title: Lipophilization of Hydroxytyrosol-Enriched Fractions from Olea europaea L. Byproducts and Evaluation of the in Vitro Effects on a Model of Colorectal Cancer Cells.
abstract: A hydroxytyrosol (HTyr)-enriched fraction containing HTyr 6% w/w, derived from Olea europaea L. byproducts and obtained using an environmentally and economically sustainable technology, was lipophilized under green chemistry conditions. The effects of three fractions containing hydroxytyrosyl butanoate, octanoate, and oleate, named, respectively, lipophilic fractions 5, 6, and 7, and unreacted HTyr on the human colon cancer cell line HCT8-β8 engineered to overexpress estrogen receptor β (ERβ) were evaluated and compared to those of pure HTyr. The experimental data demonstrated that HTyr and all fractions showed an antiproliferative effect, as had been observed by the evaluation of the cellular doubling time under these different conditions (mean control, 32 ± 4 h; HTyr 1, 65 ± 9 h; fraction 5, 64 ± 11 h; fraction 6, 62 ± 14 h; fraction 7, 133 ± 30 h). As evidenced, fraction 7 containing hydroxytyrosyl oleate showed the highest activity. These results were related to the link with ER-β, which was assessed through simultaneous treatment with an inhibitor of ERβ.
authors.affiliation: Department of Agricultural and Forestry Sciences (DAFNE), University of Tuscia , Via S. Camillo de Lellis, 01100 Viterbo, Italy.
authors.forename: Roberta
authors.identifier: http://orcid.org/0000-0002-2548-3876
authors.initials: R
authors.lastname: Bernini
authors.affiliation: Department of Agricultural and Forestry Sciences (DAFNE), University of Tuscia , Via S. Camillo de Lellis, 01100 Viterbo, Italy.
authors.forename: Isabella
authors.initials: I
authors.lastname: Carastro
authors.affiliation: Department of Surgery and Translational Medicine, University of Florence , 50134 Florence, Italy.
authors.forename: Gaia
authors.initials: G
authors.lastname: Palmini
authors.affiliation: Department of Surgery and Translational Medicine, University of Florence , 50134 Florence, Italy.
authors.forename: Annalisa
authors.initials: A
authors.lastname: Tanini
authors.affiliation: Department of Surgery and Translational Medicine, University of Florence , 50134 Florence, Italy.
authors.forename: Roberto
authors.initials: R
authors.lastname: Zonefrati
authors.affiliation: Department of Statistics, Computing, Applications "G. Parenti" (DISIA), PHYTOLAB, University of Florence , 50134 Florence, Italy.
authors.forename: Patrizia
authors.initials: P
authors.lastname: Pinelli
authors.affiliation: Department of Surgery and Translational Medicine, University of Florence , 50134 Florence, Italy.
authors.forename: Maria Luisa
authors.initials: ML
authors.lastname: Brandi
authors.affiliation: Department of Statistics, Computing, Applications "G. Parenti" (DISIA), PHYTOLAB, University of Florence , 50134 Florence, Italy.
authors.forename: Annalisa
authors.initials: A
authors.lastname: Romani
mesh_terms: D045744:Cell Line, Tumor; D015179:Colorectal Neoplasms / Q000503:physiopathology; D047629:Estrogen Receptor beta / Q000235:genetics / Q000378:metabolism; D006801:Humans; D015394:Molecular Structure; D031658:Olea / Q000737:chemistry*; D010626:Phenylethyl Alcohol / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology*; D014866:Waste Products / Q000032:analysis*
chemical_list: D047629:Estrogen Receptor beta; D010936:Plant Extracts; D014866:Waste Products; C005975:3,4-dihydroxyphenylethanol; D010626:Phenylethyl Alcohol
keywords: Olea europaea L. byproducts; colorectal cancer (CRC); hydroxytyrosol (HTyr); hydroxytyrosyl esters; lipophilization of extracts