Synthesis and bioevaluation of a 177Lu-labeled unsymmetrical cationic porphyrin derivative as a tumor targeting agent

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• 作者：Mohini Guleria ; Tapas Das…
• 关键词：Cationic porphyrin ; p ; NH2 ; benzyl ; DOTA ; 177Lu ; Fibrosarcoma ; Swiss mice
• 刊名：Journal of Radioanalytical and Nuclear Chemistry
• 出版年：2016
• 出版时间：February 2016
• 年：2016
• 卷：307
• 期：2
• 页码：1537-1544
• 全文大小：609 KB
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• 作者单位：Mohini Guleria (1)
  Tapas Das (1)
  Haladhar Dev Sarma (2)
  Sharmila Banerjee (1)
  
  1. Radiopharmaceuticals Chemistry Section, Radiochemistry and Isotope Group, Bhabha Atomic Research Centre, Trombay, Mumbai, 400 085, India
  2. Radiation Biology and Health Sciences Division, Bhabha Atomic Research Centre, Trombay, Mumbai, 400 085, India
  
• 刊物类别：Chemistry and Materials Science
• 刊物主题：Chemistry
  Nuclear Chemistry
  Physical Chemistry
  Nuclear Physics, Heavy Ions and Hadrons
  Diagnostic Radiology
  Inorganic Chemistry
  
• 出版者：Akad茅miai Kiad贸, co-published with Springer Science+Business Media B.V., Formerly Kluwer Academic
• ISSN：1588-2780

文摘

A cationic porphyrin derivative namely, 5-carboxymethyleneoxyphenyl-10,15,20-tri(p-N-methylpyridyl)porphyrin was synthesized and conjugated with a bi-functional chelating agent namely, p-NH₂-benzyl-DOTA (p-aminobenzyl-1,4,7,10-tetraazcyclododecane-1,4,7,10-tetraacetic acid). The porphyrin-p-NH₂-benzyl-DOTA conjugate was radiolabeled with 177LuCl₃ with a radiochemical purity of >95 %. Preliminary biological evaluation of the radiolabeled conjugate, carried out by bio-distribution studies in fibrosarcoma tumor bearing Swiss mice indicated rapid accumulation of the radiotracer in the tumor with fast clearance of the non-accumulated activity through renal pathway. However, the initially accumulated activity in the tumor exhibited fast clearance which could be attributed to its highly hydrophilic nature. Keywords Cationic porphyrin p-NH₂-benzyl-DOTA 177Lu Fibrosarcoma Swiss mice