Radiosynthesis and biological evaluation of 166Ho labeled methoxylated porphyrins as possible therapeutic agents
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166Ho labeled 5,10,15,20-tetrakis(3,4-dimethoxyphenyl) porphyrin, and 5,10,15,20-tetrakis(3,4,5-trimethoxyphenyl) porphyrin ([166Ho]–TDMPP and [166Ho]–TTMPP respectively) were prepared with acceptable radiochemical purity and specific activities. Stability and partition coefficient of the complexes were determined in the final formulations and biodistribution studies in mouse demonstrated high accumulation of [166Ho]–TDMPP in the lung and liver and less excretion through the kidney. while [166Ho]–TTMPP was mostly excreted into intestines and kidneys while lungs were a minor accumulation site. In contrast to other reported radiolanthanide labeled porphyrins these two complexes showed less liver accumulation. Further investigation of their potential therapeutic properties is of interest.
KeywordsMethoxylated porphyrins 166Ho Biodistribution Cancer therapy
Authors wish to thank Deputy of the Research of Tehran University of Medical Sciences for the financial support of this project and also special thanks to Mr M. Mazidi for performing animal studies as well as Dr. M. Erfani and Ms. F. Bolouroinovin for performing analytical experiments.
- 2.Chakraborty S, Das T, Banerjee S, Sarma HD, Venkatesh M (2007) Preparation and preliminary biological evaluation of a novel 109Pd labeled porphyrin derivative for possible use in targeted tumor therapy. Q J Nucl Med Mol Imaging 15:16–23Google Scholar
- 5.Bhadwal M, Mittal S, Das T, Sarma HD, Chakraborty S, Banerjee S, Pillai MR (2013) Synthesis and biological evaluation of 177Lu–DOTA–porphyrin conjugate: a potential agent for targeted tumor radiotherapy. Q J Nucl Med Mol Imaging (Epub ahead of print)Google Scholar
- 9.Falk JE (1975) Porohyrins and metalloporphyrins. Elsevier Science Publishing, New YorkGoogle Scholar
- 10.Manual for reactor produced radioisotopes, IAEA, Vienna, 2003, IAEA-TECDOC-1340, ISBN 92-0-101103-2, ISSN 1011-4289, ©IAEA, 2003, pp.71, Printed by the IAEA in Austria, January 2003Google Scholar
- 13.Tovmasyan AG, Rajic Z, Spasojevic I, Reboucas JS, Chen X, Salvemini D, Sheng H, Warner DS, Benov L, Batinic-Haberle I (2011) Methoxy-derivatization of alkyl chains increases the in vivo efficacy of cationic Mn porphyrins. Synthesis, characterization, SOD-like activity, and SOD-deficient E. coli study of meta Mn(III) N-methoxyalkylpyridylporphyrins. Dalton Trans 40(16):4111–4121CrossRefGoogle Scholar
- 17.Fazaeli Y, Jalilian AR, Amini MM, Aboudzadeh M, Feizi S, Rahiminezhad A, Yousefi K (2013) Preparation, nano purification, quality control and labelingoptimization of [64Cu]-5,10,15,20-tetrakis (penta fluoro phenyl) porphyrin complex as a possible imaging agent. J Radioanal Nucl Chem 295:255–263CrossRefGoogle Scholar
- 18.Utsumi T, Kobuchi H, Moriya K, Ogino T, Fujita H, Inoue K, Shuin T, Yasuda T, Utsumi K (2012) Mitochondrial localization of ABC transporter ABCG2 and its function in 5-aminolevulinic acid-mediated protoporphyrin IX accumulation. PLoS ONE 7(11):e50082. doi: 10.1371/journal.pone.0050082 CrossRefGoogle Scholar
- 19.Paknafas A, Fazaeli Y, Jalilian AR, Ahmadi A, Feizi S, Kamalidehghan M, Rahiminejad A, Khalaj A (2013) Radiosynthesis and quality control of [67Ga]-3,4-dimethoxylated porphyrin complex as a possible imaging agent. Iran J Pharm Res 12(4):735–744Google Scholar