Radioiodination of 5-aminoisoquinoline for Poly (ADP-ribose) Polymerase Targeting: An In vitro Evaluation in Colorectal Carcinoma Cells
EL-Hamoly, T., Aglan, H., Alabyad, M., Kandil, S. (2020). Radioiodination of 5-aminoisoquinoline for Poly (ADP-ribose) Polymerase Targeting: An In vitro Evaluation in Colorectal Carcinoma Cells. EKB Journal Management System, 33(1), 59-64. doi: 10.21608/ejrsa.2020.36220.1101
Tarek EL-Hamoly; Hany Aglan; Mogahed Alabyad; Shaban Kandil. "Radioiodination of 5-aminoisoquinoline for Poly (ADP-ribose) Polymerase Targeting: An In vitro Evaluation in Colorectal Carcinoma Cells". EKB Journal Management System, 33, 1, 2020, 59-64. doi: 10.21608/ejrsa.2020.36220.1101
EL-Hamoly, T., Aglan, H., Alabyad, M., Kandil, S. (2020). 'Radioiodination of 5-aminoisoquinoline for Poly (ADP-ribose) Polymerase Targeting: An In vitro Evaluation in Colorectal Carcinoma Cells', EKB Journal Management System, 33(1), pp. 59-64. doi: 10.21608/ejrsa.2020.36220.1101
EL-Hamoly, T., Aglan, H., Alabyad, M., Kandil, S. Radioiodination of 5-aminoisoquinoline for Poly (ADP-ribose) Polymerase Targeting: An In vitro Evaluation in Colorectal Carcinoma Cells. EKB Journal Management System, 2020; 33(1): 59-64. doi: 10.21608/ejrsa.2020.36220.1101

Radioiodination of 5-aminoisoquinoline for Poly (ADP-ribose) Polymerase Targeting: An In vitro Evaluation in Colorectal Carcinoma Cells

Egyptian Journal of Radiation Sciences and Applications
Article 8, Volume 33, Issue 1, July 2020, Page 59-64  XML PDF (1.21 MB)
Document Type: Original Article
DOI: 10.21608/ejrsa.2020.36220.1101
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Authors
Tarek EL-Hamolyorcid 1, 2; Hany Aglan email 3; Mogahed Alabyad1; Shaban Kandil1, 4
1Cyclotron Project, Nuclear Research Center, Atomic Energy Authority, Egypt
2Drug Radiation Research Department, National Center for Radiation Research and Technology, Atomic Energy Authority, Egypt
3Cyclotron Project, Egyptian Atomic Energy Authority Labeled Compounds Department, Hot Labs Center, Atomic Energy Authority, Egypt
4Labeled Compounds Department, Hot Labs Center, Atomic Energy Authority, Egypt
Abstract
THE ISOQUINOLINE derivative, 5-aminoisoquinoline (5-AIQ), is a potent inhibitor of poly (ADP-ribose) polymerase (PARP) activity; the DNA repairing protein frequently overexpressed in various carcinoma cells. The current study is dedicated for developing a highly specific radioiodinated PARP-1 binding tracer namlely, [131I] 5-aminoisoquinoline. The radioiodination of 5-aminoisoquinoline with 131I was carried out via electrophilic substitution reaction. In order to achieve the maximum radioiodination, the parameters including 5-aminoisoquinoline concentration, oxidizing agent, reaction time, temperature and type of solvent were optimized. the radiochemical purity was determined by high performance liquid chromatography (HPLC) using Reversed phase lichrosorb column 250×4.6 mm, C-18 5 μm. The maximum radiochemical yield was 80% with radiochemical purity reached 98%. The log P value for [131I] 5-aminoisoquinoline was found to be 2.08 ± 0.79. Data presented from Cell viability (MTT) cytotoxicity assay on Caco-2 cells showed matched IC50 values with the selected drug concentrations profile for either labeled or unlabeled 5-aminoisoquinoline. Likewise, the radioiodinated 5-aminoisoquinoline elucidated a higher cell uptake compared to free I-131.
Keywords
5-aminoisoquoline; Colorectal adenocarcinoma (Caco-2) cell line; PARP; Radiolabeling
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