Tang Long, Jiang Jianchun, Song Guoqiang, Wang Yajing, Zhuang Ziheng, Tan Ying, Xia Yan, Huang Xianfeng, Feng Xiaoqing
Institute of Chemical Industry of Forest Products, Chinese Academy of Forestry, Nanjing 210042, China.
School of Chemical Engineering, Nanjing Forestry University, Nanjing 210037, China.
Int J Mol Sci. 2021 May 26;22(11):5680. doi: 10.3390/ijms22115680.
Urolithins (hydroxylated 6-benzo[]chromen-6-ones) are the main bioavailable metabolites of ellagic acid (EA), which was shown to be a cognitive enhancer in the treatment of neurodegenerative diseases. As part of this research, a series of alkoxylated 6-benzo[]chromen-6-one derivatives were designed and synthesized. Furthermore, their biological activities were evaluated as potential PDE2 inhibitors, and the alkoxylated 6-benzo[]chromen-6-one derivative was found to have the optimal inhibitory potential (IC: 3.67 ± 0.47 μM). It also exhibited comparable activity in comparison to that of BAY 60-7550 in vitro cell level studies.
尿石素（羟基化的6-苯并[]色烯-6-酮）是鞣花酸（EA）的主要生物可利用代谢产物，EA在神经退行性疾病治疗中被证明是一种认知增强剂。作为该研究的一部分，设计并合成了一系列烷氧基化的6-苯并[]色烯-6-酮衍生物。此外，对它们作为潜在磷酸二酯酶2（PDE2）抑制剂的生物活性进行了评估，发现烷氧基化的6-苯并[]色烯-6-酮衍生物具有最佳抑制潜力（IC：3.67±0.47μM）。在体外细胞水平研究中，它与BAY 60-7550相比也表现出相当的活性。
