Safe Stephen, Jayaraman Arul, Chapkin Robert S, Howard Marcell, Mohankumar Kumaravel, Shrestha Rupesh
Department of Veterinary Physiology and Pharmacology, Texas A&M University, 4466 TAMU, College Station, TX 77843-4466 USA.
Department of Chemical Engineering, Texas A&M University, College Station, TX 77843 USA.
Toxicol Res. 2021 Jan 20;37(2):147-162. doi: 10.1007/s43188-020-00080-z. eCollection 2021 Apr.
Flavonoids are polyphenolic phytochemicals produced in fruits, nuts and vegetables and dietary consumption of these structurally diverse compounds is associated with multiple health benefits including increased lifespan, decreased cardiovascular problems and low rates of metabolic diseases. Preclinical studies with individual flavonoids demonstrate that these compounds exhibit anti-inflammatory and anticancer activities and they enhance the immune system. Their effectiveness in both chemoprevention and chemotherapy is associated with their targeting of multiple genes/pathways including nuclear receptors, the aryl hydrocarbon receptor (AhR), kinases, receptor tyrosine kinases and G protein-coupled receptors. However, despite the remarkable preclinical activities of flavonoids, their clinical applications have been limited and this is due, in part, to problems in drug delivery and poor bioavailability and these problems are being addressed. Further improvements that will expand clinical applications of flavonoids include mechanism-based precision medicine approaches which will identify critical mechanisms of action of individual flavonoids with optimal activities that can be used in combination therapies.
黄酮类化合物是在水果、坚果和蔬菜中产生的多酚类植物化学物质，饮食中摄入这些结构多样的化合物与多种健康益处相关，包括延长寿命、减少心血管问题和降低代谢疾病发生率。对单个黄酮类化合物的临床前研究表明，这些化合物具有抗炎和抗癌活性，并能增强免疫系统。它们在化学预防和化疗中的有效性与其对多种基因/途径的靶向作用有关，这些基因/途径包括核受体、芳烃受体（AhR）、激酶、受体酪氨酸激酶和G蛋白偶联受体。然而，尽管黄酮类化合物在临床前表现出显著的活性，但其临床应用却受到限制，部分原因是药物递送问题和生物利用度差，目前这些问题正在得到解决。黄酮类化合物临床应用的进一步改进包括基于机制的精准医学方法，该方法将确定具有最佳活性的单个黄酮类化合物的关键作用机制，可用于联合治疗。
