Abigail J. Manning, E. Mahdi, A. Pepper, C. Pepper, N. Al-Musayeib, J. Mahdi
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引用次数: 0
Abstract
Acetylsalicylic acid, or aspirin, is one of the most common non-steroidal anti-inflammatory drugs, which has been shown to have anti-cancer effects. However, high doses are needed making it unsuitable as an oncology agent. We have previously reported increased potency in a series of hydroxybenzoate zinc (HBZn) aspirin analogues. Here we show that 3-hydroxybenzoate magnesium (3-HBMg) and 4-hydroxybenzoate magnesium (4-HBMg) aspirin derivatives showed cytotoxic effects at doses as low as 1mM. At these concentrations, 3-HBMg and 4-HBMg aspirin increased the level of caspase-3, p53, Bax and decreased the expression of the anti-antiapoptotic protein, Bcl-2, in HT-1080 Human fibrosarcoma cells. *Correspondence to: Jassem G Mahdi, Cardiff School of Medicine, Cochrane Medical Education Centre, Heath Park, UK, E-mail: mahdij2@cardiff.ac.uk
乙酰水杨酸，或阿司匹林，是最常见的非甾体抗炎药之一，已被证明具有抗癌作用。然而，由于需要高剂量，它不适合作为肿瘤药物。我们以前报道过一系列羟基苯甲酸锌(HBZn)阿司匹林类似物的效力增加。本研究表明，3-羟基苯甲酸镁(3-HBMg)和4-羟基苯甲酸镁(4-HBMg)阿司匹林衍生物在剂量低至1mM时表现出细胞毒性作用。在这些浓度下，3-HBMg和4-HBMg阿司匹林增加了HT-1080人纤维肉瘤细胞中caspase-3、p53、Bax的水平，降低了抗凋亡蛋白Bcl-2的表达。*通信:Jassem G Mahdi，加的夫医学院，科克伦医学教育中心，希思公园，英国，E-mail: mahdij2@cardiff.ac.uk
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