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,
Highlights
In the current medical era much attention has been paid to fight the extreme assembly of reactive oxygen species (ROS), such as hydrogen peroxide, hydroxyl radicals, or superoxide anion, that aggressively interact with natural macromolecules in different tissues by chain process resulting in an oxidative damage[1,2]
Spirooxindoles 6a–p were evaluated for their anti-proliferative potency towards HepG2 liver cancer and PC-3 prostate cancer cell lines
Spirooxindoles 6a–p were more effective towards HCC HepG2 cells rather than prostate cancer PC-3 cells, except compounds 6f, 6 m and 6n
Summary
In the current medical era much attention has been paid to fight the extreme assembly of reactive oxygen species (ROS), such as hydrogen peroxide, hydroxyl radicals, or superoxide anion, that aggressively interact with natural macromolecules in different tissues by chain process resulting in an oxidative damage[1,2]. Biological systems have the capability to defend themselves against these ROS via enzymes (such as glutathione peroxidase, superoxide dismutase, and catalase) or by non-enzymatic mechanisms that involve organic antioxidants molecules (such as glutathione, vitamin C, vitamin E). These antioxidants are capable of direct scavenging the oxidant species through breaking of oxidation propagation chain reactions or through the generation of hydrogen atom in stoichiometric manner, preventing free radical-associated damage[1,2]. Novel antioxidants featuring a variety of chemical structures are needed for prevention of cancer and to augment chemotherapies for different malignancies
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