Inflammation Targeted Gd3+-Based MRI Contrast Agents Imaging Tumor and Rheumatoid Arthritis Models
文献类型：期刊论文
| 作者 | Leung, Arthur Ho-Hon2; Jin, Jiefu2; Wang, Shuxia3; Lei, Hao3; Wong, Wing-Tak1,4,5 |
| 刊名 | BIOCONJUGATE CHEMISTRY
 |
| 出版日期 | 2014-06-01 |
| 卷号 | 25期号:6页码:1112-1123 |
| 英文摘要 | Inflammatory responses are closely related to cancer progression and several diseases. Anti-inflammatory drugs that bind to inducible enzymes can be used as biomarkers for molecular imaging. Selective targeted contrast agents are expected to improve contrast-to-noise ratio (CNR) in MRI at the site of inflammation. In this work, three new Gd3+ DO3A-amide MRI contrast agents (CAs) that conjugated to mefenamic acid (MA), a commonly used nonsteroidal anti-inflammatory drug (NSAID), through different linkers, ethylenediamine (GdL1), 2,2'-oxidiethylamine (GdL2) and 4,7,10-trioxa-1,13-tridecanediamine (GdL3) were studied. Their relaxivities were GdL1 (4.74 mM(-1) s(-1)), GdL2 (4.77 mM(-1) s(-1)), and GdL3 (4.95 mM(-1) s(-1)) at 400 MHz at 25 degrees C. Their serum albumin binding properties were studied by tryptophan emission-quenching experiments, with GdL1 showing a preferential binding toward HSA and BSA as compared with GdL2 and GdL3. They showed low cytotoxicities toward HeLa cells at high concentration (0.5 mM) and high cellular uptake in U87 cells as compared with GdDOTA In vivo MRI showed increased T1-weighted contrast after intravenous injection of the agents. Moreover, T1 contrast was significantly enhanced for 1.5 h in the U87 tumor model and 2 h in the arthritis joint in adjuvant-induced arthritis (ALA) model at dosages of 0.1 and 0.03 mmol/kg, respectively. Most of the agents were cleared at 24 h post-administration in the AIA model with no observable T1 contrast. GdL1-3 showed superior retentions and intensity enhancements (IEs) at the kidney, liver, tumor, and arthritis joint to those of GdDOTA. GdL3 showed the highest relaxivity and IE at the arthritis joint and is therefore a potential candidate to be developed as MRI CAs that target inflammation. |
| WOS标题词 | Science & Technology ; Life Sciences & Biomedicine ; Physical Sciences |
| 类目[WOS] | Biochemical Research Methods ; Biochemistry & Molecular Biology ; Chemistry, Multidisciplinary ; Chemistry, Organic |
| 研究领域[WOS] | Biochemistry & Molecular Biology ; Chemistry |
| 关键词[WOS] | NONSTEROIDAL ANTIINFLAMMATORY DRUGS ; ASPIRIN-LIKE DRUGS ; IN-VIVO ; SERUM-ALBUMIN ; CYCLOOXYGENASE-2 EXPRESSION ; PROSTAGLANDIN SYNTHASE ; METAL-COMPLEXES ; MESSENGER-RNA ; PHORBOL ESTER ; KAPPA-B |
| 收录类别 | SCI |
| 语种 | 英语 |
| WOS记录号 | WOS:000337720000011 |
| 公开日期 | 2015-07-14 |
| 源URL | [http://ir.wipm.ac.cn/handle/112942/1278]  |
| 专题 | 武汉物理与数学研究所_磁共振基础研究部 |
| 作者单位 | 1.Hong Kong Polytech Univ, Dept Appl Biol & Chem Technol, Kowloon, Hong Kong, Peoples R China 2.Univ Hong Kong, Dept Chem, Pokfulam, Hong Kong, Peoples R China 3.Chinese Acad Sci, Wuhan Ctr Magnet Resonance, State Key Lab Magnet Resonance & Atom & Mol Phys, Wuhan Inst Phys & Math, Wuhan 430071, Hubei, Peoples R China 4.PearL Mat Med Dev Shenzhen Ltd, Shenzhen 518057, Peoples R China 5.Hong Kong Polytech Univ, Henry Cheng Res Lab Drug Dev, Kowloon, Hong Kong, Peoples R China |
| 推荐引用方式 GB/T 7714 | Leung, Arthur Ho-Hon,Jin, Jiefu,Wang, Shuxia,et al. Inflammation Targeted Gd3+-Based MRI Contrast Agents Imaging Tumor and Rheumatoid Arthritis Models[J]. BIOCONJUGATE CHEMISTRY,2014,25(6):1112-1123. |
| APA | Leung, Arthur Ho-Hon,Jin, Jiefu,Wang, Shuxia,Lei, Hao,&Wong, Wing-Tak.(2014).Inflammation Targeted Gd3+-Based MRI Contrast Agents Imaging Tumor and Rheumatoid Arthritis Models.BIOCONJUGATE CHEMISTRY,25(6),1112-1123. |
| MLA | Leung, Arthur Ho-Hon,et al."Inflammation Targeted Gd3+-Based MRI Contrast Agents Imaging Tumor and Rheumatoid Arthritis Models".BIOCONJUGATE CHEMISTRY 25.6(2014):1112-1123. |
入库方式： OAI收割
来源：武汉物理与数学研究所
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