Tc-linezolid as a radiotracer for brain abscess: Labeling, in silico docking, and biodistribution studies.

Appl Radiat Isot

Egyptian Atomic Energy Authority, Cairo, 13759, Egypt.

Published: October 2023

Brain abscess is a life-threatening condition that requires a timely and accurate diagnosis. In this study, linezolid, an oxazolidinone antibiotic, was labeled with technetium-99m according to the stannous chloride method. The labeling reaction factors were studied and optimized to achieve a high yield (97.4 ± 2.3%). The Tc-linezolid was radio- and physico-chemically characterized to assess its suitability as a radiopharmaceutical for the brain. In-silico docking to target peptidyltransferase showed an optimal binding fit (energy = -66.6 Kcal/mol). The complex was biologically evaluated in-vitro using binding assays in alive and heat-killed bacteria and in-vivo in an MRSA brain infection model. All results suggested that the labeled complex could potentially be a new nuclear imaging agent to diagnose and localize brain abscesses specifically.

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http://dx.doi.org/10.1016/j.apradiso.2023.110917DOI Listing

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