一个黄金复合体启动了生物活性多的功能化,应用于F标记的化学探针
Ziyun Liu1, Yuki Fukagawa1, Masaharu Yamano1
1Department of Chemical Science and Engineering, Tokyo Institute of Technology, 12-12-1-H101 Ookayama, Meguro, Tokyo, 152-8552, Japan. thiroshi@cap.mac.titech.ac.jp.
Organic & biomolecular chemistry
|July 12, 2023
概括
研究人员开发了一种新的方法来修改绿茶中的 (-) - 乙甲基酸盐 (EGCG),创造潜在的抗癌药物候选物和化学探针. 功能化的EGCG保留了其抗癌功效,并使18F标记化合物的合成成为可能.
科学领域:
- 药用化学 医学化学
- 有机合成 有机合成
- 绿茶 植物化学 绿茶 植物化学
背景情况:
- (-) 绿茶中主要的一种甲基素 - - 乙甲基酸盐 (EGCG) 通过向67kDa的拉米因受体,表现出抗癌和抗过敏活性.
- 功能化EGCG为研究和治疗提供了新药候选物和化学探针的途径.
研究的目的:
- 开发一种有效的方法来修改EGCG的A环.
- 合成18F标记的EGCG,用于成像或向放射治疗.
- 评估EGCG功能化对其抗癌疗效的影响.
主要方法:
- 用黄金催化反应与阿米多甲基2-基酸进行EGCG的电友芳香替代.
- 合成用于18F标签的前体,包括对酸敏感的保护组和基不稳定的离开组.
- 在U266细胞中评估修饰EGCG的抗癌活性,并确定18F标记EGCG的放射化学产量.
主要成果:
- 建立了一种用于A环C6和C8位置的EGCG区域选择性功能化的新方法.
- 功能化 EGCG 衍生物与新醇标记组在 U266 细胞中保持了抗癌疗效.
- 标有18F的EGCG在酸性降低保护条件下合成,其显著的放射性化学产量为8替代异构体的37%.
结论:
- 开发的黄金催化功能化策略为创建EGCG衍生品提供了一个多功能途径.
- 标有18F的EGCG的成功合成突显了这种方法在开发放射性药物的潜力.
- 这种方法为推进基于EGCG的药物发现和分子成像提供了一个有前途的平台.
更多相关视频
10:38Synthesis of Functionalized 10-nm Polymer-coated Gold Particles for Endothelium Targeting and Drug Delivery
Published on: January 15, 2018
12.6K
14:02Optimizing the Genetic Incorporation of Chemical Probes into GPCRs for Photo-crosslinking Mapping and Bioorthogonal Chemistry in Live Mammalian Cells
Published on: April 9, 2018
8.5K
相关概念视频
03:31Labeling DNA Probes
8.2K
DNA probes are fragments of DNA labeled with a reporter tag to enable their detection or purification. The resulting labeled DNA probes can then hybridize to target nucleic acid sequences through complementary base-pairing, and may be used to recover or identify these regions.
Radioisotopes, fluorophores, or small molecule binding partners like biotin or digoxigenin, are the most widely used reporter tags for labeling DNA probes. These labels can be attached to the probe DNA molecule via...
Radioisotopes, fluorophores, or small molecule binding partners like biotin or digoxigenin, are the most widely used reporter tags for labeling DNA probes. These labels can be attached to the probe DNA molecule via...
8.2K
01:20Immunogold Electron Microscopy
4.1K
Immunoelectron microscopy utilizes immunogold labeling of endogenous proteins with specific antibodies to detect and localize these proteins in cells and tissues. The procedure provides insights into the distribution and quantification of protein under different stimulation conditions offering clues about their functions. Conjugating highly electron-dense gold particles with primary or secondary antibodies allow antigen detection on and within cells, with high resolution and specificity.
4.1K