化学
神经保护
脂质过氧化
黄嘌呤氧化酶
二苯醚
螯合作用
乙醚
化学合成
抗氧化剂
立体化学
槲皮素
药理学
生物化学
酶
有机化学
体外
医学
作者
Lei Yang,Ke Huang,Hai Bo Li,Jing Gong,Feng Wang,Yu Bing Feng,Qiao Tao,Yi Hang Wu,Xiao Kun Li,Xiu Mei Wu,Su Zeng,Shawn D. Spencer,Yu Zhao,Jia Qu
摘要
A series of C7-O- and C20-O-amidated 2,3-dehydrosilybin (DHS) derivatives ((±)-1a−f and (±)-2), as well as a set of alkenylated DHS analogues ((±)-4a−f), were designed and de novo synthesized. A diesteric derivative of DHS ((±)-3) and two C23 esterified DHS analogues ((±)-5a and (±)-5b) were also prepared for comparison. The cell viability of PC12 cells, Fe2+ chelation, lipid peroxidation (LPO), free radical scavenging, and xanthine oxidase inhibition models were utilized to evaluate their antioxidative and neuron protective properties. The study revealed that the diether at C7−OH and C20−OH as well as the monoether at C7−OH, which possess aliphatic substituted acetamides, demonstrated more potent LPO inhibition and Fe2+ chelation compared to DHS and quercetin. Conversely, the diallyl ether at C7−OH and C20−OH was more potent in protection of PC12 cells against H2O2-induced injury than DHS and quercetin. Overall, the more lipophilic alkenylated DHS analogues were better performing neuroprotective agents than the acetamidated derivatives. The results in this study would be beneficial for optimizing the therapeutic potential of lignoflavonoids, especially in neurodegenerative disorders such as Alzheimer's and Parkinson's disease.
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