Current Drug Targets

Francis J. Castellino
Kleiderer-Pezold Professor of Biochemistry
Director, W.M. Keck Center for Transgene Research
Dean Emeritus, College of Science
230 Raclin-Carmichael Hall, University of Notre Dame
Notre Dame, IN 46556


Anticarcinogenic Actions of Tributyrin, A Butyric Acid Prodrug

Author(s): Renato Heidor, Juliana Festa Ortega, Aline de Conti, Thomas Prates Ong and Fernando Salvador Moreno

Affiliation: Department of Food and Experimental Nutrition, Faculty of Pharmaceutical Sciences, University of São Paulo, 580 Prof. Lineu Prestes Avenue, Building 14, 05508-900, São Paulo, SP, Brazil.


Bioactive food compounds (BFCs) exhibit potential anticarcinogenic effects that deserve to be explored. Butyric acid (BA) is considered a promising BFC and has been used in clinical trials; however, its short half-life considerably restricts its therapeutic application. Tributyrin (TB), a BA prodrug present in milk fat and honey, has more favorable pharmacokinetic properties than BA, and its oral administration is also better tolerated. In vitro and in vivo studies have shown that TB acts on multiple anticancer cellular and molecular targets without affecting non-cancerous cells. Among the TB mechanisms of action, the induction of apoptosis and cell differentiation and the modulation of epigenetic mechanisms are notable. Due to its anticarcinogenic potential, strategies as lipid emulsions, nanoparticles, or structured lipids containing TB are currently being developed to improve its organoleptic characteristics and bioavailability. In addition, TB has minimal toxicity, making it an excellent candidate for combination therapy with other agents for the control of cancer. Despite the lack of data available in the literature, TB is a promising molecule for anticancer strategies. Therefore, additional preclinical and clinical studies should be performed using TB to elucidate its molecular targets and anticarcinogenic potential.

Keywords: Bioactive food compounds, butyrate, butyric acid, cancer, cellular targets, chemoprevention, molecular targets, tributyrin

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Article Details

Page: [1720 - 1729]
Pages: 10
DOI: 10.2174/138945012804545443
Price: $58