Extraction, purification and radioiodination of Khellin as cancer theranostic agent

Adli A Selim; Basma M Essa; Islam M Abdelmonem; Mohamed A Amin; Mona O Sarhan

doi:10.1016/j.apradiso.2021.109970

Extraction, purification and radioiodination of Khellin as cancer theranostic agent

Appl Radiat Isot. 2021 Dec:178:109970. doi: 10.1016/j.apradiso.2021.109970. Epub 2021 Oct 2.

Authors

Adli A Selim¹, Basma M Essa², Islam M Abdelmonem³, Mohamed A Amin⁴, Mona O Sarhan⁵

Affiliations

¹ Labeled Compounds Department, Hot Laboratories Centre, Egyptian Atomic Energy Authority (EAEA), Cairo, 13759, Egypt; Radioisotopes Production Facility, Second Egyptian Research Reactor Complex, Egyptian Atomic Energy Authority (EAEA), Cairo, 13759, Egypt. Electronic address: [email protected].
² Radioactive Isotopes and Generator Department, Hot Laboratories Centre, Egyptian Atomic Energy Authority (EAEA), Cairo, 13759, Egypt.
³ Nuclear Chemistry Department, Hot Laboratories Centre, Egyptian Atomic Energy Authority (EAEA), Cairo, 13759, Egypt.
⁴ Analytical Chemistry Department, Benha University, Benha, 13511, Egypt.
⁵ Labeled Compounds Department, Hot Laboratories Centre, Egyptian Atomic Energy Authority (EAEA), Cairo, 13759, Egypt. Electronic address: [email protected].

PMID: 34619628
DOI: 10.1016/j.apradiso.2021.109970

Abstract

Khellin was successfully extracted from Ammi visnaga fruits with a recovery percent of 96.15%. Next radio-iodination of Khellin was successfully achieved with a high yield. The biodistribution study of [¹³¹I]iodo-khellin in tumour bearing mice revealed that khellin preferentially localization at tumour tissue. Target prediction study for [¹³¹I]iodo-khellin revealed that PI3K and VEGFR are potential targets for iodo-khellin with good affinity. The results of this study potentiate [¹³¹I]iodo-khellin as a good theranostic agent for tumour imaging and therapy.

Keywords: Extraction; Iodine-131; Khellin; Molecular modelling; Radiolabeling; Theranostic.

MeSH terms

Animals
Chromatography, High Pressure Liquid / methods
Humans
Iodine Radioisotopes / administration & dosage*
Iodine Radioisotopes / chemistry
Khellin / chemistry
Khellin / isolation & purification
Khellin / metabolism*
Male
Mice
Molecular Docking Simulation
Neoplasms / metabolism
Neoplasms / therapy*
Phosphatidylinositol 3-Kinases / metabolism
Precision Medicine*
Receptors, Vascular Endothelial Growth Factor / metabolism
Tissue Distribution

Substances

Iodine Radioisotopes
Iodine-131
Khellin
Receptors, Vascular Endothelial Growth Factor