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Sunday, 24 May 2015

A bioguided identification of the active compounds that contribute to the antiproliferative/cytotoxic effects of rosemary extract on colon cancer cells

Volume 80, June 2015, Pages 215–222

A bioguided identification of the active compounds that contribute to the antiproliferative/cytotoxic effects of rosemary extract on colon cancer cells


Highlights

Rosemary extracts show cytotoxic effects in cancer cell models but their active compounds are yet to be discovered.
Bioguided fractionation of rosemary extract was achieved by preparative HPLC and fractions characterized by HPLC-ESI-QTOF-MS.
Carnosic acid, carnosol, 12-methoxycarnosic acid, taxodione, hinokione and betulinic acid are the most active compounds.
Comparative antiproliferative study on the fractions and the whole extract revealed potential synergistic effects.
The antiproliferative or cytotoxic mechanism deserves further attention.

Abstract

Rosemary extracts have exhibited potential cytostatic or cytotoxic effects in several cancer cell models but their bioactive compounds are yet to be discovered. In this work, the anticancer activity of a rosemary-leaf extract and its fractions were assayed to identify the phenolic compounds responsible for their antiproliferative/cytotoxic effects on a panel of human colon cancer cell lines. Bioguided fractionation of the rosemary-leaf extract was achieved by semi-preparative chromatography. The rosemary extract and the compounds in the fractions were characterized and quantified by HPLC-ESI-QTOF-MS. Cellular viability in the presence of these fractions and the whole extract was determined after 24 or 48 h incubations by using an MTT assay. Fractions containing diterpenes or triterpenes were the most active but not as much as the whole extract. In conclusion, carnosic acid, carnosol, 12-methoxycarnosic acid, taxodione, hinokione and betulinic acid were the putative candidates that contributed to the observed antiproliferative activity of rosemary in human colon cancer cells. Whether the effects of the extract and fractions are only cytostatic or cytotoxic needs to be elucidated. Nevertheless, the comparative antiproliferative study on the fractions and whole extract revealed potential synergistic effects between several components in the extract that may deserve further attention.

Keywords

  • Antiproliferative activity;
  • Cytotoxicity;
  • Colon cancer;
  • HPLC-ESI-QTOF-MS;
  • Rosemary;
  • Terpenoids

Corresponding author. Department of Analytical Chemistry, Faculty of Sciences, University of Granada, Avda Fuentenueva s/n, 18071, Granada, Spain. Tel.: +34958248409; fax: +34958243328.
1
These authors contributed equally to this work.
2
These authors share co-senior authorship.