Micro-PET imaging of β-glucuronidase activity by the hydrophobic conversion of a glucuronide probe

Shey Cherng Tzou, Steve Roffler, Kuo Hsiang Chuang, Hsin Pei Yeh, Chien Han Kao, Yu Cheng Su, Chiu Min Cheng, Wei Lung Tseng, Jentaie Shiea, I. Hong Harm, Kai Wen Cheng, Bing Mae Chen, Jeng Jong Hwang, Tian Lu Cheng, Hsin Ell Wang

Research output: Contribution to journalArticlepeer-review

17 Citations (Scopus)


Purpose: To develop a new glucuronide probe for micro-positron emission topography (PET) that can depict β-glucuronidase (βG)-expressing tumors in vivo. Materials and Methods: All animal experiments were preapproved by the Institutional Animal Care and Use Committee. A βG-specific probe was generated by labeling phenolphthalein glucuronide (PTH-G) with iodine 131 (131I) or 124I. To test the specificity of the probe in vitro, 124I-PTH-G was added to CT26 and βG-expressing CT26 (CT26/βG) cells. Mice bearing CT26 and CT26/βG tumors (n = 6) were injected with 124I-PTH-G and subjected to micro-PET imaging. A βG-specific inhibitor D-saccharic acid 1,4-lactone monohydrate was used in vitro and in vivo to ascertain the specificity of the glucuronide probes. Finally, the biodistributions of the probes were determined in selected organs after injection of 131I-PTH-G to mice bearing CT26 and CT26/βG tumors (n = 14). Differences in the radioactivity in CT26 and CT26/βG tumors were analyzed with the Wilcoxon signed rank test. Results: 124I-PTH-G was selectively converted to 124I-PTH (phenolphthalein), which accumulated in CT26/βG cells and tumors in vitro. The micro-PET images demonstrated enhanced activity in CT26/βG tumors resulting from βG-mediated conversion and trapping of the radioactive probes. Accumulation of radioactive signals was 3.6-, 3.4-, and 3.3-fold higher in the CT26/βG tumors than in parental CT26 tumors at 1, 3, and 20 hours, respectively, after injection of the probe (for all the three time points, P < .05). Conclusion: Hydrophilic-hydrophobic conversion of 124I-PTH-G probe can aid in imaging of βG-expressing tumors in vivo.

Original languageEnglish
Pages (from-to)754-762
Number of pages9
Issue number3
Publication statusPublished - Sept 2009
Externally publishedYes

ASJC Scopus subject areas

  • Radiology Nuclear Medicine and imaging


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