Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.
Department of Chemistry of Medicinal Plants, National Research Centre, Dokki, Egypt.
J Enzyme Inhib Med Chem. 2020 Dec;35(1):831-839. doi: 10.1080/14756366.2020.1743281.
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.
在当前的医学时代，螺噁吲哚母核作为一种特权杂螺环骨架脱颖而出，它是广泛的生物活性天然分离产物（如士的宁和螺噁利司他汀 A 和 B）和合成化合物的核心。有趣的是，人们对开发具有双重抗氧化和抗癌活性的螺噁吲哚衍生物关注甚少。在这种情况下，对一系列螺噁吲哚 6a-p 进行了研究，以评估它们对 HepG2 肝癌和 PC-3 前列腺癌细胞系的抗癌作用。发现螺噁吲哚 6a 对 HepG2 和 PC-3 细胞均具有高效的增殖抑制作用（IC50 值分别为 6.9 和 11.8 μM）。随后，评估了螺噁吲哚 6a 在 HepG2 细胞中诱导细胞凋亡的潜力，通过 Bax/Bcl-2 比值和 caspase-3 表达水平的显著升高，证实了其促凋亡作用。
