Department of Cancer Imaging and Metabolism, H. Lee Moffitt Cancer Center & Research Institute, Tampa, FL 33612, USA.
Bioorg Med Chem Lett. 2013 Apr 1;23(7):2061-4. doi: 10.1016/j.bmcl.2013.02.008. Epub 2013 Feb 13.
A scaffold bearing eight terminal alkyne groups was synthesized from sucrose, and copies of an azide-terminated Gd-DOTA complex were attached via copper(I)-catalyzed azide-alkyne cycloaddition. The resulting contrast agent (CA) was administered by gavage to C3H mice. Passage of the CA through the gastrointestinal (GI) tract was followed by T1-weighted magnetic resonance imaging (MRI) over a period of 47h, by which time the CA had exited the GI tract. No evidence for leakage of the CA from the GI tract was observed. Thus, a new, orally administered CA for MRI of the GI tract has been developed and successfully demonstrated.
一种带有 8 个末端炔基的支架是由蔗糖合成的,通过铜(I)催化的叠氮-炔环加成反应将末端叠氮化物的 Gd-DOTA 复合物连接到支架上。通过灌胃将得到的造影剂(CA)给予 C3H 小鼠。通过 T1 加权磁共振成像(MRI)在 47 小时的时间内监测 CA 通过胃肠道(GI)的过程,此时 CA 已经离开 GI 道。未观察到 CA 从 GI 道泄漏的迹象。因此,开发了一种新的、可口服的用于胃肠道 MRI 的 CA,并成功进行了验证。