Functional L-lysine dendritic macromolecules as liver-imaging probes.
Liver-imaging probes are prepared through the conjugation of Gd chelates and galactosyl moieties to peptide dendrimers. The dendritic probes possessing highly controlled structures and a single molecular weight have a two-fold increase in T(1) relaxivity to 9.1 x 10(3) (Gd M)(-1) s(-1) compared to Gd-DTPA. No obvious cytotoxicity of this multifunctional dendritic agent is discovered in vitro. The dendrimer bearing galactosyl moieties leads to a much-higher hepatocyte-cell uptake in vitro and provides good signal-intensity enhancement (35%) of mouse liver in vivo especially at 60 min after intravenous injection. In comparison, non-targeting Gd dendrimers provide only an 11% enhancement of imaging contrast at the same time point. Overall, the dendrimers bearing galactosyl moieties may be used as liver-imaging probes.
Luo
Kui
K
National Engineering Research Center for Biomaterials, Sichuan University, Chengdu 610064, PR China.
Liu
Gang
G
Zhang
Xiaowei
X
She
Wenchuan
W
He
Bin
B
Nie
Yu
Y
Li
Li
L
Wu
Yao
Y
Zhang
Zhirong
Z
Gong
Qiyong
Q
Gao
Fabao
F
Song
Bin
B
Ai
Hua
H
Gu
Zhongwei
Z
D000818:Animals; D050091:Dendrimers / Q000378:metabolism*; D008099:Liver / Q000378:metabolism*; D008239:Lysine / Q000378:metabolism*; D008279:Magnetic Resonance Imaging; D009682:Magnetic Resonance Spectroscopy; D051379:Mice
D050091:Dendrimers; D008239:Lysine