Synthesis of a novel ester of hydroxytyrosol and α-lipoic acid exhibiting an antiproliferative effect on human colon cancer HT-29 cells.
A novel ester of hydroxytyrosol and α-lipoic acid was synthesized in satisfactory yield by original and simple procedures and evaluated about its antiproliferative activity on the human colorectal adenocarcinoma HT-29 cell line. The compound exhibited a cell growth inhibitory activity significantly more potent than the corresponding parent natural compounds, very likely due to the induction of cell cycle arrest in the G2/M phase. These data suggest that the novel ester might exert a more effective antitumour activity than hydroxytyrosol and α-lipoic acid.
Dipartimento di Agrobiologia e Agrochimica, Università degli Studi della Tuscia, Via S. Camillo De Lellis snc, 01100 Viterbo, Italy. berninir@unitus.it
Roberta
R
Bernini
Fernanda
F
Crisante
Nicolò
N
Merendino
Romina
R
Molinari
Maria Chiara
MC
Soldatelli
Francesca
F
Velotti
D002453:Cell Cycle / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects; D003110:Colonic Neoplasms / Q000473:pathology*; D004952:Esters; D019073:HT29 Cells; D006801:Humans; D010626:Phenylethyl Alcohol / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D008063:Thioctic Acid / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
D004952:Esters; C005975:3,4-dihydroxyphenylethanol; D008063:Thioctic Acid; D010626:Phenylethyl Alcohol