科研成果详情

题名Synthetic Chalcones with Potent Antioxidant Ability on H2O2-Induced Apoptosis in PC12 Cells
作者
发表日期2014-10
发表期刊INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES   影响因子和分区
语种英语
原始文献类型Article
关键词chalcone derivatives antioxidant PC12 cells Nrf2-ARE pathway GCLC HO-1
其他关键词HEME OXYGENASE-1 ; ANTICANCER ; ANALOGS ; PROTECTS ; STRESS ; AGENTS
摘要Chalcone derivatives (E)-3-(4-hydroxy-3-methoxyphenyl)-1-(4-methoxyphenyl) prop-2-en-1-one and (E)-3-(4-hydroxyphenyl)-1-(4-methoxyphenyl) prop-2-en-1-one (Compounds 1 and 2) have been demonstrated to be potent anti-inflammatory agents in our previous study. In light of the relationship of intracellular mechanisms between anti-inflammatories and antioxidants, we further designed and synthesized a series of chalcone derivatives based on 1 and 2, to explore their antioxidant efficacy. The majority of the derivatives exhibited strong protective effects on PC12 (PC12 rat pheochromocytoma) cells exposed to H2O2, and all compounds were nontoxic. A preliminary structure-activity relationship was proposed. Compounds 1 and 1d ((E)-2-methoxy-4-(3-(4-methoxyphenyl)-3-oxoprop-1-en-1-yl) phenyl acrylate) exerted the action in a good dose-dependent manner. Quantitative RT-PCR (qRT-PCR) and western blot analysis showed that 1 and 1d significantly improve the expression of nuclear factor erythroid 2 p45-related factor 2 (Nrf2)-dependent antioxidant genes g-Glutamylcysteine Ligase Catalytic Subunit (GCLC) and heme oxygenase-1 (HO-1) and their corresponding proteins (gamma-glutamyl cysteine synthase (gamma-GCS) and HO-1) in PC12 cells. Inhibition of GCLC and HO-1 by specific inhibitors, L-buthionine-S-sulfoximine (BSO) and zinc protoporphyrin (ZnPP), respectively, partially reduce the protective effect of 1 and 1d. These data present a series of novel chalcone analogs, especially compounds 1 and 1d, as candidates for treating oxidative stress-related disease by activating the Nrf2-antioxidant responsive element (ARE) pathway.
资助项目Zhejiang Province Natural Science Funding of China [Y13H300005, LY12H30004]; National Natural Science Foundation of ChinaNational Natural Science Foundation of China (NSFC) [81272462, 81102310]; Technology Foundation for Medical Science of Zhejiang Province [2012KYA129]
出版者MDPI AG
出版地BASEL
ISSN1422-0067
EISSN1422-0067
卷号15期号:10页码:18525-18539
DOI10.3390/ijms151018525
页数15
WOS类目Biochemistry & Molecular Biology ; Chemistry, Multidisciplinary
WOS研究方向Biochemistry & Molecular Biology ; Chemistry
WOS记录号WOS:000344457200053
收录类别SCIE ; PUBMED ; SCOPUS
URL查看原文
PubMed ID25318055
PMC记录号PMC4227230
SCOPUSEID2-s2.0-84907822244
通讯作者地址[Wu, Jian-Zhang]Chemical Biology Research Center,School of Pharmaceutical Sciences,Wenzhou Medical University,Wenzhou,325035,China
Scopus学科分类Catalysis;Molecular Biology;Spectroscopy;Computer Science Applications;Physical and Theoretical Chemistry;Organic Chemistry;Inorganic Chemistry
引用统计
被引频次:40[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符https://kms.wmu.edu.cn/handle/3ETUA0LF/18905
专题药学院(分析测试中心)
第一临床医学院(信息与工程学院)、附属第一医院_计算机与信息管理系
通讯作者Wu, Jian-Zhang
作者单位
1.Chemical Biology Research Center,School of Pharmaceutical Sciences,Wenzhou Medical University,Wenzhou,325035,China;
2.Institute of Sports Science,Wenzhou Medical University,Wenzhou,325035,China;
3.College of Information Science and Computer Engineering,Wenzhou Medical University,Wenzhou,325035,China
第一作者单位药学院(分析测试中心);  生物有机与药物化学研究中心
通讯作者单位药学院(分析测试中心);  生物有机与药物化学研究中心
第一作者的第一单位药学院(分析测试中心)
推荐引用方式
GB/T 7714
Wu, Jian-Zhang,Cheng, Chan-Chan,Shen, Lai-Lai,et al. Synthetic Chalcones with Potent Antioxidant Ability on H2O2-Induced Apoptosis in PC12 Cells[J]. INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES,2014,15(10):18525-18539.
APA Wu, Jian-Zhang., Cheng, Chan-Chan., Shen, Lai-Lai., Wang, Zhan-Kun., Wu, Shou-Biao., ... & Qiu, Pei-Hong. (2014). Synthetic Chalcones with Potent Antioxidant Ability on H2O2-Induced Apoptosis in PC12 Cells. INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES, 15(10), 18525-18539.
MLA Wu, Jian-Zhang,et al."Synthetic Chalcones with Potent Antioxidant Ability on H2O2-Induced Apoptosis in PC12 Cells".INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES 15.10(2014):18525-18539.

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