新型川芎内酯类似物作为神经保护剂的设计与合成。
Design and synthesis of novel senkyunolide analogues as neuroprotective agents.
作者信息
Fang Yuanying, Wang Rikang, Wang Qi, Sun Yongbing, Xie Saisai, Yang Zunhua, Li Min, Jin Yi, Yang Shilin
机构信息
National Engineering Research Center for Manufacturing Technology of TCM Solid Preparation, Jiangxi University of Traditional Chinese Medicine, Nanchang 330006, China.
College of Pharmacy, Jiangxi University of Traditional Chinese Medicine, Nanchang 330004, China.
出版信息
Bioorg Med Chem Lett. 2018 Feb 15;28(4):668-672. doi: 10.1016/j.bmcl.2018.01.018. Epub 2018 Jan 12.
A class of senkyunolide analogues bearing benzofuranone fragment were designed, synthesized and evaluated for their neuroprotective effect in models of oxygen glucose deprivation (OGD) and oxidative stress. All tested compounds showed neuroprotection profile based on the cell viability assay. In particular, derivatives 1f-1i possessing furoxan-based nitric oxide releasing functionality exhibited significant biological activities in OGD models. More importantly, compound 1g containing short linker with furoxan displayed the most potent neuroprotection at the concentration of 100 μM (cell survival up to 145.2%). Besides, 1g also showed the middle level neuroprotective effect in model of oxidative stress.
设计、合成了一类带有苯并呋喃酮片段的川芎内酯类似物，并在氧糖剥夺（OGD）和氧化应激模型中评估了它们的神经保护作用。基于细胞活力测定，所有测试化合物均显示出神经保护作用。特别是，具有基于呋咱的一氧化氮释放功能的衍生物1f-1i在OGD模型中表现出显著的生物活性。更重要的是，含有与呋咱相连的短连接子的化合物1g在100μM浓度下表现出最强的神经保护作用（细胞存活率高达145.2%）。此外，1g在氧化应激模型中也表现出中等水平的神经保护作用。
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