Evaluation of the relationship between [¹⁸F]FDG and P-glycoprotein expression: an experimental study

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• 作者：Chunjing Yu^a ; ^b ; Weixing Wan^b ; Bin Zhang^c ; Shengming Deng^c ; Tzu-Chen Yen^d ; ^{yen1110@adm.cgmh.org.tw} ; Yiwei Wu^c ; ^{wuyiwei3988@gmail.com}
• 关键词：P-glycoprotein ; Rhodamine 123 ; [18F]FDG ; Bcap37/MDR1 ; Micro-PET
• 刊名：Nuclear Medicine and Biology
• 出版年：2012
• 期刊代码：43_09698051
• 类别：ph
• 出版时间：July, 2012
• 卷：39
• 期：5
• 页码：671-678
• 文件大小：901 K

摘要

Introduction

P-glycoprotein (P-gp) is a cell-membrane-associated protein that transports a variety of drug substrates. We sought to evaluate the relationship between 2-[¹⁸F]fluoro-2-deoxy-d-glucose ([¹⁸F]FDG) and P-gp expression using breast carcinoma Bcap37/multidrug resistant (MDR1) and Bcap37 in vitro and in vivo.

Methods

The function of P-gp expressed in Bcap37/MDR1 cells was evaluated using verapamil (VER), a classical inhibitor of P-gp. The accumulation of ^99mTc-methoxyisobutylisonitrile ([^99mTc]MIBI) in vitro was measured. In vivo imaging of severe combined immune deficiency (SCID) mice implanted with Bcap37 and Bcap37/MDR1 cells was performed by scintigraphy and micro-positron emission tomography (PET).

Results

The uptake of [^99mTc]MIBI was 0.62%卤0.05%in the Bcap37/MDR1 cells and 2.02%卤0.28%in the Bcap37 cells. VER significantly increased the uptake of [^99mTc]MIBI in the Bcap37/MDR1 cells (1.90%卤0.09%) but not in the Bcap37 cells (2.15%卤0.27%). In vivo, neither the Bcap37 nor Bcap37/MDR1 tumors grown in the SCID mice could be detected by [^99mTc]MIBI scintigraphy. Both the Bcap37 and Bcap37/MDR1 tumors were visible by micro-PET. The mean standardized uptake value (SUV) was significantly higher in the Bcap37 tumors (1.00卤0.06) than in the Bcap37/MDR1 (0.67卤0.11) tumors. VER significantly increased the mean SUV in the Bcap37/MDR1 tumors (1.02卤0.16) but not in the Bcap37 tumors (1.09卤0.22).

Conclusions

[¹⁸F]FDG combined with VER may be an effective noninvasive method of determining P-gp expression in tumors.