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EtNBS and EtNBS-COOH PDT efficacy in ovarian cancer cells

机译:EtNBS和EtNBS-COOH PDT在卵巢癌细胞中的功效

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The effective treatment of metastatic cancer continues to be a challenge due to the highly invasive nature of metastatic lesions and their propensity to develop therapeutic resistance. Optimal therapeutic regimens for peritoneal metastases should have both rapid uptake and penetrate throughout cancerous lesions. Using in vitro models of ovarian cancer, we have found that the cores of tumor nodules are both hypoxic and acidic, rendering most chemotherapeutic agents ineffective, and considerably reducing the therapeutic efficacy of the majority of photodynamic therapy (PDT) and radiation therapy regimens. PDT using EtNBS, a cationic photosensitizer, is a promising approach for treating these hypoxic and acidic nodule cores as it rapidly accumulates into the hypoxic cores of tumor nodules, and is effective even in completely anoxic environments. To improve the uptake rate of EtNBS into cells, we utilized a carboxylic acid terminated derivative of EtNBS that is zwitterionic at biological pH levels. In this study, we investigated the effect of this structural change on PDT efficacy in ovarian cancer cells.
机译:由于转移性病变的高度侵袭性及其发展成治疗耐药性的倾向,有效治疗转移性癌症仍然是一个挑战。腹膜转移的最佳治疗方案应迅速吸收并穿透整个癌性病变。使用卵巢癌的体外模型,我们发现肿瘤结节的核心既缺氧又呈酸性,这使大多数化学治疗剂无效,并大大降低了大多数光动力疗法(PDT)和放射疗法的治疗效果。使用EtNBS(一种阳离子光敏剂)的PDT是治疗这些缺氧和酸性结节核心的有前途的方法,因为它迅速积累到肿瘤结节的缺氧核心中,甚至在完全缺氧的环境中也有效。为了提高EtNBS进入细胞的吸收速率,我们利用了EtNBS的羧酸封端衍生物,该衍生物在生物pH值水平上为两性离子。在这项研究中,我们调查了这种结构变化对卵巢癌细胞中PDT功效的影响。

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