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Small benzothiazole molecule induces apoptosis and prevents metastasis through DNA interaction and c-MYC gene supression in diffuse-type gastric adenocarcinoma cell line
Chemico-Biological Interactions ( IF 5.1 ) Pub Date : 2018-08-11 , DOI: 10.1016/j.cbi.2018.08.006
Felipe Pantoja Mesquita , Laine Celestino Pinto , Bruno Moreira Soares , Adrhyann Jullyanne de Sousa Portilho , Emerson Lucena da Silva , Ingryd Nayara de Farias Ramos , André Salim Khayat , Caroline Aquino Moreira-Nunes , Mirna Marques Bezerra , Eliza de Lucas Chazin , Thatyana Rocha Alves Vasconcelos , Rommel Mario Rodríguez Burbano , Maria Elisabete Amaral de Moraes , Raquel Carvalho Montenegro

Chemo-resistance has been reported as a relevant barrier for the efficiency of gastric cancer treatment. Therefore, the development of effective and safe drugs for cancer chemotherapy is still a challenge. The purpose of this study was to evaluate the anticancer potential of (E)-2-(((2-(benzo[d]thiazo-2-yl)hydrazono)methyl)-4-nitrophenol) (AFN01) against gastric cancer cell lines. Our results showed promising anticancer activity against gastric cancer cells ACP-02 (IC50 = 1.0 μM) and mild activity against other cell lines including non-malignant gastric cell MNP-01 (IC50 = 3.4 μM). This compound significantly induced S phase cell cycle arrest, prevented cell migration and triggered apoptosis in a concentration-dependent manner. Moreover, AFN01 was significantly more genotoxic against tumoral cell ACP-02, when compared to non-malignant cells, such as MNP-01 and healthy peripheral mononuclear blood cells. AFN01 also synergistically interacts with doxorubicin suppressing cell proliferation and c-MYC gene expression in gastric cancer cell line model, with remarkable c-MYC overexpression. Although further pre-clinical and clinical studies are required to explore its safety and efficiency, AFN01 may represent a promising lead anticancer agent for the treatment of gastric cancer.



中文翻译:

苯并噻唑小分子通过弥散型胃腺癌细胞系中的DNA相互作用和c-MYC基因抑制来诱导细胞凋亡并防止转移

耐药性已被报告为胃癌治疗效率的相关障碍。因此,开发有效且安全的用于癌症化疗的药物仍然是一个挑战。这项研究的目的是评估(E)-2-((((2-(benzo [ d ] thiazo-2-yl)hydrazono)methyl)-4-nitrophenol)(AFN01)对胃癌细胞的抗癌潜力线。我们的结果表明,针对胃癌细胞ACP-02(IC 50  = 1.0μM)的抗癌活性前景良好,对包括非恶性胃细胞MNP-01(IC 50)在内的其他细胞系的抗癌活性也较弱 = 3.4μM)。该化合物以浓度依赖的方式显着诱导S期细胞周期停滞,阻止细胞迁移并引发细胞凋亡。此外,与非恶性细胞(如MNP-01和健康的外周单个核血细胞)相比,AFN01对肿瘤细胞ACP-02的遗传毒性更高。AFN01还与阿霉素协同作用,在胃癌细胞系模型中抑制细胞增殖和c-MYC基因表达,并具有明显的c-MYC过表达。尽管需要进一步的临床前和临床研究来探索其安全性和有效性,但AFN01可能代表了一种有前途的治疗胃癌的主要抗癌药。

更新日期:2018-08-11
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