Radioiodination and in vivo assessment of the potential of newly synthesized pyrrolizine-5-carboxamides derivative in tumor model.

Autor: Mahmoud AF; Labeled Compounds Dept. Hot Labs Center, Atomic Energy Authority, Cairo, Egypt., Aboumanei MH; Labeled Compounds Dept. Hot Labs Center, Atomic Energy Authority, Cairo, Egypt. Electronic address: Mohamed.aboumanei@must.edu.eg., Abdelhalim S; Labeled Compounds Dept. Hot Labs Center, Atomic Energy Authority, Cairo, Egypt., Hassan YA; Pharmaceutics Department Faculty of Pharmacy, Delta University for Science and Technology Gamasa, Egypt., Ibrahim IT; Labeled Compounds Dept. Hot Labs Center, Atomic Energy Authority, Cairo, Egypt; Faculty of Pharmacy, Albayan University, Baghdad, Iraq.
Jazyk: angličtina
Zdroj: Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine [Appl Radiat Isot] 2020 Dec; Vol. 166, pp. 109369. Date of Electronic Publication: 2020 Aug 08.
DOI: 10.1016/j.apradiso.2020.109369
Abstrakt: Recently, pyrrolizine derivatives have been reported to possess numerous anticancer activities. In a previous study, (EZ)-6-((4-chlorobenzylidene)-amino)-7-cyano-N-(p-tolyl)-2,3-dihydro-1H-pyrrolizine carboxamide (EZPCA) compound was synthesized and the cytotoxic activity of EZPCA toward COX-2 enzyme (overexpressed in cancer cells) was reported. In order to assess the suitability of this compound as a promising pilot structure for in vivo applications, EZPCA was radiolabeled with radioiodine-131 ( 131 I) and various factors affecting radiolabeling process were studied. Quality control studies of [ 131 I]iodo-EZPCA were performed using paper chromatography and HPLC was used as a co-chromatographic technique for confirming the radiochemical yield. Biodistribution studies of [ 131 I]iodo-EZPCA were undertaken in normal and tumor bearing mice. The radiochemical yield percentage of [ 131 I]iodo-EZPCA was 94.20 ± 0.12%. The biodistribution results showed evident tumor uptake of [ 131 I]iodo-EZPCA with promising target/non-target (T/NT) ratios. As a conclusion, these data suggest that [ 131 I]iodo-EZPCA had high binding efficiency, high tumor uptake and sufficient stability to be used be used in diagnostic studies.
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Databáze: MEDLINE
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