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99mTc-Luteolin: Radiolabeling, In Silico ADMET and Biological Evaluation as a Natural Tracer Tumor imaging

Dina M. El-Sharawy, S. I. Khater, Essam H.M, Noheir H. Sherif, Hossam M. Hassan, Abeer H. Elmaidomy

2021Journal of Radiation Research and Applied Sciences14 citationsDOIOpen Access PDF

Abstract

The focus of the staged work was radiolabelled 5,7,3ʹ, 4ʹ tetra-hydroxy flavone (Luteolin), isolated from Plantago lanceolata L., (F. Plantaginaceae), with 99mtechnetium (99mTc) to produce a natural tracer 99mTc-Luteolin (99mTc-Lut), and to evaluate the biological distribution in silico and in vivo. Labeling was carried out by reduction reaction using SnCl2 as reducing agent giving a maximum radiochemical yield (RCY) up to 97% at 40°C, pH4, for 30 min., with concentration of 99mTc and Luteolin of 150 μL. The tracer (99mTc-Lut) showed 12 h., in vitro stability. In silico ADMET screening of 99mTc-Lut indicated its high bioavailability in all body organs. The bio-distribution profile indicating the highly uptake of the tracer 99mTc-Lut, in tumor mice target/non-target ratio (T/NT) up to two-fold compared to normal mice, whereas the clearance from mice was observed via both renal and feces pathway. 99mTc-Lut, could be valued as a probable natural radiopharmaceutical tracer for tumor appearance.

Topics & Concepts

LuteolinChemistryTRACERIn silicoIn vivoBioavailabilityRadiochemistryChromatographyPharmacologyBiochemistryFlavonoidBiologyNuclear physicsAntioxidantBiotechnologyPhysicsGeneGlycosylation and Glycoproteins ResearchRadiopharmaceutical Chemistry and ApplicationsDrug Transport and Resistance Mechanisms
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