Absorption of kaempferol from endive, a source of kaempferol-3-glucuronide, in humans

Abstract

Objective: To determine the absorption, excretion and metabolism of kaempferol in humans. Design: A pharmacokinetic study of kaempferol from endive over 24 h. Subjects: Four healthy males and four healthy females. Results: Kaempferol, from a relatively low dose (9 mg), was absorbed from endive with a mean maximum plasma concentration of 0.1 mM, at a time of 5.8 h, indicating absorption from the distal section of the small intestine and/or the colon. Although a 7.5-fold interindividual variation between the highest and lowest maximum plasma concentration was observed, most individuals showed remarkably consistent pharmacokinetic profiles. This contrasts with profiles for other flavonoids that are absorbed predominantly from the large intestine (eg rutin). An average of 1.9% of the kaempferol dose was excreted in 24 h. Most subjects also showed an early absorption peak, probably corresponding to kaempferol-3-glucoside, present at a level of 14% in the endive. Kaempferol-3-glucuronide was the major compound detected in plasma and urine. Quercetin was not detected in plasma or urine indicating a lack of phase I hydroxylation of kaempferol. Conclusions: Kaempferol is absorbed more efficiently than quercetin in humans even at low oral doses. The predominant form in plasma is a 3-glucuronide conjugate, and interindividual variation in absorption and excretion is low, suggesting that urinary kaempferol could be used as a biomarker for exposure. Sponsorship: Biotechnology and Biological Sciences Research council for core strategic funding and the University of Leeds for a departmental fellowship (AJD).

The Small Polyphenolic Molecule Kaempferol Increases Cellular Energy Expenditure and Thyroid Hormone Activation

“…The current data are novel in that KPF is identified not only as a xenobiotic agent that could increase energy expenditure, but also one that could regulate thyroid hormone activation. However, it must be noted that the KPF concentrations that produced biologic effects seen in this study (2-20 mol/l) cannot easily be attained via dietary supplementation, since for example ingestion of ϳ9 mg KPF contained in a cup of endive soup raises serum KPF concentrations to only ϳ0.1 mol/l (34). Nevertheless, it is fascinating to speculate as to whether beneficial effects of KPF on human metabolism and thyroid hormone action could be realized if the molecule could be delivered such that plasma levels reached 2 mol/l, a concentration sufficient to substantially induce D2 activity in our studies.…”

Radiosensitization of non-small cell lung cancer by kaempferol

“…The anti-angiogenic properties of kaempferol have also been well documented (19). Among the flavonols, kaempferol is absorbed particularly well when administered orally, even in low doses, with minimal inter-individual variation (20). Kaempferol is reportedly effective against pancreatic cancer, human lung non-small carcinoma and glioma cells (21)(22)(23).…”

Development and Validation of UV Spectrophotometric Method for the Estimation of Kaempferol in Kaempferol: Hydrogenated Soy PhosphatidylCholine (HSPC) Complex

“…1 It is widely distributed in the plant kingdom such as onion, kale, endive and tea along with formed as secondary metabolites through the phenylpropenoid biosynthetic pathway. 2 Although it has broad spectrum importance, researcher have been isolated it from different plants like Asclepias cyriaca L., 3 Crocus sativus L., 4 Cassia alata L., 5 Capsella bursa-patoris L., 6 Leptadenia pyrotechnica L., 7 and broccoli 8 and also reported its various pharmacotherapeutic effects like anticancer, 7 antioxidant, 9,10 anti-infl ammatory 11 and hepatoprotective 12 etc. kaempferol revealed low to moderate absorption, which results poor bioavailability ~2%.…”