The Sunlight Experiment

Compound Monograph

Kaempferitrin

Kaempferitrin is kaempferol-3,7-O-α-L-dirhamnoside (synonym lespedin) — a flavonol diglycoside of epazote, Justicia and many plants. No human trial of the isolate exists; its evidence is a small preclinical set led by a genuine insulin-mimetic antidiabetic signal (it stimulates glucose uptake in skeletal muscle and is hypoglycaemic in diabetic rodents), with anti-inflammatory and antioxidant data. Poorly absorbed and hydrolysed toward kaempferol in the gut.

Work in progress

Where Does It Come From? (5)

Kaempferitrin is a naturally occurring flavonol glycoside (kaempferol-3,7-o-α-l-dirhamnoside), found in Epazote and 4 other sources. It is well tolerated orally (low toxicity).

Bauhinia forficata Epazote Dysphania ambrosioides Justicia spicigeraKenafSedum dendroideum

Pharmacology & Research

Kaempferitrin is the 3,7-dirhamnoside of kaempferol (synonym lespedin, an identity established in 1951 13Reference 131951Identity of lespedin with kaempferitrinView study →) — a sibling of the monoglucoside astragalin, from which it differs by carrying a second (7-position) sugar and swapping glucose for rhamnose (twice). Its evidence is a small, multi-lab preclinical literature clustered on one genuinely distinctive signal: an insulin-mimetic antidiabetic effect. Unlike most flavonol glycosides, kaempferitrin shows an intact-molecule action in muscle — so it is not purely a kaempferol prodrug — although its poor absorption and gut-flora hydrolysis toward kaempferol still make chronic oral benefit bioavailability-limited. No human trials of the isolate exist.

What the evidence supports
  • A genuine, somewhat kaempferitrin-specific antidiabetic signal: the intact molecule stimulates glucose uptake in skeletal muscle and adipocyte insulin signalling, and is hypoglycaemic in diabetic rodents 1,3,2Reference 12004AnimalInsulinomimetic effects of kaempferitrin on glycaemia and on ¹⁴C-glucose uptake in rat soleus muscleView study →Reference 32009Kaempferitrin activates the insulin signalling pathway and stimulates secretion of adiponectin in 3T3-L1 adipocytesView study →Reference 22004Hypoglycemic effect and antioxidant potential of kaempferol-3,7-O-(α)-dirhamnoside from Bauhinia forficata leavesView study →.
  • The honest headline: no human trials; the glucose-uptake data are tissue-divergent (muscle up, one adipocyte study down), and the anti-inflammatory/antioxidant signals are largely shared with the kaempferol class 4Reference 42009Kaempferitrin inhibits GLUT4 translocation and glucose uptake in 3T3-L1 adipocytesView study →.
Evidence by indicationStrength of support
Antidiabetic / Insulin-MimeticShaky
40%
Anti-InflammatoryShaky
28%
AntioxidantShaky
24%
Antitumour / HepatoprotectiveUnsupported
16%
1. Antidiabetic / insulin-mimetic

The most-developed and most kaempferitrin-specific activity. Kaempferitrin acutely stimulates ¹⁴C-glucose uptake in rat soleus (skeletal) muscle in an insulin-mimetic, insulin-signalling-dependent manner 1Reference 12004AnimalInsulinomimetic effects of kaempferitrin on glycaemia and on ¹⁴C-glucose uptake in rat soleus muscleView study →, activates insulin signalling and adiponectin secretion in adipocytes 3Reference 32009Kaempferitrin activates the insulin signalling pathway and stimulates secretion of adiponectin in 3T3-L1 adipocytesView study →, drives glucose uptake in skeletal muscle 5Reference 52013Insulin signalling: a potential pathway for the stimulatory effect of kaempferitrin on glucose uptake in skeletal muscleView study →, and in mice modulated hepatic AMPK phosphorylation and lowered PEPCK (gluconeogenesis) after a high-fat/high-sucrose diet 6Reference 62026AnimalKaempferitrin modulates AMPK phosphorylation and PEPCK expression in the liver after a short-term high-fat, high-sucrose diet in miceView study →; the classic in-vivo anchor is a hypoglycaemic + antioxidant effect in diabetic rats for the isolated dirhamnoside from Bauhinia forficata 2Reference 22004Hypoglycemic effect and antioxidant potential of kaempferol-3,7-O-(α)-dirhamnoside from Bauhinia forficata leavesView study →.

Gap: all preclinical, and tissue-divergent — one adipocyte study reports kaempferitrin inhibits GLUT4 translocation and glucose uptake 4Reference 42009Kaempferitrin inhibits GLUT4 translocation and glucose uptake in 3T3-L1 adipocytesView study →, conflicting with the muscle picture, with no standardised dose-response and no human trial 1,4Reference 12004AnimalInsulinomimetic effects of kaempferitrin on glycaemia and on ¹⁴C-glucose uptake in rat soleus muscleView study →Reference 42009Kaempferitrin inhibits GLUT4 translocation and glucose uptake in 3T3-L1 adipocytesView study →.

2. Anti-inflammatory

Kaempferitrin shows consistent NF-κB restraint across unrelated models: it attenuated LPS-induced septic acute lung injury 7Reference 72023AnimalKaempferitrin alleviates LPS-induced septic acute lung injury in mice through downregulating the NF-κB pathwayView study →, inhibited proliferation and inflammation in rheumatoid-arthritis synoviocytes 8Reference 82019Kaempferitrin inhibits proliferation, induces apoptosis and ameliorates inflammation in rheumatoid-arthritis fibroblast-like synoviocytesView study →, and reduced renal inflammation and fibrosis by inhibiting NOX4-mediated tubular ferroptosis 9Reference 92024Kaempferitrin attenuates unilateral-ureteral-obstruction-induced renal inflammation and fibrosis by inhibiting NOX4-mediated tubular ferroptosisView study →.

Gap: three single-model rodent/cell studies, with no replication or human data, largely shared with the kaempferol/flavonol class 7,8Reference 72023AnimalKaempferitrin alleviates LPS-induced septic acute lung injury in mice through downregulating the NF-κB pathwayView study →Reference 82019Kaempferitrin inhibits proliferation, induces apoptosis and ameliorates inflammation in rheumatoid-arthritis fibroblast-like synoviocytesView study →.

3. Antioxidant

Kaempferitrin’s antioxidant activity overlaps its antidiabetic story: radical scavenging linked to hypoglycaemia in diabetic rats 2Reference 22004Hypoglycemic effect and antioxidant potential of kaempferol-3,7-O-(α)-dirhamnoside from Bauhinia forficata leavesView study → and protection of mesangial cells from advanced-glycation-end-product-induced apoptosis and oxidative stress 14Reference 142018Protective effects of kaempferitrin on advanced-glycation-end-product-induced mesangial-cell apoptosis and oxidative stressView study →.

Gap: class-level flavonol antioxidant behaviour in narrow models, not distinctively kaempferitrin 2,14Reference 22004Hypoglycemic effect and antioxidant potential of kaempferol-3,7-O-(α)-dirhamnoside from Bauhinia forficata leavesView study →Reference 142018Protective effects of kaempferitrin on advanced-glycation-end-product-induced mesangial-cell apoptosis and oxidative stressView study →.

4. Antitumour / hepatoprotective

Kaempferitrin induces intrinsic apoptosis in HeLa cells 10Reference 102013Kaempferitrin induces apoptosis via the intrinsic pathway in HeLa cellsView study →, and as the major compound of an epazote ethanol extract it produced antitumour and hepatoprotective effects in a human-liver-cancer mouse xenograft without hepatotoxicity 11Reference 112023AnimalKaempferitrin, a major compound from the ethanol extract of Chenopodium ambrosioides (epazote), exerts antitumour and hepatoprotective effects in mice with human liver-cancer xenograftsView study →.

Gap: heterogeneous and exploratory — single studies at the isolate or extract level, with no translational follow-up 10,11Reference 102013Kaempferitrin induces apoptosis via the intrinsic pathway in HeLa cellsView study →Reference 112023AnimalKaempferitrin, a major compound from the ethanol extract of Chenopodium ambrosioides (epazote), exerts antitumour and hepatoprotective effects in mice with human liver-cancer xenograftsView study →.

Mechanisms

Target / pathwayEffectRelevant to
Skeletal-muscle glucose uptake (insulin-mimetic)↑ uptake, insulin-signalling-dependentantidiabetic
Insulin signalling (IR → PI3K/Akt) + adiponectinpathway activated; ↑ adiponectinantidiabetic
GLUT4 translocationtissue-divergent — muscle uptake up, but inhibited in one adipocyte studyantidiabetic (nuance/contradiction)
Hepatic AMPK / PEPCK↑ AMPK, ↓ PEPCK → ↓ gluconeogenesisantidiabetic (in vivo)
NF-κB; NOX4 → tubular ferroptosissuppressed; inhibitedanti-inflammatory / antioxidant
ROS / AGE-induced oxidative stressreduceddiabetic-complication protection
Intrinsic (mitochondrial) apoptosispro-apoptotic in tumour cellsantitumour

Pharmacokinetics

No dedicated human pharmacokinetics exists. As a flavonol 3,7-di-O-rhamnoside, kaempferitrin is a poorly absorbed, high-polarity diglycoside: the two rhamnose units block passive uptake, and human intestinal flora biotransform it by stepwise deglycosylation (loss of rhamnose → monorhamnoside intermediates → the aglycone kaempferol), which is then conjugated 12Reference 122005The biotransformation of kaempferitrin by human intestinal floraView study →. The net result is low, non-sustained systemic exposure to the intact parent, and a meaningful fraction of chronic in-vivo activity should be read as kaempferol-equivalent exposure (see kaempferol). The important nuance: the acute insulin-mimetic muscle effects are reported for the intact molecule in ex-vivo/cell systems, so the antidiabetic mechanism is not purely a kaempferol proxy — but oral, whole-animal benefit is bioavailability-limited.

Clinical trials

There are no randomised or open-label human trials of isolated kaempferitrin for any indication; human relevance is limited to dietary/traditional intake within kaempferitrin-bearing plants (epazote, Justicia spicigera, Bauhinia forficata).

CompletedPlannedTerminatedPreclinical
—(none, isolate)——Small multi-lab set (antidiabetic-led)

Last checked: July 2026.

Toxicity & Safety

Kaempferitrin is a dietary flavonol glycoside in food and medicinal plants, used across preclinical studies as a protective or benign agent with no dietary harm signal — consistent with a [low] flag; notably, the epazote-extract xenograft study reported antitumour efficacy without hepatotoxicity 11Reference 112023AnimalKaempferitrin, a major compound from the ethanol extract of Chenopodium ambrosioides (epazote), exerts antitumour and hepatoprotective effects in mice with human liver-cancer xenograftsView study →. There is no isolate toxicology, genotoxicity or human safety dataset, and cautions are theoretical and generic to concentrated polyphenol supplements (possible additive effects with antiplatelet/anticoagulant therapy). One specific pharmacodynamic caution: given the insulin-mimetic/glucose-lowering signal, additive hypoglycaemia with antidiabetic drugs is plausible in theory though unquantified in humans.

Pregnancy & lactation

Dietary amounts fine; avoid isolated supplements. Kaempferitrin as naturally present in foods and herbs is considered fine, but an isolated or concentrated supplement should be avoided in pregnancy and lactation — there are no human or reproductive-safety data for the isolate.

Dosage

There is no efficacy dose established (no human trials) and no standard supplemental dose — kaempferitrin is obtained incidentally through diet and herbal preparations rather than dosed on its own, and any oral efficacy target is undercut by its poor absorption and gut-flora hydrolysis to kaempferol, so a meaningful “kaempferitrin dose” cannot honestly be stated.

References

  1. (2004). Insulinomimetic effects of kaempferitrin on glycaemia and on ¹⁴C-glucose uptake in rat soleus muscle. Chemico-Biological Interactions. https://pubmed.ncbi.nlm.nih.gov/15501431/
  2. (2004). Hypoglycemic effect and antioxidant potential of kaempferol-3,7-O-(α)-dirhamnoside from Bauhinia forficata leaves. Journal of Natural Products. https://pubmed.ncbi.nlm.nih.gov/15165145/
  3. (2009). Kaempferitrin activates the insulin signalling pathway and stimulates secretion of adiponectin in 3T3-L1 adipocytes. European Journal of Pharmacology. https://pubmed.ncbi.nlm.nih.gov/19326566/
  4. (2009). Kaempferitrin inhibits GLUT4 translocation and glucose uptake in 3T3-L1 adipocytes. Biochemical and Biophysical Research Communications. https://pubmed.ncbi.nlm.nih.gov/19146827/
  5. (2013). Insulin signalling: a potential pathway for the stimulatory effect of kaempferitrin on glucose uptake in skeletal muscle. European Journal of Pharmacology. https://pubmed.ncbi.nlm.nih.gov/23458067/
  6. (2026). Kaempferitrin modulates AMPK phosphorylation and PEPCK expression in the liver after a short-term high-fat, high-sucrose diet in mice. Nutrition and Health. https://pubmed.ncbi.nlm.nih.gov/40390681/
  7. (2023). Kaempferitrin alleviates LPS-induced septic acute lung injury in mice through downregulating the NF-κB pathway. Allergologia et Immunopathologia. https://pubmed.ncbi.nlm.nih.gov/37937489/
  8. (2019). Kaempferitrin inhibits proliferation, induces apoptosis and ameliorates inflammation in rheumatoid-arthritis fibroblast-like synoviocytes. Phytotherapy Research. https://pubmed.ncbi.nlm.nih.gov/31155798/
  9. (2024). Kaempferitrin attenuates unilateral-ureteral-obstruction-induced renal inflammation and fibrosis by inhibiting NOX4-mediated tubular ferroptosis. Phytotherapy Research. https://pubmed.ncbi.nlm.nih.gov/38487990/
  10. (2013). Kaempferitrin induces apoptosis via the intrinsic pathway in HeLa cells. Journal of Ethnopharmacology. https://pubmed.ncbi.nlm.nih.gov/23211658/
  11. (2023). Kaempferitrin, a major compound from the ethanol extract of Chenopodium ambrosioides (epazote), exerts antitumour and hepatoprotective effects in mice with human liver-cancer xenografts. Journal of Pharmacy and Pharmacology. https://pubmed.ncbi.nlm.nih.gov/37203217/
  12. (2005). The biotransformation of kaempferitrin by human intestinal flora. Acta Pharmaceutica Sinica. https://pubmed.ncbi.nlm.nih.gov/16268506/
  13. (1951). Identity of lespedin with kaempferitrin. Nature. https://pubmed.ncbi.nlm.nih.gov/14882347/
  14. (2018). Protective effects of kaempferitrin on advanced-glycation-end-product-induced mesangial-cell apoptosis and oxidative stress. International Journal of Molecular Sciences. https://pubmed.ncbi.nlm.nih.gov/30373106/