Department of Molecular Genetics, Faculty of Biology and Environmental Protection, University of Lodz, Pomorska 141/143, 90-236 Lodz, Poland.
Doctoral School of Exact and Natural Sciences, University of Lodz, Banacha 12/16, 90-237 Lodz, Poland.
Int J Mol Sci. 2024 Oct 26;25(21):11500. doi: 10.3390/ijms252111500.
Cancer is one of the most common causes of death in the world. Despite the fact that there are many types of therapies available, cancer treatment remains a major challenge. The main reason for the ineffectiveness of chemotherapy is the acquisition of multidrug resistance (MDR) by cancer cells. One of the factors responsible for the acquisition of MDR is the NRF2 transcription factor, which regulates the expression of proteins such as , , MRP1, MRP2, and GST. In normal cells, NRF2 is the first line of defense against oxidative stress, thereby preventing carcinogenesis. Still, its hyperactivation in cancer cells causes them to acquire MDR, which significantly reduces or eliminates the effectiveness of chemotherapy. Considering the important role NRF2 plays in the acquisition of MDR, its modulators and, above all, inhibitors are being sought after, including among compounds of plant origin. NRF2 inhibition may prove to be a key element of anticancer therapy. This review summarizes the current state of knowledge about plant NRF2 inhibitors and presents the effects of their use in overcoming MDR in cancer.
癌症是世界上最常见的死亡原因之一。尽管有许多种治疗方法可用，但癌症治疗仍然是一个主要的挑战。化疗无效的主要原因是癌细胞获得了多药耐药性（MDR）。导致 MDR 获得的因素之一是 NRF2 转录因子，它调节如 GST、MRP1、MRP2 和 等蛋白质的表达。在正常细胞中，NRF2 是抵御氧化应激的第一道防线，从而防止致癌作用。然而，其在癌细胞中的过度激活导致它们获得 MDR，这大大降低或消除了化疗的有效性。鉴于 NRF2 在获得 MDR 中发挥的重要作用，正在寻找其调节剂，尤其是抑制剂，包括植物来源的化合物。NRF2 抑制可能被证明是抗癌治疗的关键因素。本文综述了目前关于植物 NRF2 抑制剂的知识状况，并介绍了它们在克服癌症 MDR 中的应用效果。
