This work reports the synthesis, radiolabeling and preliminary biodistribution results in tumor-bearing mice of the 99mTc(CO)3–AOPA colchicine conjugate. The novel ligand was successfully synthesized by conjugation of N-(acetyloxy)-2-picolylamino (AOPA) to deacetylcolchicine via a short carbonyl-methylene linker. Radiolabeling was performed
in high yield with [99mTc(CO)3]+ core. 99mTc(CO)3–AOPA colchicine conjugate was hydrophilic and was stable at room temperature. Biodistribution studies in tumor-bearing mice
showed that 99mTc(CO)3–AOPA colchicine conjugate accumulated in the tumor with good uptake and retention. However, its clearance from normal organs
was not so fast, resulting in poor T/NT ratios. Further modification on the linker or/and 99mTc-chelate to improve the tumor targeting efficacy and in vivo kinetic profiles is currently in progress.
Authors:Xiaobei Zheng, Feng Dong, Jing Yang, Xiaojiang Duan, Tingting Niu, Wangsuo Wu, and Jianjun Wang
This work reports the synthesis and preliminary biodistribution results of [131I]SIB-PEG4-CHC in tumor-bearing mice. The tributylstannyl precursor ATE-PEG4-CHC was synthesized by conjugation of ATE to amino pegylated colchicine NH2-PEG4-CHC. [131I]SIB-PEG4-CHC was radiosynthesized by electrophilic destannylation of the precursor with a yield of ~44%. The radiochemical purity
(RCP) appeared to be >95% by a Sep-Pak cartridge purification. [131I]SIB-PEG4-CHC was lipophilic and was stable at room temperature. Biodistribution studies in tumor-bearing mice showed that [131I]SIB-PEG4-CHC cleared from background rapidly, and didn’t deiodinate in vivo. However, the poor tumor localization excluded it from
further investigations as a tumor-targeted radiopharmaceuticals.
Authors:Giseli Aparecida Bernabé, S. Almeida, C. A. Ribeiro, and M. S. Crespi
The presence of colchicines (N-[(7S)-1,2,3,10-tetramethoxy-9-oxo-6,7-dihydro-5H-benzo[a]heptalen-7-yl] acetamide) and its derivative (N-acetil colchinol methyl ether) was identified that is the most used alkaloid
Authors:Ke Ren, Tiantian Feng, Hai Shi, Jianshe Ma, and Yongxi Jin
. Narciclasine does not affect the activity of proteases in vitro, but inhibits the synthesis of proteases at the ribosome level. Narciclasine is described as an anti-mitotic substance similar to colchicine. Narciclasine is also an inhibitor of peptide bond