Synthesis and Physicochemical Characterization of the DO3A-betaG and Their Complexes with Lanthanides(III) ions

• Main Authors: Yu-Zheng Su, 蘇育正
• Other Authors: 王雲銘
• Format: Others
• Language: zh-TW
• Published: 2006
• Online Access: http://ndltd.ncl.edu.tw/handle/63630821426652155700

碩士 === 高雄醫學大學 === 醫藥暨應用化學研究所碩士班 === 94 === In this study, a beta-glucuronic acid-containing ligand DO3A-betaG and a modified enzyme-cleaved ligand HE-DO3A, was designed, synthesized and characterized. [Gd(DO3A-betaG)] was incubated with beta-glucuronidase (betaG) and detected the enzyme-cleavage behavior of [Gd(DO3A-beta G)]. The betaG cleaved beta-glucuronic acid residue of [Gd(DO3A-betaG)] in 360 mins and detected by HPLC fluorescence detector. The number of inner-sphere water of [Gd(DO3A-betaG)] and [Gd(HE-DO3A)] was obtained, through the Dy3+-induced 17O water NMR shifts experiments and chemical-luminescence method. The number of inner sphere water is significantly increased from q=0.49 to 1.46. Relaximetric studies shows that the T1 value of [Gd(DO3A-betaG)]?ndecreases about 25% in the presence of betaG and proves that the q value of [Gd(DO3A-betaG)] increased in the presence of betaG. The 17O NMR experiments were conducted to estimate the water exchange rate kex298 and rotational correctional time 298?豩. The value of [Gd(DO3A-betaG)] is 52.3?e106 s?{1 and significantly higher than those of [Gd(DOTA)]?n?{ and [Gd(DTPA)]2?{?nbut slightly lower than those of [Gd(TTDA-beta-GP)]2?{?nand?n[Gd(TTDA)]2?{. The rotational correctional time value of [Gd(DO3A-FPG)] is 173 ps and similar to [Gd(TTDA-beta-GP)]2?{. [Gd(DO3A-betaG)] is potentially suitable as bio-activated MRI contrast agents.