Intestinal absorption of luteolin and luteolin 7‐O‐β‐glucoside in rats and humans

  title={Intestinal absorption of luteolin and luteolin 7‐O‐$\beta$‐glucoside in rats and humans},
  author={Kayoko Shimoi and Hisae Okada and Michiyo Furugori and Toshinao Goda and Sachiko Takase and Masayuki Suzuki and Yukihiko Hara and Hiroyo Yamamoto and Naohide Kinae},
  journal={FEBS Letters},

Metabolic Fate of Luteolin in Rats: Its Relationship to Anti-inflammatory Effect.

Luteolin glucuronides, especially luteolin-7-O-glucuronide, reduced expression of inflammatory genes in the cells, although their effects were weaker than those of luteolins, indicating that the active compound responsible for the anti-inflammatory effect of lutenolin in vivo would be lutesin glucuronide and/or residual luteolo.

Absorption and Metabolism of Luteolin and Its Glycosides from the Extract of Chrysanthemum morifolium Flowers in Rats and Caco-2 Cells.

It is suggested that luteolin and lutingolin monoglucoside are rapidly absorbed after administration of C. morifolium flower extract and that lutenolin, luteol monoglUCoside, and luteolini monoglucauronide may circulate in humans.

Pharmacokinetics of Luteolin and Metabolites in Rats

Luteolin was found to have a large volume of distribution and a high clearance, suggesting enterohepatic recirculation, and its glucuronide/sulfate conjugates were found to be subdivided into a distribution phase and a slow elimination phase for oral and intravenous administration.

Isolation of Luteolin and Luteolin-7-O-glucoside from Dendranthema morifolium Ramat Tzvel and Their Pharmacokinetics in Rats.

Luteolin-7-O-glucoside is primarily hydrolyzed to luteolin in the gastrointestinal tract and then absorbed into the systemic circulation and the pharmacokinetic data demonstrate that the areas under the concentration curves (AUCs) of lutenolin were 261 ± 33 and 611 ± 89 after luteol administration.

Deglucuronidation of a flavonoid, luteolin monoglucuronide, during inflammation.

  • K. ShimoiN. Saka N. Kinae
  • Biology, Medicine
    Drug metabolism and disposition: the biological fate of chemicals
  • 2001
The results suggest that during inflammation beta-glucuronidase is released from stimulated neutrophils or certain injured cells and then deglucuronidation of flavonoids occurs.

Metabolic Disposition of Luteolin Is Mediated by the Interplay of UDP-Glucuronosyltransferases and Catechol-O-Methyltransferases in Rats

Two pathways mediated by the interplay of UGTs and COMTs are probably involved in the metabolic disposition of luteolin, including glucuronidation and methylation.

Role of Catechol-O-Methyltransferase in the Disposition of Luteolin in Rats

The results indicated that the methylation pathway in rats was significantly reduced when luteolin was coadministered with a specific COMT inhibitor, and COMT-associated drug-drug interactions need be considered in the future in lutingolin clinical trials because the plasma concentrations and related therapeutic effects may be altered in vivo in the presence of a COMT inhibitors.



In vivo and in vitro glucuronidation of the flavonoid diosmetin in rats.

Evidence is brought that diosmetin is rapidly glucuronoconjugated in the rat and provides an explanation for the low po bioavailability of the unchanged compound that can be generalized to this important class of natural compounds.

Absorption and excretion of the soy isoflavone genistein in rats.

The results suggest that the extent of absorption of genistein is similar for the glycone and aglycone forms, and that similar long-term concentrations exist for both forms of isoflavone.

Quercetin metabolites in plasma of rats fed diets containing rutin or quercetin.

The results show that dietary flavonol are recovered in rat plasma as conjugated metabolites in non-negligible concentrations, and that these flavonols may be interesting antioxidant micronutrients with a variety of biological effects.

Absorption of dietary quercetin glycosides and quercetin in healthy ileostomy volunteers.

It is concluded that humans absorb appreciable amounts of quercetin and that absorption is enhanced by conjugation with glucose.

Protection by αG‐Rutin, a Water‐soluble Antioxidant Flavonoid, against Renal Damage in Mice Treated with Ferric Nitrilotriacetate

Results suggest that absorbed äG‐Rutin works as an antioxidant in vivo either by scavenging reactive oxygen species or by chelating ferric ions and this serves to prevent oxidative renal damage in mice treated with Fe‐NTA.

Luteolin: A Strong Antimutagen against Dietary Carcinogen, Trp-P-2, in Peppermint, Sage, and Thyme

Results revealed that luteolin contributed greatly to the antimutagenicity against Trp-P-2 in these herbs, and other common phytochemicals, α-tocopherol, carotenoids, xanthophylls, sterols, and saponins, were almost nonactive.