Absorption and Metabolism of Luteolin in Rats and Humans in Relation to in Vitro Anti-inflammatory Effects

Natsumi Hayasaka, Naoki Shimizu, Toshikazu Komoda, Satoshi Mohri, Tojiro Tsushida, Takahiro Eitsuka, Teruo Miyazawa, Kiyotaka Nakagawa

Research output: Contribution to journalArticlepeer-review

50 Citations (Scopus)


Luteolin is a flavonoid present in plants in the form of aglycone or glucosides. In this study, luteolin glucosides (i.e., luteolin-7-O-β-d-glucoside, luteolin-7-O-[2-(β-d-apiosyl)-β-d-glucoside], and luteolin-7-O-[2-(β-d-apiosyl)-6-malonyl-β-d-glucoside]) prepared from green pepper leaves as well as luteolin aglycone were orally administered to rats. Regardless of the administered luteolin form, luteolin glucuronides were mainly detected from plasma and organs. Subsequently, luteolin aglycone, the most absorbed form of luteolin in rats, was orally administered to humans. As a result, luteolin-3′-O-sulfate was mainly identified from plasma, suggesting that not only luteolin form but also animal species affect the absorption and metabolism of luteolin. When LPS-treated RAW264.7 cells were treated with luteolin glucuronides and luteolin sulfate (the characteristic metabolites identified from rats and humans, respectively), the different luteolin conjugates were metabolized in different ways, suggesting that such difference in metabolism results in their difference in anti-inflammatory effects.

Original languageEnglish
Pages (from-to)11320-11329
Number of pages10
JournalJournal of Agricultural and Food Chemistry
Issue number43
Publication statusPublished - 2018 Oct 31


  • anti-inflammatory effects
  • luteolin aglycone
  • luteolin glucuronide
  • luteolin sulfate
  • metabolism


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