Discovery of efficient stimulators for adult hippocampal neurogenesis based on scaffolds in dragon's blood
作者:Jian-Hua Liang、Liang Yang、Si Wu、Si-Si Liu、Mark Cushman、Jing Tian、Nuo-Min Li、Qing-Hu Yang、He-Ao Zhang、Yun-Jie Qiu、Lin Xiang、Cong-Xuan Ma、Xue-Meng Li、Hong Qing
DOI:10.1016/j.ejmech.2017.05.025
日期:2017.8
discovered to efficiently stimulate adult rats' neurogenesis. In-depth structure-activity relationship studies proved the necessity of a stilbene scaffold that is absent in highly cytotoxic analogs such as chalcones and heteroaryl rings and inactive analogs such as diphenyl acetylene and diphenyl ethane, and validated the importance of an NH in the carboxamide and a methylenedioxy substituent on the
由衰老和神经系统疾病引起的海马神经发生减少会损害神经回路并导致记忆丧失。一种新的铅化合物(ñ -反式-3',4'- methylenedioxystilben -4-基乙酰胺27)已发现有效地刺激成年大鼠的神经发生。深入的结构-活性关系研究证明,在高度细胞毒性类似物(如查耳酮和杂芳基环)和无活性类似物(如二苯乙炔和二苯乙烷)中不存在二苯乙烯骨架的必要性,并验证了氨甲酰胺和苯环上的亚甲二氧基取代基。免疫组织化学染色和生化分析表明,与先前报道的神经保护化学物质相比,N-二苯乙烯基羧酰胺具有神经增殖型神经发生的额外能力,从而为提高成年哺乳动物脑的可塑性提供了基础。