Identification of gut-derived metabolites of maslinic acid, a bioactive compound from Olea europaea L

Mol Nutr Food Res. 2016 Sep;60(9):2053-64. doi: 10.1002/mnfr.201501060. Epub 2016 Jun 6.

Abstract

Scope: Maslinic acid has been described to exert a chemopreventive activity in colon cancer. Hereby, we determined maslinic acid and its metabolites in the rat intestine previous oral administration as a first step in elucidating whether this triterpene might be used as a nutraceutical.

Methods and results: Maslinic acid was orally administered at 1, 2, and 5 mg/kg to male Sprague-Dawley for 2 days. At 24 h after the last administration, the content of the duodenum and jejunum, ileum, cecum, and colon was collected and extracted with methanol 80% prior to LC-APCI-MS analysis. The developed method was validated providing suitable sensitivity (LOQ of 5 nM), good recovery (97.8 ± 3.6%), linear correlation, and appropriate precision (< 9%). Maslinic acid was detected in all the segments with higher concentrations in the distal part of the intestine. LC-APCI-LTQ-ORBITRAP-MS allowed the identification of 11 gut-derived metabolites that were formed by mono-, dihydroxylation, and dehydrogenation reactions.

Conclusion: Maslinic acid undergoes phase I reactions resulting in a majority of monohydroxylated metabolites without the presence of phase II derivatives. The high concentration of maslinic acid achieved in the intestine suggests that it could exert a beneficial effect in the prevention of colon cancer.

Keywords: Intestinal metabolism; Maslinic acid; Olives; Phase I metabolites; Rat.

MeSH terms

  • Administration, Oral
  • Animals
  • Chromatography, Liquid / methods
  • Intestinal Mucosa / metabolism*
  • Intestines / drug effects
  • Limit of Detection
  • Male
  • Mass Spectrometry / methods
  • Olea / chemistry*
  • Rats, Sprague-Dawley
  • Reproducibility of Results
  • Sensitivity and Specificity
  • Triterpenes / administration & dosage
  • Triterpenes / metabolism*
  • Triterpenes / pharmacokinetics*

Substances

  • Triterpenes
  • maslinic acid