Hydroxytyrosyl ethyl ether exhibits stronger intestinal anticarcinogenic potency and effects on transcript profiles compared to hydroxytyrosol

► Hydroxytyrosol and hydroxytyrosyl ethyl ether alter genes related with colon cancer prevention in a dose dependent manner. ► Both polyphenols arrest cell cycle, induce apoptosis and enhance carcinogen detoxification. ► Hydroxytyrosyl ethyl ether shows more anticarcinogenic colorectal activity than...

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Published inFood chemistry Vol. 138; no. 2-3; pp. 1172 - 1182
Main Authors Pereira-Caro, G., Mateos, R., Traka, M.H., Bacon, J.R., Bongaerts, R., Sarriá, B., Bravo, L., Kroon, P.A.
Format Journal Article
LanguageEnglish
Published Kidlington Elsevier Ltd 01.06.2013
Elsevier
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Summary:► Hydroxytyrosol and hydroxytyrosyl ethyl ether alter genes related with colon cancer prevention in a dose dependent manner. ► Both polyphenols arrest cell cycle, induce apoptosis and enhance carcinogen detoxification. ► Hydroxytyrosyl ethyl ether shows more anticarcinogenic colorectal activity than its precursor, hydroxytyrosol. The anticarcinogenic activity of hydroxytyrosyl ethyl ether (HTy-Et) compared to its precursor hydroxytyrosol (HTy) has been studied in human Caco-2 colon adenocarcinoma cells. 451 and 977 genes were differentially expressed in Caco-2 cells exposed to HTy or HTy-Et for 24h, respectively, compared with untreated cells (P<0.005; FDR=0), using Affymetrix microarrays. Results showed that both HTy and HTy-Et inhibited cell proliferation and arrested the cell cycle by up-regulating p21 and CCNG2 and down-regulating CCNB1 protein expression. HTy and HTy-Et also altered the transcription of specific genes involved in apoptosis, as suggested by the up-regulation of BNIP3, BNIP3L, PDCD4 and ATF3 and the activation of caspase-3. Moreover, these polyphenols up-regulated xenobiotic metabolizing enzymes UGT1A10 and CYP1A1, enhancing carcinogen detoxification. In conclusion, these results highlight that HTy and its derivative HTy-Et modulate molecular mechanisms involved in colon cancer, with HTy-Et being more effective than HTy.
ISSN:0308-8146
1873-7072
DOI:10.1016/j.foodchem.2012.11.118