Boronated metalloporphyrins: a novel approach to the diagnosis and treatment of cancer using contrast-enhanced MR imaging and neutron capture therapy.

Porphyrins are a unique class of metal chelating agents that have shown specific affinity for neoplasms. The water-soluble free-base derivative, tetrakiscarborane carboxylate ester of 2,4-(alpha,beta-dihydroxyethyl) deuteroporphyrin IX (BOPP), an agent designed for neutron capture therapy, has previously demonstrated selective localization and retention in a C6 murine glioma. In the present work, the authors demonstrate that the manganese chelate of BOPP also selectively localizes in a rat 9L gliosarcoma and preferentially enhances the tumor-normal brain contrast of T1-weighted images for at least 92 hours. The data indicate a maximal enhancement of contrast between tumor and normal brain at 24 hours after injection, compared with 5 minutes for manganese (III) tetraphenylporphine sulfonate (TPPS4). The results also indicate that Mn-BOPP may have a slower uptake in the 9L glioma than Mn-TPPS4 but a longer retention in the tumor. Mn-BOPP is unique in that it represents, to the authors' knowledge, the first example of a single agent that can enhance contrast between tumor and normal tissue and be potentially effective as an agent for boron neutron capture therapy.
AuthorsL R Huang, R M Straubinger, S B Kahl, M S Koo, J J Alletto, R Mazurchuk, R I Chau, S L Thamer, R J Fiel
JournalJournal of magnetic resonance imaging : JMRI (J Magn Reson Imaging) 1993 Mar-Apr Vol. 3 Issue 2 Pg. 351-6 ISSN: 1053-1807 [Print] UNITED STATES
PMID8448397 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Research Support, U.S. Gov't, P.H.S.)
Chemical References
  • 2,4-(alpha,beta-dihydroxyethyl)deuteroporphyrin IX tetrakiscarborane carboxylate ester
  • Boron Compounds
  • Deuteroporphyrins
  • Metalloporphyrins
  • manganese(III)tetraphenylporphine sulfonate
  • Animals
  • Boron Compounds (therapeutic use)
  • Boron Neutron Capture Therapy
  • Brain Neoplasms (diagnosis, radiotherapy)
  • Deuteroporphyrins (therapeutic use)
  • Metalloporphyrins
  • Rats
  • Rats, Inbred F344
  • Tumor Cells, Cultured

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