Synthesis and preliminary biological studies of the novel conjugate 188Re-labeled meso-tetrakis(4-sulfophenyl)porphyrin in mice.

Abstract

OBJECTIVE:

The objective of this study was to evaluate the biological behaviors of a novel (188)Re-labeled meso-tetrakis(4-sulfophenyl)porphyrin (TPPS(4)) in normal mice and tumor-bearing mice.

METHODS:

TPPS(4) was synthesized and labeled by (188)ReO(4)(-). Normal KM mice and BALB/c nude mice bearing melanoma or hepatoma were prepared for distribution studies.

RESULTS:

The [(188)Re]TPPS(4) yield was >98% with a specific activity of 11.2 GBq/mol, and vitamin C could increase its stability in vitro. In normal KM mice, [(188)Re]TPPS(4) had a fast blood clearance ( approximately 90%, 24 h postinjection), low retention in vital organs and hepatotropic characteristics. In nude mice, uptakes of >4.1% and 6.5% ID/g tumor at 8 h postinjection were observed in melanoma and hepatoma, respectively; this remained at high levels of 4.7% and 5.7%, respectively, after 24 h. At 8 h, the tumor/blood and tumor/muscle ratios in melanoma-bearing and hepatoma-bearing mice were 6.2-15.2 and 6.1-24.2, respectively. Twenty-four hours later, these high ratios still continued at 8.6-22.1 and 12-26.1, respectively.

CONCLUSION:

The results obtained in this study indicate that [(188)Re]TPPS(4) has a high tumor affinity and retainable accumulation characteristics in carcinoma, which can potentially be used for tumor-targeted therapy.

• Authors: Zhiyun Jia, Houfu Deng, Manfei Pu
• Journal: Nuclear medicine and biology (Nucl Med Biol) Vol. 34 Issue 6 Pg. 643-9 (Aug 2007) ISSN: 0969-8051 [Print] United States
• PMID: 17707804 (Publication Type: Journal Article)

Chemical References

• Indicators and Reagents
• Metalloporphyrins
• Radioisotopes
• Radiopharmaceuticals
• rhenium tetrakis(4-sulfophenyl)porphyrin
• Rhenium

Topics

• Animals
• Chromatography, High Pressure Liquid
• Hydrogen-Ion Concentration
• Indicators and Reagents
• Isotope Labeling
• Liver Neoplasms, Experimental (metabolism)
• Melanoma, Experimental (metabolism)
• Metalloporphyrins (chemical synthesis)
• Mice
• Mice, Inbred BALB C
• Mice, Nude
• Radioisotopes
• Radiopharmaceuticals (chemical synthesis)
• Rhenium
• Tissue Distribution