99m Tc-labeled teicoplanin and its biological evaluation in experimental animals for detection of bacterial infection

Motaleb, M. A.; El-Tawoosy, M.; Mohamed, Sameera; Borei, I. H.; Ghanem, Hala M.; Massoud, A.

doi:10.1134/s1066362214050154

Cited by 16 publications

(8 citation statements)

References 17 publications

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“…Radiolabeled 99m Tc-teicoplanin was shown to accumulate in high concentration (in 2 h) at the site of S. aureus in infected mice [148]. In another study, 99m Tc-vancomycin also showed similar affinity towards S. aureus infection foci [149].…”

Section: Glycopeptidesmentioning

confidence: 92%

Synthetic approaches to radiochemical probes for imaging of bacterial infections

Dutta

Naicker

Ebenhan

et al. 2017

European Journal of Medicinal Chemistry

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This present review provides an account on the available synthetic strategies employed to radiolabel commercial and potential bacteria-selective probes for tomographic imaging. These molecular probes encompass leukocytes, antibodies, small molecules, peptides, antibiotics, macrolides, vitamins, oligomers and siderophores. Although this technique has shown to be a valuable tool for non-invasive infection imaging, more development is required to create easy-to-radiolabel kit solutions/procedures for the preparation of the probes.

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Section: Glycopeptidesmentioning

confidence: 92%

Synthetic approaches to radiochemical probes for imaging of bacterial infections

Dutta

Naicker

Ebenhan

et al. 2017

European Journal of Medicinal Chemistry

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“…A standard dose containing the same injected amount was counted simultaneously and accounted as 100% activity [ 66 ] The uptake was expressed as percentage injected dose/gram tissue (%ID/g). Blood, bone, and muscles were assumed to be 7%, 10%, and 40% of the total body weight, respectively [ 67 ]. Data are reported as the mean ± SE.…”

Section: Methodsmentioning

confidence: 99%

Discovery of New Coumarin-Based Lead with Potential Anticancer, CDK4 Inhibition and Selective Radiotheranostic Effect: Synthesis, 2D & 3D QSAR, Molecular Dynamics, In Vitro Cytotoxicity, Radioiodination, and Biodistribution Studies

et al. 2021

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Novel 6-bromo-coumarin-ethylidene-hydrazonyl-thiazolyl and 6-bromo-coumarin-thiazolyl-based derivatives were synthesized. A quantitative structure activity relationship (QSAR) model with high predictive power r2 = 0.92, and RMSE = 0.44 predicted five compounds; 2b, 3b, 5a, 9a and 9i to have potential anticancer activities. Compound 2b achieved the best ΔG of –15.34 kcal/mol with an affinity of 40.05 pki. In a molecular dynamic study 2b showed an equilibrium at 0.8 Å after 3.5 ns, while flavopiridol did so at 0.5 Å after the same time (3.5 ns). 2b showed an IC50 of 0.0136 µM, 0.015 µM, and 0.054 µM against MCF-7, A-549, and CHO-K1 cell lines, respectively. The CDK4 enzyme assay revealed the significant CDK4 inhibitory activity of compound 2b with IC50 of 0.036 µM. The selectivity of the newly discovered lead compound 2b toward localization in tumor cells was confirmed by a radioiodination biological assay that was done via electrophilic substitution reaction utilizing the oxidative effect of chloramine-t. 131I-2b showed good in vitro stability up to 4 h. In solid tumor bearing mice, the values of tumor uptake reached a height of 5.97 ± 0.82%ID/g at 60 min p.i. 131I-2b can be considered as a selective radiotheranostic agent for solid tumors with promising anticancer activity.

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“…The uptake was expressed as percentage injected dose/gram tissue (%ID/g). Blood, bone, and muscles were assumed to be 7%, 10%, and 40% of the total body weight, respectively …”

Section: Methodsmentioning

confidence: 99%

“…Blood, bone, and muscles were assumed to be 7%, 10%, and 40% of the total body weight, respectively. 39 Data are reported as the mean ± SE. Data were analyzed using compare means function in SPSS software (Version 20.0).…”

Section: Biodistribution Study Of Compoundmentioning

confidence: 99%

Radioiodination and biological distribution of a new s‐triazine derivative for tumor uptake evaluation

Motaleb

Ibrahim

Sarhan

et al. 2018

Labelled Comp Radiopharmac

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A newly synthesized s-triazine derivative 1,1',1″-(((1,3,5-triazine-2,4,6-triyl) tris (azanediyl)) tris (benzene-4,1-diyl))tris (ethan-1-one), (1), was synthesized as a part of an ongoing research for development of novel s-triazine-based radiopharmaceuticals. In-vitro cell viability assay against different human cancer cell lines showed very promising inhibitory activity of the synthesized compound. This finding encouraged the radioiodination of 1 to study the degree of its localization in tumor site for evaluating the possibility of its use as a tumor imaging agent. The biodistribution study showed good localization of the radioiodinated derivative 2 at tumor site following i.v. administration in solid tumor-bearing mice. Finally, in a trial to understand the mechanism of the anticancer effect exerted by 1, a target prediction study and a docking study were performed. The results of the first study showed that focal adhesion kinase is a possible target for compound 1 and the docking study confirmed successful binding of both compound 1 and its radioiodinated derivative 2 to the binding site of focal adhesion kinase. As a conclusion, the results of this study suggest that, compound 2 could be used as a potential agent for tumor imaging after preclinical trials.

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99m Tc-labeled teicoplanin and its biological evaluation in experimental animals for detection of bacterial infection

Cited by 16 publications

References 17 publications

Synthetic approaches to radiochemical probes for imaging of bacterial infections

Synthetic approaches to radiochemical probes for imaging of bacterial infections

Discovery of New Coumarin-Based Lead with Potential Anticancer, CDK4 Inhibition and Selective Radiotheranostic Effect: Synthesis, 2D & 3D QSAR, Molecular Dynamics, In Vitro Cytotoxicity, Radioiodination, and Biodistribution Studies

Radioiodination and biological distribution of a new s‐triazine derivative for tumor uptake evaluation

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