山柰酚抗肿瘤效应与机制研究进展

Anti-tumor Effect and Mechanism of Kaempferol:A Review

癌症威胁人类健康,新治疗手段应用于癌症治疗能显著延长患者生存时间,但并未改善放化疗患者的不良反应,提高患者的预后仍需癌症研究学者的不断努力。近年来,中药有效成分的抗肿瘤作用受到广泛关注。山柰酚为黄酮类化合物,主要存在于药用植物山柰中,可用于治疗肥胖、心血管疾病、糖尿病等疾病,且具有良好的抗癌活性,能抑制肝癌、结肠癌、肺癌及卵巢癌等多种恶性肿瘤的发生发展。山柰酚主要抗癌形式为诱导细胞凋亡,通过促使细胞内活性氧(ROS)的生成,诱导细胞发生线粒体途径凋亡。山柰酚还可以通过干扰癌细胞周期,使多数癌细胞周期阻滞在G2/M期,并通过诱导细胞自噬发生程序性死亡,抑制细胞迁移侵袭以及血管生成,协同提高化疗药物疗效、减少不良反应等方面发挥抗肿瘤效应。山柰酚作用于一系列细胞内和细胞外靶点,参与肿瘤细胞信号通路调节,涉及磷脂酰肌醇3-激酶(PI3K)/蛋白激酶B(Akt),表皮生长因子受体(EGFR),丝裂原活化蛋白激酶(MAPK),Wnt等信号通路,但以调控PI3K/Akt信号通路为主。此外,山柰酚在肿瘤表观遗传学中也发挥重要的调控作用。笔者对山柰酚抗肿瘤活性及其机制研究进行综述,为山柰酚防治肿瘤的深入研究以及抗肿瘤药物的研发提供参考。

Cancer is a threat to human health. New treatments for cancer can significantly prolong the survival time of patients,but fail to improve the adverse reactions induced by chemoradiotherapy. Improving patient outcomes still requires the effort of cancer researchers. In recent years,the anti-tumor effects of active components from Chinese herbs have received wide attention. Kaempferol,a flavonoid mainly found in the medicinal plant Kaempferia galanga,can be used to treat obesity,cardiovascular diseases,diabetes and other diseases. It has also exhibited good efficacy in inhibiting the occurrence and development of liver cancer,colon cancer,lung cancer,ovarian cancer,and other malignant tumors. Kaempferol mainly exerts the anti-cancer effect by inducing apoptosis. Specifically,it promotes the production of intracellular reactive oxygen species(ROS)and triggers cell apoptosis through the mitochondrial pathway. Besides,it is capable of interfering with the cancer cell cycle,causing most cancer cells to arrest in the G2/M phase,and inducing cell autophagy,a programmed cell death,thus inhibiting cell migration and invasion and angiogenesis,synergistically improving chemotherapeutic drug efficacy,and reducing adverse effects. Kaempferol acts on a series of intracellular and extracellular targets to participate in the regulation of tumor cell signaling pathways, involving phosphatidylinositol 3-kinase(PI3 K)/protein kinase B(Akt),epidermal growth factor receptor(EGFR),mitogen activated protein kinase(MAPK),and Wnt signaling pathways,with the PI3 K/Akt signaling pathway being most significant. In addition,kaempferol also plays an important regulatory role in tumor epigenetics. This paper reviewed the anti-tumor effect and mechanism of kaempferol,aiming to provide reference for in-depth study on its prevention and treatment of tumor and the development of new anti-tumor drugs.