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Platelet-12 lipoxygenase targeting via a newly synthesized curcumin derivative radiolabeled with technetium-99m

Overview of attention for article published in BMC Chemistry, November 2016
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Title
Platelet-12 lipoxygenase targeting via a newly synthesized curcumin derivative radiolabeled with technetium-99m
Published in
BMC Chemistry, November 2016
DOI 10.1186/s13065-016-0220-x
Pubmed ID
Authors

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.

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The data shown below were compiled from readership statistics for 25 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Unknown 25 100%

Demographic breakdown

Readers by professional status Count As %
Researcher 5 20%
Professor > Associate Professor 4 16%
Student > Bachelor 3 12%
Student > Ph. D. Student 3 12%
Lecturer 1 4%
Other 3 12%
Unknown 6 24%
Readers by discipline Count As %
Chemistry 9 36%
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 9 36%