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Antitumor properties of certain spirooxindoles towards hepatocellular carcinoma endowed with antioxidant activity
Journal of Enzyme inhibition and Medicinal Chemistry ( IF 5.6 ) Pub Date : 2020-03-25 , DOI: 10.1080/14756366.2020.1743281
Sara T. Al-Rashood 1 , Ahmed R. Hamed 2, 3 , Ghada S. Hassan 4 , Hamad M. Alkahtani 1 , Abdulrahman A. Almehizia 1 , Amal Alharbi 1 , Mohammad M. Al-Sanea 5 , Wagdy M. Eldehna 6
Affiliation  

Abstract

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,



中文翻译:

具有抗氧化活性的某些螺菌毒素对肝细胞癌的抗肿瘤作用

摘要

在当前的医学时代,螺氧杂吲哚基序作为一种特权的杂环螺环支架而脱颖而出,代表了多种生物活性天然分离产品(如金丝茶酚和螺环孢菌素A和B)和合成化合物的核心。有趣的是,开发具有双重抗氧化剂和抗癌活性的螺并吲哚衍生物并没有引起太多关注。在这种情况下,检查了一系列螺硫辛多酯6a-p对HepG2肝细胞癌和PC-3前列腺癌细胞系的抗癌作用。发现螺氧杂吲哚6a是对HepG2和PC-3细胞的有效抗增殖剂(IC50分别为6.9和11.8 µM)。之后,评估了螺环吲哚6a在HepG2细胞中的凋亡诱导潜力,

更新日期:2020-04-20
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