3,5-Diarylpyrazole Derivatives Obtained by Ammonolysis of the Total Flavonoids from Chrysanthemum indicum Extract Show Potential for the Treatment of Alzheimer鈥檚 Disease

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• 作者：Taizong Wu ; Cheng Jiang ; Ling Wang ; Susan L. Morris-Natschke ; Hui Miao ; Lianquan Gu ; Jun Xu ; Kuo-Hsiung Lee ; Qiong Gu
• 刊名：Journal of Natural Products
• 出版年：2015
• 出版时间：July 24, 2015
• 年：2015
• 卷：78
• 期：7
• 页码：1593-1599
• 全文大小：380K
• ISSN：1520-6025

文摘

Four new 3,5-diarylpyrazole analogues (1鈥?b>4) were isolated from an extract of the flowers of Chrysanthemun indicum using a combination of ammonolysis of the total flavonoid extract and an A尾 aggregation inhibitory activity guided purification procedure. All four compounds (1鈥?b>4) showed moderate to potent activity against A尾 aggregation with EC₅₀ values of 4.3, 15.8, 1.3, and 2.9 渭M, respectively. Moreover, compound 3 showed low cytotoxicity and significant neuroprotective activity against A尾-induced cytotoxicity in the SH-SY5Y cell line. This report is the first to show that 3,5-diarylpyrazole analogues can inhibit A尾 aggregation and exhibit neuroprotective activity with potential for the treatment of Alzheimer鈥檚 disease. Taken together, the method presented here offers an alternative approach to yield bioactive compounds.