Evaluation of radioiodinated ethopabate as a potential tumor targeting agent.

Autor: Aboumanei MH; Labeled Compounds Department, Hot Labs Center, Egyptian Atomic Energy Authority, P.O. Box 11371, Cairo, Egypt. Electronic address: mohamed.aboumanei@must.edu.eg., Mahmoud AF; Labeled Compounds Department, Hot Labs Center, Egyptian Atomic Energy Authority, P.O. Box 11371, Cairo, Egypt., Motaleb MA; Labeled Compounds Department, Hot Labs Center, Egyptian Atomic Energy Authority, P.O. Box 11371, Cairo, Egypt.
Jazyk: angličtina
Zdroj: Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine [Appl Radiat Isot] 2022 Feb; Vol. 180, pp. 110063. Date of Electronic Publication: 2021 Dec 11.
DOI: 10.1016/j.apradiso.2021.110063
Abstrakt: Overexpression of folate synthesis and folate receptor in a wide variety of tumors was reported. As a result, folate derivatives have emerged as a potential candidate for tumor imaging and therapy. Ethopabate is a structural analogue of para-aminobenzoic acid (PABA), a precursor of folic acid. Ethopabate was radiolabeled with radioiodine-131 ( 131 I) via direct electrophilic substitution reaction. Several factors that might affect the radiolabeling yield were studied. Paper chromatography was utilized for testing and evaluation of [ 131 I]iodoethopabate, and HPLC was used as a co-chromatographic tool to confirm the radiochemical yield. The biodistribution of [ 131 I]iodoethopabate in normal and tumor-bearing mice was investigated. The radioiodination of ethopabate resulted in a radiochemical yield of 93.70 ± 0.19%. The biodistribution data revealed that [ 131 I]iodoethopabate was taken up by tumors with promising target/non-target (T/NT) ratios. Where, the tumor to-blood ratios were 3.30 ± 0.40 and 4.06 ± 0.10 at 1 and 4 h post injection, respectively. As a result of these findings, [ 131 I]iodoethopabate appears to have excellent tumor uptake and adequate stability to be used for diagnostic purpose in the future.
(Copyright © 2021 Elsevier Ltd. All rights reserved.)
Databáze: MEDLINE
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