title: Preparation, characterization and evaluation of (186) Re-idarubicin: a novel agent for diagnosis and treatment of hepatocellular carcinoma.
abstract: Hepatocellular carcinoma is a widely prevalent cancer, and hence, the development of radiopharmaceuticals for its management is an important issue. In the current investigation, the complexation of idarubicin with (186) Re was studied. Optimum labelling conditions were found to be 4 mg idarubicin, 1.5 mg stannous chloride dihydrate and ~70 MBq Re-186 at pH 7. The complex showed ~97.6% RCY value at 20 min and remained stable up to 24 h in the presence of 2.5 mg ascorbic acid. Molecular docking was performed to evaluate the complex binding to its target DNA-human topoisomerase II complex. Result of the in vivo evaluation showed that the complex tends to preferentially localize in cancerous tissues. The in vitro cell growth inhibition assay showed that the effect of the (186) Re-idarubicin was stronger than the effect of cold idarubicin, which strongly suggested that its cytotoxicity was mainly because of radiotoxicity rather than chemotherapeutic activity.
authors.affiliation: Atomic Energy Authority, Cairo, Egypt.
authors.forename: O A
authors.initials: OA
authors.lastname: El-Kawy
authors.affiliation: Atomic Energy Authority, Cairo, Egypt.
authors.forename: H M
authors.initials: HM
authors.lastname: Talaat
mesh_terms: D000818:Animals; D000903:Antibiotics, Antineoplastic / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D006528:Carcinoma, Hepatocellular / Q000000981:diagnostic imaging; D045744:Cell Line, Tumor; D004250:DNA Topoisomerases, Type II / Q000737:chemistry / Q000378:metabolism; D006801:Humans; D015255:Idarubicin / Q000737:chemistry*; D008113:Liver Neoplasms / Q000000981:diagnostic imaging; D051379:Mice; D062105:Molecular Docking Simulation; D011485:Protein Binding; D011868:Radioisotopes / Q000737:chemistry; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D012211:Rhenium / Q000737:chemistry*; D014018:Tissue Distribution; D059005:Topoisomerase II Inhibitors / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology
chemical_list: D000903:Antibiotics, Antineoplastic; D011868:Radioisotopes; D019275:Radiopharmaceuticals; D059005:Topoisomerase II Inhibitors; D012211:Rhenium; D004250:DNA Topoisomerases, Type II; D015255:Idarubicin
keywords: diagnosis; hepatocellular carcinoma; idarubicin; molecular modelling; rhenium-186; treatment