| China is a country with high incidence of esophageal cancer, and the main methods to treat esophageal cancer are surgery, radiotherapy and chemotherapy, which is usually combined with radiotherapy and chemotherapy in the treatment of esophageal cancer. Chemotherapy is an important means for the treatment of esophageal cancer, especially for advanced esophageal cancer, the effect is obvious, the inhibition of the tumor is more direct. In recent years, clinical chemotherapy for esophageal cancer are the most commonly used cisplatin and 5- fluorouracil, mitomycin. These chemotherapy drugs to a certain extent, there are more or less the lack of a more or less, so the treatment effect is different, the effect of the drug treatment of esophageal cancer is best to make evaluation. Such as cisplatin, although has broad-spectrum anti-cancer and role, and other advantages, but of the toxic effects caused by the kidney also nots allow to ignore; effect of mitomycin efficiency is higher, but on bone marrow also strongly inhibited. So in the choice of chemotherapy for esophageal cancer should not be to blindly seek esophageal cancer effects of drug therapy for the purpose, but should be combined with the specific stages of patient status and esophageal cancer development and designing a drug treatment program. At present, the existing chemotherapy drugs can cause injury to the patient’s body to a certain extent, which causes the patient can not tolerate the pain caused by chemotherapy, and the treatment compliance is poor. Therefore, it is very important to find a low toxic and effective drug.At present this study of the synthesis of Benzo(d) pyrido(2,3-f)(1,3) zepine(BPZ) compounds in vitro in the biological mechanisms of two kinds of esophageal carcinoma Eca-109 and TE-1 cells for the study. The results showed that different concentrations of BPZ on the two kinds of cells in vitro growth were significantly inhibited; morphological characteristics of drug treated cells showed significant apoptosis; using Annexin V/PI staining and cell apoptosis by flow cytometry quantitative Eca-109 and TE-1 found that the two cell survival rate decreased with the increase of BPZ concentration has obvious the concentration dependent; PI staining by flow cytometry cell cycle results showed that after treatment with BPZ in two esophageal cancer cell cycle arrest of G2/M with the increase of the dose was blocked; mitochondrial membrane potential(JC-1) test results showed that the membrane potential of two kinds of esophageal carcinoma cells after treatment with BPZ significantly decreased the immune protein; Western blot(Western blot) test found that apoptosis related protein, Caspase family Caspase9 and 3 BPZ with the treatment of concentrated activation level Degree increased; caspase 3 cleavage of poly adenosine acid phosphate ribose polymerase 1(poly ADP ribose polymerase, PARP) produced the 89 kd fragment accumulation level increased; with bpz to the increase of drug concentration, cells in the anti apoptotic Bcl-2 protein content decreased, and cell in promoting apoptosis Bax protein content is increased; but phosphorylation of p53 content is not affected by bpz concentration changes. Blot Western test showed that with the increase of BPZ concentration, the expression level of Cyclin B1 in Eca-109 and TE-1 decreased significantly with the increase of G2/M concentration in cell cycle arrest.In summary, BPZ has obvious growth inhibitory effect on Eca-109 and TE-1 two kinds of cells, which is not dependent on P53 regulation by the two G2/M cycle arrest. |
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