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放射性标记白藜芦醇负载金纳米粒子(Tc-Res-AuNP)在结肠癌组织中的生理性摄取和滞留。

Physiological uptake and retention of radiolabeled resveratrol loaded gold nanoparticles (Tc-Res-AuNP) in colon cancer tissue.

机构信息

Centre for Nuclear Medicine, Panjab University, Chandigarh, 160014, India.

Department of Biophysics, Panjab University, Chandigarh, 160014, India.

出版信息

Nanomedicine. 2018 Apr;14(3):1059-1071. doi: 10.1016/j.nano.2018.01.008. Epub 2018 Jan 31.

Abstract

When tagged with a suitable radionuclide, the cancer targeting properties of trans-resveratrol could be utilized to locate cancerous sites in the body using radionuclide imaging technique. However, the polyphenol due to its rapid and extensive metabolism exhibits low bioavailability in vivo. The study was designed to enhance the cancer targeting efficacy of radiolabeled resveratrol using nano-based technology. Technetium-99m labeled resveratrol loaded gold nanoparticles (Res-AuNP) were synthesized, characterized and evaluated for their cancer targeting efficacy in HT29 colon cancer cells and in animal cancer model. Results of various investigations were compared to corresponding results obtained for Tc-AuNP and Tc-resveratrol. Cancer cell internalization observed for Tc-Res-AuNP was significantly higher than that of Tc-AuNP and Tc-resveratrol. Also, a gradual rise in target to nontarget uptake with time was observed following i.v. administration of Tc-Res-AuNP to colon tumor bearing rats, demonstrating better in vivo targeting of colon adenocarcinoma with Tc-Res-AuNP when compared to Tc-resveratrol.

摘要

当与合适的放射性核素标记时,trans-resveratrol 的癌症靶向特性可以利用放射性核素成像技术来定位体内的癌症部位。然而,由于多酚的快速广泛代谢,其在体内的生物利用度较低。本研究旨在利用基于纳米技术提高放射性标记白藜芦醇的癌症靶向效果。合成、表征并评价了负载金纳米粒子的锝-99m 标记白藜芦醇(Res-AuNP)在 HT29 结肠癌细胞和动物癌症模型中的癌症靶向效果。将各种研究的结果与相应的 Tc-AuNP 和 Tc-resveratrol 的结果进行了比较。Tc-Res-AuNP 的癌细胞内化明显高于 Tc-AuNP 和 Tc-resveratrol。此外,静脉注射 Tc-Res-AuNP 后,在荷结肠癌大鼠中观察到随着时间的推移,目标到非目标摄取逐渐增加,表明与 Tc-resveratrol 相比,Tc-Res-AuNP 对结肠腺癌的体内靶向性更好。

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