Does Oral Apigenin Have Real Potential for a Therapeutic Effect in the Context of Human Gastrointestinal and Other Cancers?

Eva F. DeRango-Adem, Jonathan Blay

Résultat de recherche: Review articleexamen par les pairs

80 Citations (Scopus)

Résumé

Apigenin (4′, 5, 7-trihydroxyflavone) is a plant flavone that has been found to have various actions against cancer cells. We evaluated available evidence to determine whether it is feasible for apigenin to have such effects in human patients. Apigenin taken orally is systemically absorbed and recirculated by enterohepatic and local intestinal pathways. Its bioavailability is in the region of 30%. Once absorbed from the oral route it reaches maximal circulating concentration (Cmax) after a time (Tmax) of 0.5–2.5h, with an elimination half-life (T1/2) averaging 2.52 ± 0.56h. Using a circulating concentration for efficacy of 1–5μmol/L as the target, we evaluated data from both human and rodent pharmacokinetic studies to determine if a therapeutic concentration would be feasible. We find that oral intake of dietary materials would require heroic ingestion amounts and is not feasible. However, use of supplements of semi-purified apigenin in capsule form could reach target blood levels using amounts that are within the range currently acceptable for other supplements and medications. Modified formulations or parenteral injection are suitable but may not be necessary. Further work with direct studies of pharmacokinetics and clinical outcomes are necessary to fully evaluate whether apigenin will contribute to a useful clinical strategy, but given emerging evidence that it may interact beneficially with chemotherapeutic drugs, this is worthy of emphasis. In addition, more effective access to intestinal tissues from the oral route raises the possibility that apigenin may be of particular relevance to gastrointestinal disorders including colorectal cancer.

Langue d'origineEnglish
Numéro d'article681477
JournalFrontiers in Pharmacology
Volume12
DOI
Statut de publicationPublished - mai 18 2021

Note bibliographique

Funding Information:
We thank B. Diaconu for assisting with early collection of references. JB is a Senior Scientist of the BHCRI.

Publisher Copyright:
© Copyright © 2021 DeRango-Adem and Blay.

ASJC Scopus Subject Areas

  • Pharmacology
  • Pharmacology (medical)

PubMed: MeSH publication types

  • Journal Article
  • Review

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