Reem Ibrahim Al-Wabli, Tamer Mostafa Mohamed Hafez Sakr, Mohammed Abdou Khedr, Adly Abdallah Selim, Mohamed Abd El-Motaleb Abd El-Rahman, Wafaa Abdou Zaghary
Abstract
One of the most popular techniques for cancer detection is the nuclear medicine technique. The present research focuses on Platelet-12-lipoxygenase (P-12-LOX) as a promising target for treating and radio-imaging tumor tissues. Curcumin was reported to inhibit this enzyme via binding to its active site.
A novel curcumin derivative was successfully synthesized and characterized with yield of 74%. It was radiolabeled with the diagnostic radioisotope technetium-99m with 84% radiochemical yield and in vitro stability up to 6 h. The biodistribution studies in tumor bearing mice confirmed the high affinity predicted by the docking results with a free binding energy value of (ΔG -50.10 kcal/mol) and affinity (13.64 pki) showing high accumulation in solid tumor with target/non-target ratio >6.
The newly synthesized curcumin derivative, as a result of a computational study on platelet-12 lipoxygenase, showed its excellent free binding energy (∆G -50.10 kcal/mol) and high affinity (13.64 pKi). It could be an excellent radio-imaging agent that targeting tumor cells via targeting of P-12-LOX.Graphical abstractThis novel curcumin derivative was successfully synthesized and radiolabeled with technetium-99m and biologically evaluated in tumor bearing mice that showed high accumulation in solid tumor with target/non-target ratio >6 confirming the affinity predicted by the docking results. Predicted binding mode of a new curcumin derivative in complex with 12-LOX active site. b Curcumin itself in the 12-LOX active site biological distribution of (99m)Tc-curcumin derivative complex in solid tumor bearing Albino mice.
Pharmacology, Toxicology and Pharmaceutical Science
2
8%
Biochemistry, Genetics and Molecular Biology
2
8%
Veterinary Science and Veterinary Medicine
1
4%
Neuroscience
1
4%
Other
1
4%
Unknown
8
33%
Attention Score in Context
Attention Score in Context
This research output has an Altmetric Attention Score of 1. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 12 April 2017.
All research outputs
#21,157,205
of 25,986,827 outputs
Outputs from Chemistry Central Journal
#1
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Outputs of similar age
#317,417
of 420,416 outputs
Outputs of similar age from Chemistry Central Journal
#3
of 4 outputs
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