The Inhibitory Effects of the Natural Stilbene Piceatannol on Lactate Transport In Vitro Mediated by Monocarboxylate Transporters

IF 4.5 2区农林科学 Q1 FOOD SCIENCE & TECHNOLOGY Molecular Nutrition & Food Research Pub Date : 2024-09-29 DOI:10.1002/mnfr.202400414

Andrés P. Ibacache-Chía, Jimena A. Sierralta, Andreas Schüller

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Abstract

Scope

Lactate, a signaling molecule and energy source, crosses membranes through monocarboxylate transporters (MCTs). MCT1 and MCT4 are potential cancer drug targets due to their role in metabolic reprogramming of cancer cells. Stilbenes, plant secondary metabolites found in several food sources, have anticancer effects, though their mechanisms of action are not well understood. This study links the anticancer activity of natural stilbenes to tumor cell lactate metabolism.

Methods and results

The impact of resveratrol, pinostilbene, pterostilbene, rhapontigenin, and piceatannol on lactate transport is studied using a fluorescence resonance energy transfer (FRET)-based lactate sensor. The viability and migration of cells expressing MCT1 or MCT4 are also evaluated. Piceatannol inhibits MCT1 effectively at low micromolar concentrations, with less effect on MCT4. All stilbenes significantly reduce cell viability and migration.

Conclusions

These findings indicate that both MCTs are stilbene targets, with piceatannol highlighted as a cost-effective, low-toxicity compound for studying MCTs in cancer, providing a new mechanism of action of the therapeutic and nutraceutical effects of natural polyphenols. This enriches the understanding of dietary polyphenols in cancer prevention and therapy.

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天然二苯乙烯皮夏单宁对单羧酸盐转运体介导的体外乳酸盐转运的抑制作用

乳酸盐是一种信号分子和能量来源，通过单羧酸盐转运体（MCTs）穿过细胞膜。MCT1 和 MCT4 是潜在的抗癌药物靶点，因为它们在癌细胞的代谢重编程中发挥作用。二苯乙烯是存在于多种食物中的植物次生代谢产物，具有抗癌作用，但其作用机制尚不十分清楚。这项研究将天然二苯乙烯类化合物的抗癌活性与肿瘤细胞的乳酸代谢联系起来。

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来源期刊

Molecular Nutrition & Food Research 工程技术-食品科技

CiteScore

8.70

自引率

1.90%

发文量

250

审稿时长

1.7 months

期刊介绍： Molecular Nutrition & Food Research is a primary research journal devoted to health, safety and all aspects of molecular nutrition such as nutritional biochemistry, nutrigenomics and metabolomics aiming to link the information arising from related disciplines: Bioactivity: Nutritional and medical effects of food constituents including bioavailability and kinetics. Immunology: Understanding the interactions of food and the immune system. Microbiology: Food spoilage, food pathogens, chemical and physical approaches of fermented foods and novel microbial processes. Chemistry: Isolation and analysis of bioactive food ingredients while considering environmental aspects.