Laboratory of Diet, Nutrition and Cancer, Department of Food and Experimental Nutrition, Faculty of Pharmaceutical Sciences, University of São Paulo, Brazil.
Curr Drug Targets. 2012 Dec;13(14):1720-9. doi: 10.2174/138945012804545443.
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.
生物活性食物化合物（BFCs）具有潜在的抗癌作用，值得进一步研究。丁酸（BA）被认为是一种很有前途的 BFC，已被用于临床试验；然而，其半衰期短极大地限制了其治疗应用。三丁酸甘油酯（TB）是一种存在于乳脂和蜂蜜中的 BA 前体药物，具有比 BA 更理想的药代动力学特性，其口服给药也更容易耐受。体外和体内研究表明，TB 通过多种抗癌细胞和分子靶点发挥作用，而不影响非癌细胞。在 TB 的作用机制中，诱导细胞凋亡和分化以及调节表观遗传机制值得注意。由于其抗癌潜力，目前正在开发包含 TB 的脂质乳剂、纳米粒子或结构化脂质等策略，以改善其感官特性和生物利用度。此外，TB 毒性极小，使其成为与其他药物联合治疗癌症的理想候选药物。尽管文献中缺乏相关数据，但 TB 是一种很有前途的抗癌策略分子。因此，应该使用 TB 进行更多的临床前和临床研究，以阐明其分子靶点和抗癌潜力。
