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新型香豆素类白藜芦醇衍生物的合成及其生物活性研究
引用本文:李敏欣,黎勇坤,刘蓓,尹芃程,高慧,毛泽伟. 新型香豆素类白藜芦醇衍生物的合成及其生物活性研究[J]. 化学通报, 2019, 82(11): 1043-1046
作者姓名:李敏欣  黎勇坤  刘蓓  尹芃程  高慧  毛泽伟
作者单位:云南中医药大学中药学院 昆明650500
基金项目:国家自然科学基金(81560620),云南省科学技术厅-云南中医药大学应用基础研究联合专项(2017FF117 (-023)),云南中医药大学大学生创新创业训练计划项目(2018008)
摘    要:白藜芦醇是一种具有广泛生物活性的茋类化合物。为了寻找活性较强的新型分子,以白藜芦醇为原料出发,经Vilsmeier甲酰化和Knoevenagel缩合,合成了3个未见文献报道的香豆素类白藜芦醇衍生物 (E)-7-羟基-5-(4-羟基苯乙烯基)香豆素(3a-3c),其结构经1H NMR、13C NMR和HRMS确证。抗炎和抗氧化活性结果发现,化合物3a具有与地塞米松相当的抗炎活性,并对超氧阴离子和羟基自由基有较强的清除作用,可做进一步研究。

关 键 词:白藜芦醇  香豆素  抗炎活性  抗氧化活性
收稿时间:2019-06-16
修稿时间:2019-07-27

Synthesis and biological evaluation of new coumarin-resveratrol derivatives
Li Min-xin,Li Yong-kun,Liu Bei,Yin Peng-cheng,Gao Hui and Mao Ze-wei. Synthesis and biological evaluation of new coumarin-resveratrol derivatives[J]. Chemistry, 2019, 82(11): 1043-1046
Authors:Li Min-xin  Li Yong-kun  Liu Bei  Yin Peng-cheng  Gao Hui  Mao Ze-wei
Affiliation:School of Pharmacy,Yunnan University of Traditional Chinese Medicine
Abstract:Resveratrol exhibits a broad range of biological activities. In order to study new biological agents, three novel (E)-7-hydroxy-5-(4-hydroxystyryl)coumarin derivatives (3a-3c) have been designed and synthesized starting from resveratrol by Vilsmeier formylation and Knoevenagel condensation. The structure were characterized by 1H NMR, 13C NMR and HRMS, and in vitro anti-inflammatory and antioxidant activities were evaluated. The results demonstrated that the anti-inflammatory potency of compound 3a was almost equal to that of the positive control dexamethasone, and displayed good superoxide anion and hydroxyl free radical scavenging effect.
Keywords:resveratrol   coumarin   anti-inflammatory activity   antioxidant activity
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