Xu Xingyu, Li Cong, Lei Min, Zhu Zhiyuan, Yan Jianming, Shen Xu, Hu Lihong
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, University of Chinese Academy of Sciences, Chinese Academy of Sciences, Shanghai 201203, PR China.
School of Life Science, Shanghai University, 99 Shangda Road, Shanghai 200444, PR China.
Bioorg Med Chem Lett. 2016 Jul 1;26(13):2988-2991. doi: 10.1016/j.bmcl.2016.05.028. Epub 2016 May 10.
A series of arctigenin-4-yl carbamate derivatives were synthesized and evaluated for potency in reducing β-amyloid (Aβ) content in HEK293-APPswe cells. Most of the arctigenin-4-yl aralkyl or aryl carbamate derivatives showed improved potency in reducing Aβ content. Among the synthesized compounds, arctigenin-4-yl (3-chlorophenyl)carbamate (20) exhibited the strongest potency with 78.7% Aβ content reduction at 20μM. Furthermore, the effect of arctigenin-4-yl (4-chlorophenyl)carbamate (19) and arctigenin-4-yl (3-chlorophenyl)carbamate (20) on lowing Aβ content was better than arctigenin under the concentrations of 1, 10 and 20μM.
合成了一系列牛蒡子苷元-4-基氨基甲酸酯衍生物，并评估了它们在降低HEK293-APPswe细胞中β-淀粉样蛋白（Aβ）含量方面的效力。大多数牛蒡子苷元-4-基芳烷基或芳基氨基甲酸酯衍生物在降低Aβ含量方面表现出更高的效力。在合成的化合物中，牛蒡子苷元-4-基（3-氯苯基）氨基甲酸酯（20）表现出最强的效力，在20μM时Aβ含量降低78.7%。此外，在1、10和20μM的浓度下，牛蒡子苷元-4-基（4-氯苯基）氨基甲酸酯（19）和牛蒡子苷元-4-基（3-氯苯基）氨基甲酸酯（20）降低Aβ含量的效果优于牛蒡子苷元。
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