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The role of CYP2E1 in the development of hepatocellular carcinoma (HCC), the final complication of FLD, remains controversial. Specifically, CYP2E1 has not yet been defined as a molecular target for HCC therapy. In addition, a CYP2E1\u2010specific drug has not been developed. We have already shown that our newly developed CYP2E1 inhibitor 12\u2010imidazolyl\u20101\u2010dodecanol (I\u2010ol) was therapeutically effective against alcoholic and nonalcoholic steatohepatitis. In this study, we investigated the effect of I\u2010ol on HCC tumorigenesis and whether I\u2010ol could serve as a possible treatment option for terminal\u2010stage FLD. I\u2010ol exerted a very highly significant antitumour effect against hepatocellular HepG2 cells. Cell viability was reduced in a dose\u2010dependent manner, with only the highest doses causing a cytotoxic effect associated with caspase 3\/7 activation. Comparable results were obtained for the model colorectal adenocarcinoma cell line, DLD\u20101, whose tumorigenesis is also associated with CYP2E1. Transcriptome analyses showed a clear effect of I\u2010ol on apoptosis and cell\u2010cycle regulation, with the increased expression of p27Kip1 being particularly noticeable. These observations were confirmed at the protein level for HepG2 and DLD\u20101 cells grafted on a chorioallantoic membrane. Cell\u2010cycle analysis showed a complete loss of proliferating cells with a simultaneous increase in S\u2010phase arrest beginning at a threshold dose of 30\u2009<jats:italic>\u03bc<\/jats:italic>M. I\u2010ol also reduced xenograft tumour growth in nude mice. This antitumour effect was not associated with tumour cachexia. I\u2010ol was not toxic to healthy tissues or organs. This study demonstrates for the first time the therapeutic effect of the specific CYP2E1 inhibitor I\u2010ol on the tumorigenesis of HCC. Our findings imply that I\u2010ol can potentially be applied therapeutically on patients at the final stage of FLD.<\/jats:p>","DOI":"10.1155\/2021\/8854432","type":"journal-article","created":{"date-parts":[[2021,2,2]],"date-time":"2021-02-02T21:29:31Z","timestamp":1612301371000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":8,"title":["A New CYP2E1 Inhibitor, 12\u2010Imidazolyl\u20101\u2010dodecanol, Represents a Potential Treatment for Hepatocellular 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