芒柄花素抗肿瘤作用机制的研究进展  

Research Progress on Anti-tumor Mechanism of Formononetin

作　　者：赵玉民 冯叶雯 张黎[1] 余成浩[1] ZHAO Yu-min;FENG Ye-wen;ZHANG Li;YU Cheng-hao(Chengdu University of Traditional Chinese Medicine,Chengdu 610036,China)

机构地区：[1]成都中医药大学,成都610036

出　　处：《中国实验方剂学杂志》2021年第10期193-203,共11页Chinese Journal of Experimental Traditional Medical Formulae

基　　金：国家自然科学基金项目(81673878);四川省青年科技创新研究团队项目(2020JDTD0022);中医药“杏林学者”学科人才研究促进计划项目(XSGG2019006)。

摘　　要：芒柄花素(FN)是一种从红三叶草、黄芪和鸡血藤等药用草本植物中提取的植物异黄酮。研究表明,芒柄花素具有较强的抗肿瘤生物活性,可作为抗肿瘤药物治疗各种恶性肿瘤。迄今为止的研究表明,芒柄花素通过多种分子机制与途径对肿瘤产生抑制增殖、诱导凋亡、抑制迁移和侵袭、诱导细胞周期停滞等作用,可以在乳腺癌、结直肠癌、前列腺癌、膀胱癌和肺癌等多种肿瘤细胞和动物模型中观察到这些抗肿瘤活性。主要抗肿瘤活性体现在触发活性氧(ROS)生成、调节磷脂酰肌醇3-激酶(PI3K)/蛋白激酶B(Akt)/雷帕霉素靶蛋白(mTOR)和丝裂原活化蛋白激酶(MAPK)信号通路;抑制酪氨酸激酶1(JAK1),酪氨酸激酶2(JAK2)和非受体酪氨酸激酶(c-Src)的激活;调节细胞角蛋白19(CK19),基质金属蛋白酶(MMP),微小RNA-21(miR-21),核纤层蛋白A/C抗体(Lamin A/C),细胞周期蛋白D1(Cyclin D1)和细胞周期蛋白E1(Cyclin E1)的表达。此外,笔者对于芒柄花素衍生物的抗肿瘤作用研究也进行了综述。通过对芒柄花素的化学结构进行修饰,目前已得到多种具有抗肿瘤作用的衍生物。实验结果表明芒柄花素的一些衍生物具有更强的抗肿瘤活性和较低的细胞毒性,分子作用机制研究仍需要进一步深入。综上所述,芒柄花素及其衍生物可能成为抗肿瘤的潜在新药。Formononetin is a kind of plant isoflavones extracted from medicinal herbs such as Trifolium pratense,Astragalus membranaceus and Spatholobi Caulis have shown that formononetin has strong anti-tumor biological activity,and can be used as an anti-tumor drug in the treatment of various malignant tumors. Many studies so far have shown that formononetin can inhibit cell proliferation,induce cell apoptosis,inhibit cell migration and invasion,and induce cell cycle arrest on tumors through a variety of molecular mechanisms and pathways. These antitumor activities can be observed in cells of various tumors such as breast cancer,colorectal cancer,prostate cancer,bladder cancer and lung cancer in trials and animal models. Examples of these effects include triggering the generation of reactive oxygen species(ROS),regulating phosphatidylinositol-3-kinase/protein kinase B/mammalian target of rapamycin(PI3 K/Akt/mTOR) and Mitogen-activated protein kinases(MAPK)signaling pathways,inhibiting the activation of tyrosine kinase(JAK1 and JAK2)and nonreceptor tyrosine kinase(c-Src),and regulating cytokeratin 19(CK19),matrix metalloproteinases(MMP),microRNA-21(miR-21),lamin A/C antibody(Lamin A/C),expression of Cyclin D1 and Cyclin E1. In addition,the anti-tumor effects of formononetin derivatives were reviewed in this paper. By modifying the chemical structure of formononetin,many related derivatives have been obtained. Experimental results have shown that some derivatives of formononetin have stronger anti-tumor activity and lower cytotoxicity,but the related molecular mechanism of action still needs to be explored further in-depth. In conclusion,formononetin and its derivatives may become potential anti-tumor drugs.

关 键 词：芒柄花素 抗肿瘤 衍生物 作用机制 

分 类 号：R22[医药卫生—中医基础理论] R242[医药卫生—中医学]