Department of Biochemistry, University of Allahabad, Prayagraj, Uttar Pradesh, India.
Lake Erie College of Osteopathic Medicine, Bradenton, FL, United States.
Adv Protein Chem Struct Biol. 2021;125:215-257. doi: 10.1016/bs.apcsb.2020.12.005. Epub 2021 Feb 9.
Ferulic acid (4-hydroxy-3-methoxycinnamic acid, FA), a hydroxycinnamic acid derived from various seeds, nuts, leaves, and fruits, exists in a free form as well as is covalently conjugated with polysaccharides, glycoproteins, polyamines, lignin, and hydroxy fatty acids of plant cell walls. It exhibits a variety of pharmacological effects, such as antioxidant, anti-inflammatory, vasodilatory, antithrombotic, antimicrobial, anti-allergic, antiviral, hepatoprotective, and anticancer activities. FA induces the expression of cell cycle-related proteins, such as p53 and p21, and reduces cyclin D1 and cyclin E levels. Moreover, FA triggers apoptosis and autophagic cell death depending on intracellular reactive oxygen species production in various cancer cell lines. The potential apoptotic action of FA is mediated by altered expression of procaspase-3, procaspase-8, procaspase-9, poly (ADP ribose) polymerase, Bcl-2, and Bax. It blocks the activation of both the canonical Smad and noncanonical extracellular-signal-regulated kinase/Akt (protein kinase B) pathways in various cancer cells. However, due to low solubility and permeability, its availability to biological systems is limited. Therefore, encapsulation of FA into chitosan tripolyphosphate nanoparticles may enhance its cytocompatibility, solubility, and anticancer potential. The nanohybrids of FA and double layered hydroxide exhibit cellular delivery properties of intercalated molecules on cancer cell lines. This chapter summarizes the anticancer efficacy of FA with an emphasis on the role of apoptosis, and underlying molecular mechanisms involving various signaling pathways in tumor cells.
阿魏酸(4-羟基-3-甲氧基肉桂酸,FA)是一种来源于各种种子、坚果、叶子和果实的羟基肉桂酸,以游离形式存在,也与多糖、糖蛋白、多胺、木质素和植物细胞壁的羟基脂肪酸共价结合。它表现出多种药理作用,如抗氧化、抗炎、血管舒张、抗血栓形成、抗菌、抗过敏、抗病毒、保肝和抗癌活性。FA 诱导细胞周期相关蛋白的表达,如 p53 和 p21,并降低细胞周期蛋白 D1 和 E 的水平。此外,FA 在各种癌细胞系中根据细胞内活性氧的产生触发细胞凋亡和自噬性细胞死亡。FA 的潜在凋亡作用是通过改变前半胱氨酸天冬氨酸蛋白酶-3、前半胱氨酸天冬氨酸蛋白酶-8、前半胱氨酸天冬氨酸蛋白酶-9、多聚(ADP 核糖)聚合酶、Bcl-2 和 Bax 的表达来介导的。它阻断了各种癌细胞中经典 Smad 和非经典细胞外信号调节激酶/Akt(蛋白激酶 B)途径的激活。然而,由于低溶解度和低渗透性,其在生物系统中的可用性受到限制。因此,将 FA 包封到壳聚糖三聚磷酸酯纳米粒子中可能会提高其细胞相容性、溶解度和抗癌潜力。FA 与双层氢氧化物的纳米杂化物表现出对癌细胞系中插入分子的细胞内传递特性。本章总结了 FA 的抗癌功效,重点介绍了细胞凋亡的作用以及肿瘤细胞中各种信号通路的潜在分子机制。