Department of Thyroid Surgery, The First Hospital of Jilin University, 71 Xinmin Street, Changchun, Jilin 130021, P. R. China.
Org Biomol Chem. 2018 Feb 28;16(9):1591-1597. doi: 10.1039/c7ob03108d.
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.
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。