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基于甘草次酸修饰卟啉的纳米粒子用于癌症的光动力疗法。

Nanoparticles based on glycyrrhetinic acid modified porphyrin for photodynamic therapy of cancer.

机构信息

Department of Thyroid Surgery, The First Hospital of Jilin University, 71 Xinmin Street, Changchun, Jilin 130021, P. R. China.

出版信息

Org Biomol Chem. 2018 Feb 28;16(9):1591-1597. doi: 10.1039/c7ob03108d.

Abstract

Self-assembled small molecules, as a novel form of drug presentation, have splendid capabilities for water stability and cell endocytosis. Photodynamic therapy (PDT) is regarded as a promising cancer treatment because it is less invasive and has fewer side effects. In this work, an amphiphilic glycyrrhetinic acid-porphyrin conjugate (TPP-GA) was designed and synthesized, and this could self-assemble into nanoparticles (TPP-GA NPs) in water. The morphology of the TPP-GA NPs was observed using transmission electron microscopy (TEM) and their stability in water was revealed by dynamic light scattering (DLS). The PDT effect of the TPP-GA NPs was confirmed by means of in vitro experiment, after photostability verification. It could be conceived that the application of TPP-GA NPs for PDT is a feasible choice and this work shows progress in the self-assembly of amphiphilic small organic molecules.

摘要

自组装小分子作为一种新的药物递呈形式,具有出色的水稳定性和细胞内吞能力。光动力疗法(PDT)被认为是一种有前途的癌症治疗方法,因为它的侵入性较小,副作用也较少。在这项工作中,设计并合成了一种两亲性甘草次酸-卟啉偶联物(TPP-GA),它可以在水中自组装成纳米颗粒(TPP-GA NPs)。通过透射电子显微镜(TEM)观察 TPP-GA NPs 的形态,并通过动态光散射(DLS)揭示其在水中的稳定性。经过光稳定性验证后,通过体外实验证实了 TPP-GA NPs 的 PDT 效应。可以想象,TPP-GA NPs 用于 PDT 的应用是一个可行的选择,这项工作展示了两亲性小分子自组装的进展。

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