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211At labeled substance P (5–11) as potential radiopharmaceutical for glioma treatment

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dc.abstract.enIntroduction The purposes of the present work were to label substance P (5–11) with 211At using a rhodium(III) complex with a bifunctional ligand–2-(1,5,9,13-tetrathiacyclohexadecan-3-yloxy)acetic acid ([16aneS4]-COOH) and to assess the in vitro stability and toxicity of the obtained radiobioconjugate. Methods Two approaches were evaluated to obtain 131I/211At-Rh[16aneS4]-SP5–11 radiobioconjugates, based on 2-step and 1-step syntheses. In the first method 131I/211At-Rh[16aneS4]-COOH complexes were obtained that required further coupling to a biomolecule. In the second approach, the bioconjugate [16aneS4]-SP5–11 was synthesized and further labeled with 131I and 211At through the utilization of a Rh(III) metal cation bridge. The synthesized compounds were analyzed by HPLC, TLC and paper electrophoresis. Results The 131I/211At-Rh[16aneS4]-COOH complexes were obtained in high yield and possessed good stability in PBS and CSF. Preliminary studies on coupling of 131I-Rh[16aneS4]-COOH to substance P (5–11) in 2-step synthesis showed that this procedure was too long with respect to 211At half-life, prompting us to improve it by finally using a 1-step synthesis. This strategy not only shortened the labeling time, but also increased final yield of 131I/211At-Rh[16aneS4]-SP5–11 radiobioconjugates. The stability of both compounds in PBS and CSF was high. Toxicity studies with the 211At-Rh[16aneS4]-SP5–11 demonstrated that radiobioconjugate significantly reduced T98G cell viability in a dose dependent manner reaching 20% of survival at the highest radioactivity 1200 kBq/mL. Conclusions The radiobioconjugate 211At-Rh[16aneS4]-SP5–11 revealed its potential in killing glioma T98G cells during in vitro studies; therefore further animal studies to are required to determine its in vivo stability and treatment potential in normal and xenografted mice.
dc.affiliationUniwersytet Warszawski
dc.contributor.authorSzkliniarz, Katarzyna
dc.contributor.authorMęczyńska-Wielgosz, Sylwia
dc.contributor.authorJastrzębski, Jerzy
dc.contributor.authorPruszyński, Marek
dc.contributor.authorWąs, Bogdan
dc.contributor.authorŁyczko, Krzysztof
dc.contributor.authorŁyczko, Monika
dc.contributor.authorKruszewski, Marcin
dc.contributor.authorStolarz, Anna
dc.contributor.authorMajkowska-Pilip, Agnieszka
dc.contributor.authorBilewicz, Aleksander
dc.date.accessioned2024-01-24T15:35:37Z
dc.date.available2024-01-24T15:35:37Z
dc.date.issued2017
dc.description.financeNie dotyczy
dc.description.volume53
dc.identifier.doi10.1016/J.NUCMEDBIO.2017.05.008
dc.identifier.issn0969-8051
dc.identifier.urihttps://repozytorium.uw.edu.pl//handle/item/100040
dc.identifier.weblinkhttps://www.sciencedirect.com/science/article/pii/S0969805116302773
dc.languageeng
dc.pbn.affiliationphysical sciences
dc.relation.ispartofNuclear Medicine and Biology
dc.relation.pages1-8
dc.rightsClosedAccess
dc.sciencecloudnosend
dc.subject.enRadioiodination
dc.subject.enAstatine-211
dc.subject.enRhodium complexes
dc.subject.enSubstance P
dc.subject.enMacrocyclic thioether
dc.title211At labeled substance P (5–11) as potential radiopharmaceutical for glioma treatment
dc.typeJournalArticle
dspace.entity.typePublication