Dai Yunpeng, Yin Jipeng, Huang Yu, Chen Xueli, Wang Guodong, Liu Yajun, Zhang Xianghan, Nie Yongzhan, Wu Kaichun, Liang Jimin
Engineering Research Center of Molecular and Neuro Imaging of Ministry of Education & School of Life Science and Technology, Xidian University, Xi'an, Shaanxi 710071, China.
State Key Laboratory of Cancer Biology and Xijing Hospital of Digestive Diseases, Xijing Hospital, Fourth Military Medical University, Xi'an 710032, China.
Biomed Opt Express. 2016 Mar 4;7(4):1149-59. doi: 10.1364/BOE.7.001149. eCollection 2016 Apr 1.
We quantified molecular specificity of Cy5.5-GX1 in vivo with dynamic fluorescence imaging to better understand its kinetic properties. According to whether or not free GX1 was injected and when it was injected, twelve of BGC-823 xenografted mice were randomly divided into three groups and underwent a 60 minute dynamic fluorescence scanning. Combined with a principal-component analysis, the binding potential (Bp) of the probe was determined by both Logan graphical analysis with reference tissue model (GARTM) and Lammertsma simplified reference tissue model (SRTM). The sum of the pharmacokinetic rate constants (SKRC) was quantified by the Gurfinkel exponential model (GEXPM). Cy5.5-GX1 specifically targeted tumor both in vitro and in vivo. We obtained similar quantification results of Bp (GARTM Bp = 0.582 ± 0.2655, SRTM Bp = 0.618 ± 0.2923), and obtained a good linear relation between the Bp value and the SKRC value. Our results indicate that the SKRC value is more suitable for an early-stage kinetic data analysis, and the Bp value depicts kinetic characteristics under the equilibrium state. Dynamic fluorescence imaging in conjunction with various kinetic models are optimal tools to quantify molecular specificity of the Cy5.5-GX1 probe in vivo.
我们通过动态荧光成像在体内定量分析了Cy5.5-GX1的分子特异性，以更好地了解其动力学特性。根据是否注射游离GX1以及注射时间，将12只BGC-823异种移植小鼠随机分为三组，并进行了60分钟的动态荧光扫描。结合主成分分析，通过参考组织模型的Logan图形分析（GARTM）和Lammertsma简化参考组织模型（SRTM）确定探针的结合潜能（Bp）。通过Gurfinkel指数模型（GEXPM）对药代动力学速率常数之和（SKRC）进行定量分析。Cy5.5-GX1在体外和体内均能特异性靶向肿瘤。我们获得了相似的Bp定量结果（GARTM Bp = 0.582 ± 0.2655，SRTM Bp = 0.618 ± 0.2923），并且在Bp值和SKRC值之间获得了良好的线性关系。我们的结果表明，SKRC值更适合早期动力学数据分析，而Bp值描述了平衡状态下的动力学特征。动态荧光成像结合各种动力学模型是在体内定量分析Cy5.5-GX1探针分子特异性的最佳工具。
