Preparation of C-23 esterified silybin derivatives and evaluation of their lipid peroxidation inhibitory and DNA protective properties
文献类型：期刊论文
| 作者 | Wang, Feng2,3; Huang, Kexin3; Yang, Leixiang2; Gong, Jingxu1; Tao, Qiaofeng2,3; Li, Haibo2; Zhao, Yu2,3; Zeng, Su2; Wu, Xiumei3; Stoeckigt, Joachim2,4 |
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY
 |
| 出版日期 | 2009-09-01 |
| 卷号 | 17期号:17页码:6380-6389 |
| 关键词 | Flavonolignan Silybin derivative Antioxidant Lipid peroxidation Free radical scavenger DNA damage protective Fe2+ ion chelation |
| ISSN号 | 0968-0896 |
| DOI | 10.1016/j.bmc.2009.07.023 |
| 文献子类 | Article |
| 英文摘要 | A diverse series of C-23 esterified silybin derivatives (1a-n) were designed and synthesized. The antioxidative properties of these compounds were evaluated by 1,1-diphenyl-2-picrylhydrazyl (DPPH) and superoxide anion radical scavenging, ferrous ion chelation, and inhibition of rat liver homogenate lipid peroxidation. Their protective effects on the prevention of hydrogen peroxide induced DNA damage were also investigated. Most of the synthesized compounds exhibited more effective antioxidant activities than silybin. The esterified silybin analogues displayed satisfactory performance especially on iron chelation and antiperoxidative activity. Compound 1n in particular exhibited remarkable antiperoxidative effect with an IC50 value of 0.2 +/- 0.1 mu M, which was stronger than that of quercetin (IC50 = 1.8 +/- 0.6 mu M). Compounds 1c, 1e, 1g, 1h and 1k displayed potent, dose-dependent protective properties against DNA cleavage. The results of the bioassays support the antioxidative and DNA protective effects of these synthesized silybin derivatives. (C) 2009 Elsevier Ltd. All rights reserved. |
| WOS关键词 | RADICAL SCAVENGERS ; OXIDATIVE STRESS ; ANTIOXIDANT ; DISEASE ; SILYMARIN ; FLAVONOIDS ; MECHANISM ; DAMAGE |
| 资助项目 | DAAD-CSC PPP[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:000269029100029 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279143]  |
| 专题 | 天然药物化学研究室 |
| 通讯作者 | Zhao, Yu |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China; 2.Zhejiang Univ, Coll Pharmaceut Sci, Hangzhou 310058, Zhejiang, Peoples R China; 3.Wenzhou Med Coll, Sch Pharm, Key Lab So Zhejiang TCM R&D, Wenzhou 325035, Peoples R China; 4.Johannes Gutenberg Univ Mainz, Inst Pharm, Lehrstuhl Pharmazeut Biol, D-55099 Mainz, Germany |
| 推荐引用方式 GB/T 7714 | Wang, Feng,Huang, Kexin,Yang, Leixiang,et al. Preparation of C-23 esterified silybin derivatives and evaluation of their lipid peroxidation inhibitory and DNA protective properties[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2009,17(17):6380-6389. |
| APA | Wang, Feng.,Huang, Kexin.,Yang, Leixiang.,Gong, Jingxu.,Tao, Qiaofeng.,...&Qu, Jia.(2009).Preparation of C-23 esterified silybin derivatives and evaluation of their lipid peroxidation inhibitory and DNA protective properties.BIOORGANIC & MEDICINAL CHEMISTRY,17(17),6380-6389. |
| MLA | Wang, Feng,et al."Preparation of C-23 esterified silybin derivatives and evaluation of their lipid peroxidation inhibitory and DNA protective properties".BIOORGANIC & MEDICINAL CHEMISTRY 17.17(2009):6380-6389. |
入库方式： OAI收割
来源：上海药物研究所
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