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用于光动力疗法的水溶液中原卟啉IX性能的增强。

Enhancement of protoporphyrin IX performance in aqueous solutions for photodynamic therapy.

作者信息

Homayoni Homa, Jiang Ke, Zou Xiaoju, Hossu Marius, Rashidi Leila Hossein, Chen Wei

机构信息

Nano-Biophysics Lab, Department of Physics, University of Texas at Arlington, Arlington, TX 76019, USA; Joint Biomedical Engineering Program, University of Texas at Arlington, Arlington, TX 76019, USA; University of Texas Southwestern Medical Center, Dallas, TX 75235, USA.

Nano-Biophysics Lab, Department of Physics, University of Texas at Arlington, Arlington, TX 76019, USA.

出版信息

Photodiagnosis Photodyn Ther. 2015 Jun;12(2):258-66. doi: 10.1016/j.pdpdt.2015.01.003. Epub 2015 Jan 27.

Abstract

Molecular modification of protoporphyrin IX (PpIX) was conducted to improve its water solubility and therapeutic performance for photodynamic therapy. The carboxylic acid and the two nitrogen atoms in the core of PpIX molecule were protonated following by conjugation with 3-aminopropyl triethoxysilane (APTES). Then, folic acid (FA) was conjugated to the APTES-coated PpIX (MPpIX) through chemical bonding between FA and protonated PpIX. The results showed that APTES coating can stabilize PpIX and increase its water solubility. Consequently, this leads to the enhancement in luminescence and singlet oxygen production. Upon X-ray irradiation, singlet oxygen can be detected in the MPpIX but not in PpIX. This means that MPpIX can be used for deep cancer treatment as X-ray can penetrate deeply into tissue. Molecular modification also reduces the dark toxicity of PPIX and increases their cell uptake. All these traits indicate that the Molecular modification of PpIX may potentially improve the efficacy of photodynamic therapy for cancer treatment.

摘要

对原卟啉IX(PpIX)进行了分子修饰,以提高其水溶性和光动力疗法的治疗性能。将PpIX分子核心中的羧酸和两个氮原子质子化,随后与3-氨丙基三乙氧基硅烷(APTES)共轭。然后,通过叶酸(FA)与质子化的PpIX之间的化学键合,将叶酸(FA)与APTES包覆的PpIX(MPpIX)共轭。结果表明,APTES包覆可以稳定PpIX并增加其水溶性。因此,这导致发光和单线态氧产生增强。在X射线照射下,MPpIX中可检测到单线态氧,而PpIX中则检测不到。这意味着MPpIX可用于深部癌症治疗,因为X射线可以深入穿透组织。分子修饰还降低了PPIX的暗毒性并增加了它们的细胞摄取。所有这些特性表明,PpIX的分子修饰可能会提高癌症治疗光动力疗法的疗效。

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