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首页> 外文期刊>Journal of enzyme inhibition and medicinal chemistry. >Antitumor properties of certain spirooxindoles towards hepatocellular carcinoma endowed with antioxidant activity
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Antitumor properties of certain spirooxindoles towards hepatocellular carcinoma endowed with antioxidant activity

机译:抗氧化活性赋予肝细胞癌某种螺氧吲哚啉的抗肿瘤性质

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In the current medical era, spirooxindole motif stands out as a privileged heterospirocyclic scaffold that represents the core for a wide range of bioactive naturally isolated products (such as Strychnofoline and spirotryprostatins A and B) and synthetic compounds. Interestingly, no much attention has been paid to develop spirooxindole derivatives with dual antioxidant and anticancer activities. In this context, a series of spirooxindoles 6a-p was examined for their anticancer effect towards HepG2 hepatocellular carcinoma and PC-3 prostate cancer cell lines. Spirooxindole 6a was found to be an efficient anti-proliferative agent towards both HepG2 and PC-3 cells (IC50?=?6.9 and 11.8?μM, respectively). Afterwards, spirooxindole 6a was assessed for its apoptosis induction potential in HepG2 cells, where its pro-apoptotic impact was approved via the significant elevation in the Bax/Bcl-2 ratio and the expression levels of caspase-3.
机译:在目前的医学时代,螺氧吲哚基序作为特征的异质环状支架,其代表着各种生物活性天然分离的产物(如脱苯甲孔和螺旋霉属植物A和B)和合成化合物的核心。有趣的是,没有重视肌脂吲哚衍生物的支付,具有双抗氧化和抗癌活动。在这种情况下,检查了一系列螺氧吲哚醇6a-p,用于对Hepg2肝细胞癌和PC-3前列腺癌细胞系进行抗癌作用。发现螺氧吲哚6a是朝向HepG2和PC-3细胞的有效抗增殖剂(IC50?=Δ6.9和11.8≤μm)。然后,评估螺氧吲哚6a,用于其HepG2细胞中的凋亡诱导潜力,其中通过Bax / Bcl-2比的显着升高和Caspase-3的表达水平来批准其促凋亡的影响。

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