一种用于硼中子俘获治疗的含双酚 A-肽共轭物新型脂质体的合成与评价
Synthesis and evaluation of a novel liposome containing BPA-peptide conjugate for BNCT.
作者信息
Shirakawa Makoto, Yamamto Tetsuya, Nakai Kei, Aburai Kenichi, Kawatobi Sho, Tsurubuchi Takao, Yamamoto Yohei, Yokoyama Yuusaku, Okuno Hiroaki, Matsumura Akira
机构信息
Department of Graduate School of Comprehensive Human Sciences, Faculty of Functional and Regulatory Medical Sciences, University of Tsukuba, Japan.
出版信息
Appl Radiat Isot. 2009 Jul;67(7-8 Suppl):S88-90. doi: 10.1016/j.apradiso.2009.03.101. Epub 2009 Apr 1.
We aimed at securing sufficient concentrations of (10)B in boron neutron capture therapy (BNCT) by developing a new drug delivery system. We have designed and developed a novel lipid analog and succeeded in using it to develop the new boron component liposome. It consisted of three different kinds of amino acid derivatives and two fatty acids, and could react directly with the peptide synthesized first on resin by Fmoc solid-phase synthesis. In this study, lipid analog conjugated with HIV-TAT peptide (domain of human immunodeficiency virus TAT protein) and boronophenylalanine (BPA) was synthesized and successfully incorporated into liposomes.
我们旨在通过开发一种新的药物递送系统，在硼中子俘获疗法（BNCT）中确保足够浓度的硼-10。我们设计并开发了一种新型脂质类似物，并成功地用它开发了新的硼成分脂质体。它由三种不同的氨基酸衍生物和两种脂肪酸组成，并且可以通过Fmoc固相合成法直接与首先在树脂上合成的肽反应。在本研究中，合成了与HIV-TAT肽（人类免疫缺陷病毒TAT蛋白的结构域）和硼苯丙氨酸（BPA）缀合的脂质类似物，并成功地将其掺入脂质体中。
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