李敏欣,黎勇坤,刘蓓,尹芃程,高慧,毛泽伟.化学通报,2019,82(11):1043-1046. |
新型香豆素类白藜芦醇衍生物的合成及其生物活性研究 |
Synthesis and biological evaluation of new coumarin-resveratrol derivatives |
投稿时间:2019-06-16 修订日期:2019-07-27 |
DOI: |
中文关键词: 白藜芦醇 香豆素 抗炎活性 抗氧化活性 |
英文关键词:resveratrol coumarin anti-inflammatory activity antioxidant activity |
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) |
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中文摘要: |
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。 |
英文摘要: |
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. |
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