is installed by a C-glycosyltransferase (CGT). Reconstructing the routes in yeast is revealing: when a CGT glycosylates the finished flavone directly, the product is almost exclusively the 6-C-glucoside — isoorientin (and, on the apigenin side, isovitexin) 12Reference 12Vanegas KG et al. · 2018Indirect and direct routes to C-glycosylated flavones in Saccharomyces cerevisiaeView study →. The alternative “indirect” route glucosylates a 2-hydroxyflavanone intermediate and yields mixtures of the 6-C and 8-C isomers, with 3’-hydroxylation tilting the balance toward the 8-C product orientin 12Reference 12Vanegas KG et al. · 2018Indirect and direct routes to C-glycosylated flavones in Saccharomyces cerevisiaeView study →. Isoorientin is thus the characteristic direct-route luteolin C-glycoside.

Functionally, C-glycosylflavones like isoorientin contribute to a plant’s antioxidant and UV-protective flavonoid pool and to stress and defence chemistry — the same radical-scavenging property that dominates the pharmacology. As with any constituent, this plant-biology role does not translate into a human-pharmacology claim.

Prevalence in Nature

Isoorientin is widespread but rarely dominant across plants as a whole — yet it is frequently the dominant C-glycoside within the specific plants that carry it. It occurs across several families, typically alongside its co-glycosides (orientin, vitexin, isovitexin). Documented sources include the aerial parts of chickweed (Stellaria media) and passionflower (Passiflora incarnata), passion-fruit (Passiflora edulis), bamboo leaves (Phyllostachys / Bambusa spp.), Cecropia and millet 1,2,8Reference 1Ziqubu K et al. · 2020Isoorientin: a dietary flavone with the potential to ameliorate diverse metabolic complicationsView study →Reference 2Budzianowski J et al. · 1991Studies on antioxidative activity of some C-glycosylflavonesView study →Reference 8Andrade-Cetto A · 2001AnimalHypoglycemic effect of Cecropia obtusifolia on streptozotocin diabetic ratsView study →.

Where it has been quantified, isoorientin often outstrips its 8-C twin. In bamboo leaf it is the leading C-glycoside at roughly 1.0–2.8 mg/g — far above the co-occurring orientin (0–0.07 mg/g) 13Reference 13Wang J et al. · 2012Rapid screening for flavone C-glycosides in the leaves of different species of bamboo and simultaneous quantitation of four marker compounds by HPLC-UV/DADView study →. In Passiflora edulis it is likewise the marker C-glycoside: reviews report on the order of ~5 mg/g in the leaf and roughly 16 mg/L in the fruit pulp, though those figures come from journals without retrievable identifiers and are given here as orientation, not verified points (see the gaps tracker). In chickweed and passionflower it is a characteristic but unquantified constituent 2Reference 2Budzianowski J et al. · 1991Studies on antioxidative activity of some C-glycosylflavonesView study →.

Major Natural Sources

SourcePlant partReported isoorientin content
Bamboo (Phyllostachys / Bambusa spp.)leaves~1.0–2.8 mg/g 13Reference 13Wang J et al. · 2012Rapid screening for flavone C-glycosides in the leaves of different species of bamboo and simultaneous quantitation of four marker compounds by HPLC-UV/DADView study →
Passion fruit (Passiflora edulis)leaf / fruit pulpreported ~5 mg/g leaf; not quantified here
Passionflower, chickweedaerial partsmarker constituent, not quantified here 2Reference 2Budzianowski J et al. · 1991Studies on antioxidative activity of some C-glycosylflavonesView study →
Cecropia, milletleaf / grainreported, not quantified here 1,8Reference 1Ziqubu K et al. · 2020Isoorientin: a dietary flavone with the potential to ameliorate diverse metabolic complicationsView study →Reference 8Andrade-Cetto A · 2001AnimalHypoglycemic effect of Cecropia obtusifolia on streptozotocin diabetic ratsView study →

These are content figures for the stated matrix (e.g. dried leaf), not whole-plant percentages, and they shift with species, processing and method.

Discovery & Synthesis

Isoorientin is a long-known luteolin C-glycoside — the “homo”/6-C isomer named in parallel with orientin. 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 across many species through the 20th century, and much of the modern isolate work has used material from Sasa borealis bamboo grass, Pueraria tuberosa and passion-fruit 3,6Reference 3Lim JH et al. · 2007Isoorientin induces Nrf2 pathway-driven antioxidant response through phosphatidylinositol 3-kinase signalingView study →Reference 6Anilkumar K et al. · 2017Evaluation of anti-inflammatory properties of isoorientin isolated from tubers of Pueraria tuberosaView study →.

Modern synthesis of isoorientin 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 C-glycosyltransferase (with or without a flavanone 2-hydroxylase) in Saccharomyces cerevisiae; notably, direct flavone glycosylation yields the 6-C product isoorientin essentially cleanly 12Reference 12Vanegas KG et al. · 2018Indirect and direct routes to C-glycosylated flavones in Saccharomyces cerevisiaeView study →. There is no large-scale commercial manufacture; material for research is obtained by extraction from rich sources (bamboo leaf, passion-fruit, millet) or by such biosynthetic routes.

Patents: not yet researched.

Toxicity & Safety

Isoorientin carries a low toxicity flag. It is a constituent of ordinary foods and beverages — chickweed (a wild edible green), passion-fruit, bamboo-leaf extract (a food antioxidant) and millet — consumed for generations without a specific safety signal attached to the molecule, and its poor absorption further limits systemic exposure 1,9Reference 1Ziqubu K et al. · 2020Isoorientin: a dietary flavone with the potential to ameliorate diverse metabolic complicationsView study →Reference 9Shi P et al. · 2015AnimalMetabolism and plasma pharmacokinetics of isoorientin, a natural active ingredient, in Sprague-Dawley male rats after oral and intravenous administrationView study →. In the one in-vivo profiling study, doses of 15–30 mg/kg produced no apparent acute toxicity and no gastric damage 7Reference 7Küpeli E et al. · 2004AnimalEvaluation of in vivo biological activity profile of isoorientinView 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.

Safety at a Glance
Low / no toxicity
  • Low-toxicity dietary flavonoid. A normal constituent of chickweed, passion-fruit, bamboo-leaf extract and millet, with no specific safety signal and limited systemic absorption 1,9Reference 1Ziqubu K et al. · 2020Isoorientin: a dietary flavone with the potential to ameliorate diverse metabolic complicationsView study →Reference 9Shi P et al. · 2015AnimalMetabolism and plasma pharmacokinetics of isoorientin, a natural active ingredient, in Sprague-Dawley male rats after oral and intravenous administrationView study →.
  • All evidence is preclinical. No human trials of the isolate exist — efficacy and safety in people are simply unknown.
  • Poor bioavailability undercuts potency. Oral bioavailability is ~9% in rats; in-vitro and rodent effects occur at exposures an oral dose may not reach, so do not read the mechanistic results as a delivered human benefit 9Reference 9Shi P et al. · 2015AnimalMetabolism and plasma pharmacokinetics of isoorientin, a natural active ingredient, in Sprague-Dawley male rats after oral and intravenous administrationView study →.
  • Marker, not proven active, in its herbs. Its presence does not make isoorientin responsible for a plant’s effect — the Cecropia hypoglycaemia and passionflower anxiolysis are the whole extracts’ 1,8Reference 1Ziqubu K et al. · 2020Isoorientin: a dietary flavone with the potential to ameliorate diverse metabolic complicationsView study →Reference 8Andrade-Cetto A · 2001AnimalHypoglycemic effect of Cecropia obtusifolia on streptozotocin diabetic ratsView study →.

Dosage

There is no established or recommended human dose for isolated isoorientin. The figures in the literature are preclinical: cell-culture concentrations (typically low micromolar) and rodent doses, including the 15–30 mg/kg used in the hepatoprotection and anti-nociception work 4,7Reference 4Fan X et al. · 2018Isoorientin ameliorates APAP-induced hepatotoxicity via activation of Nrf2 antioxidative pathway: the involvement of AMPK/Akt/GSK3βView study →Reference 7Küpeli E et al. · 2004AnimalEvaluation of in vivo biological activity profile of isoorientinView study → and the 150 mg/kg oral dose used to map its pharmacokinetics 9Reference 9Shi P et al. · 2015AnimalMetabolism and plasma pharmacokinetics of isoorientin, a natural active ingredient, in Sprague-Dawley male rats after oral and intravenous administrationView study →. None is convertible to human self-dosing, and the compound’s low (~9%) oral bioavailability would in any case complicate translating a rodent dose to an oral human one 9Reference 9Shi P et al. · 2015AnimalMetabolism and plasma pharmacokinetics of isoorientin, a natural active ingredient, in Sprague-Dawley male rats after oral and intravenous administrationView study →.

Real human exposure is dietary and indirect — isoorientin arrives as one C-glycosylflavone within chickweed, passionflower, passion-fruit, bamboo-leaf products and millet, whose own dosing (as foods or standardised herbal extracts) is decided at the herb/product level, not the molecule level. These are research figures and food-exposure notes, not a personal recommendation.

References

  1. Ziqubu K, Dludla PV, Joubert E, Muller CJF, Louw J, Tiano L, Nkambule BB, Kappo AP, Mazibuko-Mbeje SE (2020). Isoorientin: a dietary flavone with the potential to ameliorate diverse metabolic complications. Pharmacological Research. https://pubmed.ncbi.nlm.nih.gov/32407953/
  2. 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/
  3. Lim JH, Park HS, Choi JK, Lee IS, Choi HJ (2007). Isoorientin induces Nrf2 pathway-driven antioxidant response through phosphatidylinositol 3-kinase signaling. Archives of Pharmacal Research. https://pubmed.ncbi.nlm.nih.gov/18254247/
  4. Fan X, Lv H, Wang L, Deng X, Ci X (2018). Isoorientin ameliorates APAP-induced hepatotoxicity via activation of Nrf2 antioxidative pathway: the involvement of AMPK/Akt/GSK3β. Frontiers in Pharmacology. https://pubmed.ncbi.nlm.nih.gov/30546306/
  5. Fan X, Wei W, Huang J, Liu X, Ci X (2020). Isoorientin attenuates cisplatin-induced nephrotoxicity through the inhibition of oxidative stress and apoptosis via activating the SIRT1/SIRT6/Nrf-2 pathway. Frontiers in Pharmacology. https://pubmed.ncbi.nlm.nih.gov/32256355/
  6. Anilkumar K, Reddy GV, Azad R, Yarla NS, Dharmapuri G, Srivastava A, Kamal MA, Pallu R (2017). Evaluation of anti-inflammatory properties of isoorientin isolated from tubers of Pueraria tuberosa. Oxidative Medicine and Cellular Longevity. https://pubmed.ncbi.nlm.nih.gov/28243356/
  7. Küpeli E, Aslan M, Gürbüz I, Yesilada E (2004). Evaluation of in vivo biological activity profile of isoorientin. Zeitschrift für Naturforschung C. https://pubmed.ncbi.nlm.nih.gov/15666535/
  8. Andrade-Cetto A, Wiedenfeld H (2001). Hypoglycemic effect of Cecropia obtusifolia on streptozotocin diabetic rats. Journal of Ethnopharmacology. https://pubmed.ncbi.nlm.nih.gov/11694359/
  9. Shi P, Lin X, Yao H (2015). Metabolism and plasma pharmacokinetics of isoorientin, a natural active ingredient, in Sprague-Dawley male rats after oral and intravenous administration. Xenobiotica. https://pubmed.ncbi.nlm.nih.gov/26084374/
  10. Kim B, Lee KY, Park B (2021). Isoorientin inhibits amyloid β25-35-induced neuronal inflammation in BV2 cells by blocking the NF-κB signaling pathway. Molecules. https://pubmed.ncbi.nlm.nih.gov/34834150/
  11. Trettel CDS, et al. (2021). The mechanisms of calcium mobilization by procyanidins, flavonols and flavonoids from Cecropia glaziovii Snethl in pulmonary endothelial cell cultures endorse its popular use as vasodilator phytomedicine. Biomedicine & Pharmacotherapy. https://pubmed.ncbi.nlm.nih.gov/34610498/
  12. Vanegas KG, Larsen AB, Eichenberger M, Fischer D, Mortensen UH, Naesby M (2018). Indirect and direct routes to C-glycosylated flavones in Saccharomyces cerevisiae. Microbial Cell Factories. https://pubmed.ncbi.nlm.nih.gov/29986709/
  13. Wang J, Yue YD, Jiang H, Tang F (2012). Rapid screening for flavone C-glycosides in the leaves of different species of bamboo and simultaneous quantitation of four marker compounds by HPLC-UV/DAD. International Journal of Analytical Chemistry. https://pubmed.ncbi.nlm.nih.gov/22654910/