Tumor-selective macromolecular MRI contrast agents

摘要

Tumor-selective macromolecular ligands containing 5-(p-Carbonyloxyphenyl)-10,15,20-triphenylporphyrin(HPTP) moiety (PHEA-DTPA-HPTP and PAEA-DTPA-HPTP) were prepared by the incorporation of diethylenetriaminepentaacetic acid (DTPA) and 5-(p-hydroxylphenyl)-10,15,20-triphenylporphyrin(HPTP) as the tumor-selective group in poly[#alpha#,#beta#-(N-(2-hydroxyethyl)-L-aspartamide)](PHEA) and poly-(#alpha#,#beta#-(N-(2-hydroxyethyl)-L-aspartamide)](PAEA).These ligands were further complexed with gadolinium chloride to form two tumor-selective macromolecular MRI contrast agents PHEA-Gd-DTPA-HPTP and PAEA-Gd-DTPA-HPTP.Relaxivity studies showed that both the polyaspartamide-gadolinium complexes possess higher relaxation effectiveness than that of the clinically used Gd-DTPA.Magnetic resonance imaging of tumors in mice indicated that these two polyaspartamide MRI contrast agents containing 5-9p-Carbonlyoxyphenyl)-10,15,20-triphenylporphyrin moiety cansignificanltyenhance the contrast MRIs of Hepatoma (H_(22)) and Ehrlich ascites carcinoma after injection and are takenup selectively by these cancers in mice.