当前位置: X-MOL 学术Bioorg. Med. Chem. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Synthesis and bioactivity evaluation of a myelin-specific contrast agent for magnetic resonance imaging of myelination in central nervous system
Bioorganic & Medicinal Chemistry ( IF 3.5 ) Pub Date : 2023-03-21 , DOI: 10.1016/j.bmc.2023.117257
Bin Wei 1 , Na Weng 2 , Lei Fu 1 , Yuxuan Li 1 , Xu Wang 2 , Ruijuan Yin 3 , Tao Jiang 4
Affiliation  

Demyelination exists in many neurological diseases of nervous system, such as stroke. Currently, magnetic resonance imaging (MRI) has been the main tool for diagnosing and monitoring the myelin related diseases. However, the conventional MRI unable to distinguish demyelinating lesions from other inflammatory lesions. To address this problem, we have designed and prepared a myelin specific magnetic resonance contrast agent, Gd-DTDAS, which was based myelin specific moiety MeDASg and Gd-DTPAh. In this work, we verified the specificity and sensitivity of Gd-DTDAS to myelin. Moreover, we investigated the specific binding ability of Gd-DTDAS to myelin sheath in the MCAO micei models. The in vivo imaging results showed that Gd-DTDAS can bind to the undamaged myelin sheath in the BBB disruption areas, and in turn reduce the relaxation time. The fluorescence images also showed significant fluorescence in the brain right infarct area of the MCAO model mice with administration of Gd-DTDAS. The above results confirmed that Gd-DTDAS could be preferentially distributed in areas with high myelination and can detect focally induced demyelination.



中文翻译:

用于中枢神经系统髓鞘形成磁共振成像的髓鞘特异性造影剂的合成及生物活性评价

脱髓鞘存在于中风等神经系统的许多神经系统疾病中。目前,磁共振成像(MRI)已成为诊断和监测髓鞘相关疾病的主要工具。然而,传统的 MRI 无法区分脱髓鞘病变与其他炎症病变。为了解决这个问题,我们设计并制备了一种髓鞘特异性磁共振造影剂 Gd-DTDAS,它基于髓鞘特异性部分 MeDAS g和 Gd-DTPA h。在这项工作中,我们验证了 Gd-DTDAS 对髓磷脂的特异性和敏感性。此外,我们研究了 Gd-DTDAS 与 MCAO 小鼠髓鞘的特异性结合能力楷模。体内成像结果表明,Gd-DTDAS 可以与 BBB 破坏区域未受损的髓鞘结合,进而减少弛豫时间。荧光图像还显示在给予 Gd-DTDAS 的 MCAO 模型小鼠的大脑右侧梗塞区域中有明显的荧光。上述结果证实 Gd-DTDAS 可以优先分布在髓鞘形成高的区域,并且可以检测局灶性脱髓鞘。

更新日期:2023-03-21
down
wechat
bug