联苯基姜黄素类似物的合成及其抗氧化活性研究  

Synthesis and antioxidant activity of biphenyl curcumin analogues

作　　者：韦星船[1] 曹敏峰 段彦飞[1] 蔡伟平[1] 杨前程[1] 邓妮[1] 任保川 

机构地区：[1]广州大学化学化工学院,广州510006

出　　处：《中国新药杂志》2014年第23期2777-2780,共4页Chinese Journal of New Drugs

基　　金：广东省科技计划项目(2011B050400028);广州市科技计划项目(12C32011623)

摘　　要：目的:以姜黄素为先导化合物,设计合成具有更强抗氧化活性的含联苯基姜黄素类似物,筛选出具有潜在药用价值的化合物。方法:利用联苯单甲醛分别与多种环酮化合物通过羟醛缩合反应合成4种含联苯基姜黄素类似物,通过DPPH分析法测定产物的抗氧化活性。结果与结论:通过1H-NMR,MS等方法对产物进行结构表征,表明所合成4种化合物均为目标产物。产物的抗氧化活性检测结果表明,所合成的4种化合物均具有清除DPPH自由基能力,其中化合物A2,A3,A4的抗氧化活性均比姜黄素、天然抗氧化剂VC和合成抗氧化剂BHT的抗氧化活性更强,其中产物2,9-双(联苯亚甲基)-2-茚酮的抗氧化能力为姜黄素的2.9倍,具有进一步开发研究的价值。Objective： To synthesize 4 biphenyl curcumin analogues with potential medicinal value based on curcumin, which should have a biological activity higher than curcumin itself. Methods： Four compounds were synthesized with 4-biphenylcarboxaldehyde and different kinds of ketone compounds according to aldol reaction, and their antioxidant activity was tested by a DPPH radical elimination method. Results and Conclusion： All compounds were proved by 1^H NMR and MS and other methods. The results of antioxidant activity showed that all the four compounds had a DPPH radical-eliminating activity, and the activity of three compounds （ A2 , A3 and A4 ） was several times stronger than eurcumin. Thus, these biphenyl curcumin analogues may have values of further development and researching.

关 键 词：联苯基 姜黄素类似物 合成 DPPH自由基 抗氧化活性 

分 类 号：R914.5[医药卫生—药物化学]