Jiangsu Food and Pharmaceutical Science College, Huaian, Jiangsu, People's Republic of China.
Department of Natural Medicinal Chemistry, China Pharmaceutical University, Nanjing, People's Republic of China.
Nat Prod Res. 2020 Aug;34(16):2289-2294. doi: 10.1080/14786419.2018.1536708. Epub 2019 Jan 2.
Canthin-6-one analogue, 4-methoxy-5-hydroxycanthin-6-one () was isolated from (D.Don) Benn., and a series of derivatives containing the framework were designed, synthesized, and evaluated for anti-proliferative activity against two human cancer cell lines, HepG2 and HCT116. Among these compounds, the most representative compound exhibited better anti-proliferative activities compared with the positive control Fluorouracil (5-FU), with IC values of 5.05 M (HepG2) and 6.65 M (HCT116), respectively. Compound triggered more significant HepG2 cell apoptosis than 5-FU did in a dose-dependent manner. Furthermore, western blot assay indicated that could enhance the expression of p65 while promoting pro-apoptotic proteins and suppressing the anti-apoptotic proteins in a dose-dependent manner. All these results demonstrated that might be a potential agent for cancer therapy deserving further exploring.
来源于（D.Don）Benn 的咔啉-6-酮类似物，4-甲氧基-5-羟基咔啉-6-酮（），并设计、合成了一系列含有该骨架的衍生物，用于评估它们对两种人癌细胞系 HepG2 和 HCT116 的抗增殖活性。在这些化合物中，最具代表性的化合物 表现出比阳性对照氟尿嘧啶（5-FU）更好的抗增殖活性，IC 值分别为 5.05 M（HepG2）和 6.65 M（HCT116）。化合物 以剂量依赖的方式比 5-FU 诱导更显著的 HepG2 细胞凋亡。此外，Western blot 分析表明， 可以在剂量依赖性方式下增强 p65 的表达，同时促进促凋亡蛋白和抑制抗凋亡蛋白。所有这些结果表明， 可能是一种有前途的癌症治疗药物，值得进一步探索。
