细胞凋亡显像剂^(99)Tc^m-HYNIC-Annexin Ⅴ的制备及其生物评价

Preparation and Evaluation of ^(99)Tc^m-HYNICAnnexin Ⅴ for Apoptosis Imaging

合成了双功能螯合剂琥珀酰亚胺-6-肼基吡啶-3-甲酸(HYNIC)。并将HYNIC成功地应用于AnnexinⅤ的偶连和标记中。结果表明:每个AnnexinⅤ的蛋白分子能偶连2个HYNIC,标记率为98%,标记物的放化纯度在6 h后仍然>95%;99Tcm-HYNIC-AnnexinⅤ在动物模型中能有效检测细胞凋亡。因此,99Tcm-HYNIC-AnnexinⅤ有望成为检测肿瘤治疗效果的显像剂。

Bifunctional chelating agent succinimidyl 6 tert-boc-hydrazinopyridine-3-carboxylic acid（HYNIC） is synthesized and successfully applied in the conjugating and radiolabeling of annexin V. One molecular of annexin V is conjugated with two molecular of HYNIC. The labeling ratio of the labeled compound is 98~, and the radiochemical purity of 95% is remained after 6 h. ^99Tc^m-HYNIC Annexin V has heen successfully evaluated in animal models and the results show that the cell apoptosis can be assaied by which.