Radio-iodination and biological evaluation of pentoxifylline as a novel probe for diagnosis of intermittent claudication.

Autor: Motaleb MA; Labeled Compounds Department, Hot Lab Center, Egyptian Atomic Energy Authority, 11371, Cairo, Egypt., Shweeta HA; Labeled Compounds Department, Hot Lab Center, Egyptian Atomic Energy Authority, 11371, Cairo, Egypt., Aboumanei MH; Labeled Compounds Department, Hot Lab Center, Egyptian Atomic Energy Authority, 11371, Cairo, Egypt. Electronic address: Dr.mohamedaboumanei@gmail.com.
Jazyk: angličtina
Zdroj: Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine [Appl Radiat Isot] 2022 Nov; Vol. 189, pp. 110429. Date of Electronic Publication: 2022 Aug 24.
DOI: 10.1016/j.apradiso.2022.110429
Abstrakt: The diagnosis of intermittent claudication (IC) is challenging. Imaging with radiopharmaceuticals provides a new method for detecting acute IC. Pentoxifylline improves blood flow to ischemic tissues via increasing erythrocyte elasticity and inhibiting platelet aggregation. Pentoxifylline was radio-iodinated with radioiodine-131 ( 131 I) through a direct electrophilic substitution reaction. Furthermore, various factors that might influence the radiolabeling strategy were investigated. The radiochemical yield of [ 131 I]iodopentoxiphyline was evaluated by using paper chromatography and HPLC methods. The biodistribution pattern of [ 131 I]iodopentoxiphyline was studied, where Swiss albino mice was used as a model of acute limb ischemia-reperfusion. The maximum radiochemical yield of pentoxifylline was found to be 94.11 ± 2.35%. The biodistribution findings revealed that [ 131 I]iodopentoxiphyline was significantly deposited at the ischemic site (left hind limbs), with encouraging target/non-target (T/NT) ratios. At 0.25 and 1 h post injection, the uptake of [ 131 I]iodo-pentoxifylline was 5.30 ± 0.30 and 9.98 ± 1.12%, respectively. Also, the maximum T/NT ratio for [ 131 I]iodo-pentoxifylline (9.45 ± 0.26) was obtained at 0.25 h post injection. Due to safety and selectivity, [ 131 I]iodo-pentoxifylline may be a good prospective diagnostic tool for early identification of IC. Moreover, the outcome of this study can be expected to apply to I-123 as well.
Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.
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Databáze: MEDLINE