Theranostic Polyaminocarboxylate-Cyanine-Transferrin Conjugate for Anticancer Therapy and Near-Infrared Optical Imaging.
Theranostic Polyaminocarboxylate-Cyanine-Transferrin Conjugate for Anticancer Therapy and Near-Infrared Optical Imaging.
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用于抗癌治疗和近红外光学成像的治疗诊断聚氨基羧酸盐-花青-转铁蛋白缀合物。
DOI：
10.1002/cmdc.201600072
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发表时间：
2016-10-06
期刊：
影响因子：
3.4
通讯作者：
Chong, Hyun-Soon
中科院分区：
文献类型：
--
作者：
Kang, Chi Soo;Ren, Siyuan;Sun, Xiang;Chong, Hyun-Soon
使用铁络合剂去铁剂已被认为是一种很有前途的抗肿瘤治疗策略。在此，我们报道了一种用于靶向铁络合癌症治疗和近红外光学成像的新型治疗药物。肿瘤靶向转铁蛋白与N-NE3TA和近红外荧光菁染料(Cy5.5)复合，形成肿瘤靶向转铁蛋白。将细胞毒性螯合剂与转铁蛋白(Tf)偶联，并对相应的NE3TA-Tf结合物在转铁蛋白受体(TFR)表达升高的HeLa、HT29和PC3癌细胞中的抗增殖活性进行了表征和评价。NE3TA-Tf结合物对HeLa、HT29和PC3等肿瘤细胞具有显著的抑制活性。将近红外染料Cy5.5负载到NE3TA-Tf平台上，显微镜下观察到细胞毒性和荧光转铁蛋白结合物(N-NE3TA-Tf-Cy5.5)进入TfR高表达的癌细胞。医用结合物(N-NE3TA-Tf-Cy5.5)在靶向铁络合肿瘤治疗和近红外荧光(NIRF)成像方面具有潜在的应用前景。
Iron depletion using iron chelating agents has been recognized as a promising anti-tumor therapeutic strategy. We herein report a novel theranostic agent for targeted iron chelation cancer therapy and near IR optical imaging. The theranostic agent was prepared via incorporation of a polyaminocarboxylated-based cytotoxic chelating agent (N-NE3TA) and a near IR fluorescent cyanine dye (Cy5.5) into a tumor targeting transferrin. The cytotoxic chelating agent was conjugated to transferrin (Tf), and the corresponding NE3TA-Tf conjugate was characterized and evaluated for anti-proliferative activity in HeLa, HT29, and PC3 cancer cells with elevated expression of transferrin receptor (TfR). The NE3TA-Tf conjugate displayed significant inhibitory activity against cancer cells (HeLa, HT29, and PC3). The near IR dye Cy5.5 was loaded into the NE3TA-Tf platform, and the cytotoxic and fluorescent transferrin conjugate (N-NE3TA-Tf-Cy5.5) was microscopically shown to enter the TfR over-expressing cancer cells. The theranostic conjugate (N-NE3TA-Tf-Cy5.5) has a potential application for dual use in targeted iron chelation cancer therapy and near IR fluorescence (NIRF) imaging.
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影响因子：
3.9
作者：
Kang, Chi Soo;Wu, Ningjie;Chong, Hyun-Soon
通讯作者：
Chong, Hyun-Soon
影响因子：
24.5
作者：
Brookes, M. J.;Hughes, S.;Tselepis, C.
通讯作者：
Tselepis, C.
影响因子：
6.6
作者：
KEER, HN;KOZLOWSKI, JM;GRAYHACK, JT
通讯作者：
GRAYHACK, JT
影响因子：
4.7
作者：
MUJUMDAR, RB;ERNST, LA;WAGGONER, AS
通讯作者：
WAGGONER, AS
影响因子：
4.9
作者：
Chong, Hyun-Soon;Song, Hyun A.;Mhaske, Santosh B.
通讯作者：
Mhaske, Santosh B.