Gheorgheosu Dorina, Duicu Oana, Dehelean Cristina, Soica Codruta, Muntean Danina
Department of Pharmaceutical Chemistry, "Victor Babes" University of Medicine and Pharmacy, 2, Eftimie Murgu Sq., 300041, Timisoara, Romania.
Anticancer Agents Med Chem. 2014;14(7):936-45. doi: 10.2174/1871520614666140223192148.
Betulinic acid (BA), a natural compound with a lupan skeleton, has been highly investigated in the past decade for a plethora of beneficial properties, including anti-cancer, anti-inflammatory, anti-angiogenic, immune-modulatory, and anti-HIV effects. In particular, BA has been reported to be effective in vitro against tumor cell lines of different origins, and also in vivo, in animal models of cancer. The best characterized mechanism of its antitumor effect consists of triggering apoptosis via the mitochondrial pathway. BA has also an anti-metastatic effect via the prevention of the epithelial-to-mesencymal transition in highly aggressive melanoma cells. Furthermore, in the same model, BA is able to counteract the pro-invasive potential of the pro-tumoral protein neutrophil gelatinaseassociated lipocalin. The present review addresses the current state of knowledge regarding the anti-tumor effects of betulinic acid, a potent chemotherapeutic agent.
桦木酸(BA)是一种具有羽扇豆骨架的天然化合物,在过去十年中因其众多有益特性而受到广泛研究,这些特性包括抗癌、抗炎、抗血管生成、免疫调节和抗HIV作用。特别是,据报道BA在体外对不同来源的肿瘤细胞系有效,在体内对癌症动物模型也有效。其抗肿瘤作用最明确的机制是通过线粒体途径触发细胞凋亡。BA还通过防止高侵袭性黑色素瘤细胞的上皮-间质转化发挥抗转移作用。此外,在同一模型中,BA能够抵消促肿瘤蛋白中性粒细胞明胶酶相关脂质运载蛋白的促侵袭潜力。本综述阐述了关于桦木酸这种有效化疗药物抗肿瘤作用的当前知识状态。