近红外荧光团对骨特异性成像的电荷和疏水性效应。
Charge and hydrophobicity effects of NIR fluorophores on bone-specific imaging.
作者信息
Bao Kai, Nasr Khaled A, Hyun Hoon, Lee Jeong Heon, Gravier Julien, Gibbs Summer L, Choi Hak Soo
机构信息
1. Division of Hematology/Oncology, Department of Medicine, Beth Israel Deaconess Medical Center and Harvard Medical School, Boston, MA 02215; ; 2. Key Laboratory of Structure-based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang, China, 110016;
1. Division of Hematology/Oncology, Department of Medicine, Beth Israel Deaconess Medical Center and Harvard Medical School, Boston, MA 02215; ; 3. Advanced Imaging Research Center, The University of Texas Southwestern Medical Center, Dallas, TX 75390;
出版信息
Theranostics. 2015 Mar 1;5(6):609-17. doi: 10.7150/thno.11222. eCollection 2015.
Recent advances in near-infrared (NIR) fluorescence imaging enabled real-time intraoperative detection of bone metastases, bone growth, and tissue microcalcification. Pamidronate (PAM) has been widely used for this purpose because of its high binding affinity toward bone and remarkable therapeutic effects. Herein we describe the development of a series of PAM-conjugated NIR fluorophores that varied in net charges and hydrophobicity, and compared their bone targeting efficiency, biodistribution, and blood clearance. Since the targeting moiety, PAM, is highly negatively charged but small, the overall in vivo bone targeting and biodistribution were mediated by the physicochemical properties of conjugated fluorophores.
近红外（NIR）荧光成像技术的最新进展使得在术中能够实时检测骨转移、骨生长和组织微钙化。帕米膦酸盐（PAM）因其对骨具有高结合亲和力和显著的治疗效果而被广泛用于此目的。在此，我们描述了一系列净电荷和疏水性不同的PAM共轭近红外荧光团的开发，并比较了它们的骨靶向效率、生物分布和血液清除率。由于靶向部分PAM带高度负电荷但体积小，因此体内整体骨靶向和生物分布由共轭荧光团的物理化学性质介导。
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