Design and synthesis of fluorescence-labeled closo-dodecaborate lipid: its liposome formation and in vivo imaging targeting of tumors for boron neutron capture therapy

Design and synthesis of fluorescence-labeled closo-dodecaborate lipid: its liposome formation and in vivo imaging targeting of tumors for boron neutron capture therapy
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DOI:
10.1039/c1ob06500a
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发表时间:
2012-01-01
影响因子:
3.2
通讯作者:
Tachikawa, Shoji
Tachikawa, Shoji
中科院分区:
化学3区
文献类型:
--
作者:
Nakamura, Hiroyuki;Ueda, Noriko;Tachikawa, Shoji

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以(S)-(+)-1,2-异丙基甘油为手性原料合成荧光标记的近十二硼烷脂质(FL-SBL)。FL-SBL很容易积累到由DSPC、CH和DSPE-PEG-OMe通过插入后协议制备的聚乙二醇化的DSPC脂质体中。FL-SBL标记的dsc脂质体的硼浓度和荧光强度随着添加剂FL-SBL的增加而增加,最大发射波长出现在531 nm处。初步的荷瘤小鼠体内成像研究显示,fl - sbl标记的dsc脂质体被递送到肿瘤组织,但没有分布到缺氧区域。
The fluorescence-labeled closo-dodecaborane lipid (FL-SBL) was synthesized from (S)-(+)-1,2-isopropylideneglycerol as a chiral starting material. FL-SBL was readily accumulated into the PEGylated DSPC liposomes prepared from DSPC, CH, and DSPE-PEG-OMe by the post insertion protocol. The boron concentrations and the fluorescent intensities of the FL-SBL-labeled DSPC liposomes increased with the increase of the additive FL-SBL, and the maximum emission wavelength of the liposomes appeared at 531 nm. A preliminary in vivo imaging study of tumor-bearing mice revealed that the FL-SBL-labeled DSPC liposomes were delivered to the tumor tissue but not distributed to hypoxic regions.