Preparation of two sets of 5,6,7-trioxygenated dihydroflavonol derivatives as free radical scavengers and neuronal cell protectors to oxidative damage
文献类型：期刊论文
| 作者 | Gong, Jingxu2,4; Huang, Kexin2; Wang, Feng3; Yang, Leixiang3; Feng, Yubing3; Li, Haibo3; Li, Xiaokun2; Zeng, Su3; Wu, Xiumei2; Stoeckigt, Joachim1,3 |
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY
 |
| 出版日期 | 2009-05-01 |
| 卷号 | 17期号:9页码:3414-3425 |
| 关键词 | 5,6,7-Trioxygenated dihydroflavonols cis-Dihydroflavonoids Antioxidant Lipid peroxidation Free radical scavenger PC12 cells Xanthine oxidase inhibitor |
| ISSN号 | 0968-0896 |
| DOI | 10.1016/j.bmc.2009.03.032 |
| 文献子类 | Article |
| 英文摘要 | An unusual class of 5,6,7-trioxygenated dihydroflavonols (3a-e and 4a-j) were designed and prepared. Their antioxidative properties were assessed by examining their capacities in several in vitro models, including superoxide anion and 1,1-diphenyl-2-picrylhydrazyl ( DPPH) radical scavenging, rat liver homogenate lipid peroxidation inhibition, PC12 cells protection from oxidative damage, and xanthine oxidase inhibition. These dihydroflavonols displayed positive quenching abilities towards O-2(center dot-) and DPPH free radicals, in which the majority exhibited superior antioxidant properties to Vitamin C. cis-Configurated compound (+/-)-3e demonstrated remarkable inhibition to LPO with an IC50 value of 1.9 +/- 0.3 mu M, which was apparently stronger than that of quercetin (IC50 = 6.0 +/- 0.4 mu M). trans-Configurated dihydroflavonol (+/-)-4h exhibited significant protective effect on PC12 cells against oxidative damage with an EC50 value of 41.5 +/- 5.3 mu M, more effective compared to that of quercetin (EC50 = 81.8 +/- 8.7 mu M). The 6-OH-5,7-dimethoxy analogue (+/-)-3d showed significant inhibition of xanthine oxidase with an IC50 value of 16.0 +/- 0.8 mu M, which is superior to that of allopurinol (IC50 = 23.5 +/- 2.0 mu M). In addition to the hypothesized action mechanism of the bio-active compounds, 3D modeling was used to analyze the relationship between the minimized-energy structures and antioxidant activities. (C) 2009 Elsevier Ltd. All rights reserved. |
| WOS关键词 | XANTHINE-OXIDASE ; STRESS ; FLAVONOIDS ; DISEASE ; BAICALEIN ; ANTIOXIDANTS ; INHIBITION ; HYPOTHESIS ; CANCER |
| 资助项目 | DAAD-CSC PPP Project[CSC [2004] ; Wenzhou Medical College[00000000] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000265683700020 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279246]  |
| 专题 | 天然药物化学研究室 |
| 通讯作者 | Li, Xiaokun |
| 作者单位 | 1.Johannes Gutenberg Univ Mainz, Lehrstuhl Pharmazeut Biol, Inst Pharm, D-55099 Mainz, Germany 2.Wenzhou Med Coll, Key Lab So Zhejiang TCM R&D, Sch Pharm, Wenzhou 325035, Peoples R China; 3.Zhejiang Univ, Coll Pharmaceut Sci, Hangzhou 310058, Zhejiang, Peoples R China; 4.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Gong, Jingxu,Huang, Kexin,Wang, Feng,et al. Preparation of two sets of 5,6,7-trioxygenated dihydroflavonol derivatives as free radical scavengers and neuronal cell protectors to oxidative damage[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2009,17(9):3414-3425. |
| APA | Gong, Jingxu.,Huang, Kexin.,Wang, Feng.,Yang, Leixiang.,Feng, Yubing.,...&Qu, Jia.(2009).Preparation of two sets of 5,6,7-trioxygenated dihydroflavonol derivatives as free radical scavengers and neuronal cell protectors to oxidative damage.BIOORGANIC & MEDICINAL CHEMISTRY,17(9),3414-3425. |
| MLA | Gong, Jingxu,et al."Preparation of two sets of 5,6,7-trioxygenated dihydroflavonol derivatives as free radical scavengers and neuronal cell protectors to oxidative damage".BIOORGANIC & MEDICINAL CHEMISTRY 17.9(2009):3414-3425. |
入库方式： OAI收割
来源：上海药物研究所
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