Hepatocellular carcinoma (HCC) is the third-leading cause of cancer-related deaths with 750,000 newly diagnosed cases each year. Surgery, radiotherapy, and chemotherapy constitute the main treatment modalities for HCC, but liver cirrhosis and damage often occur. Molecular targeted drugs have been recently developed to treat HCC. Vascular endothelial growth factor (VEGF)/VEGF receptor (VEGFR) autocrine signaling is closely related to the growth, progression, and metastasis of HCC, making the VEGF/VEGFR axis an ideal target for the development of molecular targeted agents. Here, we report the effects of the novel anti-VEGF humanized monoclonal antibody BD0801 on the growth of HCC cells in vitro and in vivo as well as the underlying mechanisms. BD0801 significantly inhibited the proliferation of HepG2, SMMC-7721, and Bel7402 cells in vitro, accompanied with an induction of apoptosis and cell cycle arrest at the G1 phase. BD0801 potently suppressed AKT, Erk1/2, and retinoblastoma (Rb) phosphorylation, while increasing p21 and decreasing cyclin D1 protein levels. BD0801 significantly inhibited growth in mouse tumor xenografts and induced cell apoptosis of HepG2 and SMMC-7721 tumor xenografts. Furthermore, BD0801 effectively reduced the vascular density and tumor tissue microvessel density (MVD). Similarly, BD0801 decreased AKT, Erk1/2, and Rb phosphorylation and cyclin D1 expression whereas it increased p21 protein expression in mouse HCC tumor xenografts. Importantly, BD0801 showed a better effect than Bevacizumab (Bev) on the inhibition of cell growth and induction of apoptosis in HCC cells in vitro and in vivo. These findings suggest that BD0801 is a potent anti-VEGF monoclonal antibody for the treatment of HCC.

译文

肝细胞癌 (HCC) 是癌症相关死亡的第三大原因,每年有750,000例新诊断病例。手术,放疗和化疗是肝癌的主要治疗方式,但经常发生肝硬化和损害。最近开发了分子靶向药物来治疗HCC。血管内皮生长因子 (VEGF)/VEGF受体 (VEGFR) 自分泌信号与HCC的生长、进展和转移密切相关,使得VEGF/VEGFR轴成为开发分子靶向药物的理想靶点。在这里,我们报告了新型抗VEGF人源化单克隆抗体BD0801对体外和体内HCC细胞生长的影响以及潜在的机制。BD0801在体外显着抑制HepG2,SMMC-7721和Bel7402细胞的增殖,并在G1期诱导凋亡和细胞周期停滞。BD0801有效抑制AKT,Erk1/2和视网膜母细胞瘤 (Rb) 的磷酸化,同时增加p21并降低细胞周期蛋白D1蛋白水平。BD0801显著抑制小鼠肿瘤异种移植物的生长,并诱导HepG2和SMMC-7721肿瘤异种移植物的细胞凋亡。此外,BD0801有效降低了血管密度和肿瘤组织微血管密度 (MVD)。同样,BD0801降低了小鼠HCC肿瘤异种移植物中AKT,Erk1/2和Rb磷酸化和cyclin D1的表达,而增加了p21蛋白的表达。重要的是,在体外和体内,BD0801在抑制HCC细胞生长和诱导凋亡方面显示出比贝伐单抗 (Bev) 更好的效果。这些发现表明BD0801是一种有效的抗VEGF单克隆抗体,可用于治疗HCC。

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