Xiao Juan, Xu Manman, Hou Teng, Huang Yongwen, Yang Chenlu, Li Jundong
Department of Gynecology, Sun Yat-sen University Cancer Center, State Key Laboratory of Oncology in South China, Collaborative Innovation Center for Cancer Medicine, Guangzhou, Guangdong 510060, P.R. China.
Department of Obstetrics and Gynecology, The First Affiliated Hospital, Sun Yat‑sen University, Guangzhou, Guangdong 510080, P.R. China.
Mol Med Rep. 2015 Sep;12(3):3249-3256. doi: 10.3892/mmr.2015.3784. Epub 2015 May 14.
Src family tyrosine kinase (SFK) activation is associated with ovarian cancer progression. Therefore, SFKs are targets for the development of potential treatments of ovarian cancer. Dasatinib is a tyrosine kinase inhibitor that targets SFK activity, and is used for the treatment of B cell and Abelson lymphomas. At the present time, the potential effect of dasatinib on ovarian cancer is not clear. The aim of the present study was to investigate the antitumor activity of dasatinib, alone and in combination with paclitaxel, in ovarian cancer in vitro and in vivo. In the present study, the expression of Src and phospho‑Src-Y416 (p‑Src) was measured in six ovarian cancer cell lines using western blotting and immunohistochemistry. In addition, cell viability and apoptosis were measured using an MTT assay and annexin V‑fluorescein isothiocyanate staining. An ovarian cancer murine xenograft model was established, in order to evaluate the antitumor effect of dasatinib alone and in combination with paclitaxel in ovarian cancer. High levels of p‑Src protein expression were observed in all cell lines, as compared with healthy cells, which indicated activation of the Src signaling pathway. p‑Src expression increased in ovarian cancer cells following paclitaxel treatment. Dasatinib treatment demonstrated anti‑ovarian cancer properties, by downregulating p‑Src expression and by inducing cancer cell apoptosis. Combined treatment with dasatinib and paclitaxel markedly inhibited proliferation and promoted apoptosis of ovarian cancer cells, compared with control cells. Combined dasatinib and paclitaxel treatment exhibited antitumor activities in vivo and in vitro (combination indices, 0.25‑0.93 and 0.31‑0.75; and tumor growth inhibitory rates, 76.7% and 58.5%, in A2780 and HO8910 cell lines, respectively), compared with paclitaxel treatment alone. Dasatinib monotherapy demonstrated anti‑ovarian cancer activities. The effects of dasatinib and paclitaxel treatments on ovarian cancer cells appeared to be mediated by the Src pathway.
Src家族酪氨酸激酶(SFK)的激活与卵巢癌进展相关。因此,SFK是卵巢癌潜在治疗药物开发的靶点。达沙替尼是一种靶向SFK活性的酪氨酸激酶抑制剂,用于治疗B细胞和阿贝尔森淋巴瘤。目前,达沙替尼对卵巢癌的潜在作用尚不清楚。本研究的目的是在体外和体内研究达沙替尼单独及与紫杉醇联合应用对卵巢癌的抗肿瘤活性。在本研究中,使用蛋白质免疫印迹法和免疫组织化学法检测了六种卵巢癌细胞系中Src和磷酸化Src-Y416(p-Src)的表达。此外,使用MTT法和膜联蛋白V-异硫氰酸荧光素染色检测细胞活力和凋亡情况。建立了卵巢癌小鼠异种移植模型,以评估达沙替尼单独及与紫杉醇联合应用对卵巢癌的抗肿瘤作用。与健康细胞相比,在所有细胞系中均观察到高水平的p-Src蛋白表达,这表明Src信号通路被激活。紫杉醇处理后,卵巢癌细胞中p-Src表达增加。达沙替尼处理通过下调p-Src表达和诱导癌细胞凋亡表现出抗卵巢癌特性。与对照细胞相比,达沙替尼和紫杉醇联合处理显著抑制卵巢癌细胞增殖并促进其凋亡。与单独使用紫杉醇处理相比,达沙替尼和紫杉醇联合处理在体内和体外均表现出抗肿瘤活性(联合指数分别为0.25-0.93和0.31-0.75;在A2780和HO8910细胞系中的肿瘤生长抑制率分别为76.7%和58.5%)。达沙替尼单药治疗表现出抗卵巢癌活性。达沙替尼和紫杉醇处理对卵巢癌细胞的作用似乎是由Src途径介导的。