化学
磁共振成像
体内
多塔
肝细胞癌
合理设计
磁共振造影剂
核医学
放射科
螯合作用
钆
内科学
纳米技术
医学
有机化学
生物
生物技术
材料科学
作者
Yinghui Ding,Xinzhong Ruan,Kun Shu,Weiyuan Xu,Y. Liu,Guangquan Mo,Jiao Xu,Yong Jian,J Zhang,Lingfeng Zhang,Keren Wang,Ji-Ting Hou,Jianliang Shen,Zhihan Yan,Fangfu Ye,Jiang Zhu,Lixiong Dai
标识
DOI:10.1021/acs.jmedchem.4c01084
摘要
Hepatobiliary-specific magnetic resonance imaging contrast agents (MRI CAs) play a crucial role in the early diagnosis of hepatocellular carcinoma (HCC). However, only two acyclic CAs, Gd-BOPTA and Gd-EOB-DTPA, exhibit unfavorable kinetic inertness. Our study focused on the development of superior stable innovative macrocyclic CAs. By introducing a lipophilic benzyloxy group (OBn) into the H4DOTA ring (Gd-L1), we achieved significant enhancement in kinetic inertness. In vivo experiments in mice demonstrated that 40% of the dosage was distributed to the liver at 5 min, providing sustained hepatic enhancement for over 35 min. We also developed an MPO-responsive MRI CA (Gd-L3), which can participate in the "peroxidase cycle" as the substrate, generating oligomers with a 3.8-fold increase in relaxivity, and selectively enhance the lesion in an acute gout mouse model. Overall, our work represents a significant advancement in the field of hepatic and inflammatory MRI, offering promising avenues for early diagnosis and improved imaging outcomes.
科研通智能强力驱动
Strongly Powered by AbleSci AI