Biomolecular Sciences Research Centre, Department of Biosciences and Chemistry, Sheffield Hallam University, The Owen Building, City Campus, Howard Street, Sheffield S1 1WB, UK.
Laboratory Medicine Department, Faculty of Applied Medical Sciences, Umm Al-Qura University, P.O. Box 715, Makkah 21955, Saudi Arabia.
Int J Mol Sci. 2021 Mar 17;22(6):3085. doi: 10.3390/ijms22063085.
Leukaemia is a malignant disease of the blood. Current treatments for leukaemia are associated with serious side-effects. Plant-derived polyphenols have been identified as potent anti-cancer agents and have been shown to work synergistically with standard chemotherapy agents in leukaemia cell lines. Polyphenols have multiple mechanisms of action and have been reported to decrease cell proliferation, arrest cell cycle and induce apoptosis via the activation of caspase (3, 8 and 9); the loss of mitochondrial membrane potential and the release of cytochrome c. Polyphenols have been shown to suppress activation of transcription factors, including NF-kB and STAT3. Furthermore, polyphenols have pro-oxidant properties, with increasing evidence that polyphenols inhibit the antioxidant activity of glutathione, causing oxidative DNA damage. Polyphenols also induce autophagy-driven cancer cell death and regulate multidrug resistance proteins, and thus may be able to reverse resistance to chemotherapy agents. This review examines the molecular mechanism of action of polyphenols and discusses their potential therapeutic targets. Here, we discuss the pharmacological properties of polyphenols, including their anti-inflammatory, antioxidant, anti-proliferative, and anti-tumour activities, and suggest that polyphenols are potent natural agents that can be useful therapeutically; and discuss why data on bioavailability, toxicity and metabolism are essential to evaluate their clinical use.
白血病是一种血液恶性疾病。目前治疗白血病的方法存在严重的副作用。植物来源的多酚类化合物已被确定为有效的抗癌药物，并已被证明在白血病细胞系中与标准化疗药物具有协同作用。多酚类化合物具有多种作用机制，已被报道通过激活 caspase（3、8 和 9）减少细胞增殖、阻止细胞周期和诱导细胞凋亡；线粒体膜电位丧失和细胞色素 c 的释放。多酚类化合物已被证明可以抑制转录因子的激活，包括 NF-κB 和 STAT3。此外，多酚类化合物具有促氧化剂特性，越来越多的证据表明多酚类化合物抑制谷胱甘肽的抗氧化活性，导致氧化 DNA 损伤。多酚类化合物还诱导自噬驱动的癌细胞死亡并调节多药耐药蛋白，因此可能能够逆转对化疗药物的耐药性。这篇综述检查了多酚类化合物的分子作用机制，并讨论了它们潜在的治疗靶点。在这里，我们讨论了多酚类化合物的药理学特性，包括它们的抗炎、抗氧化、抗增殖和抗肿瘤活性，并表明多酚类化合物是有效的天然药物，在治疗上可能有用；并讨论了为什么关于生物利用度、毒性和代谢的数据对于评估其临床应用至关重要。
