Design of the New -Dodecarborate-Containing Gemcitabine Analogue for the Albumin-Based Theranostics Composition.
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ID: 276839
2023
Combination therapy is becoming an increasingly important treatment strategy because multi-drugs can maximize therapeutic effect and overcome potential mechanisms of drug resistance. A new albumin-based theranostic containing gemcitabine -dodecaborate analogue has been developed for combining boron neutron capture therapy (BNCT) and chemotheraphy. An exo-heterocyclic amino group of gemcitabine was used to introduce dodecaborate, and a 5'-hydroxy group was used to tether maleimide moiety through an acid-labile phosphamide linker. The -trifluoroacylated homocysteine thiolactone was used to attach the gemcitabine analogue to human serum albumin (HSA) bearing Cy5 or Cy7 fluorescent dyes. The half-maximal inhibitory concentration (IC) of the designed theranostic relative to T98G cells was 0.47 mM with the correlation coefficient R = 0.82. BNCT experiments resulted in a decrease in the viability of T98G cells, and the survival fraction was ≈ 0.4.
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| Authors | Raskolupova, Valeria I;Wang, Meiling;Dymova, Maya A;Petrov, Gleb O;Shchudlo, Ivan M;Taskaev, Sergey Yu;Abramova, Tatyana V;Godovikova, Tatyana S;Silnikov, Vladimir N;Popova, Tatyana V; |
| Journal | Molecules (Basel, Switzerland) |
| Year | 2023 |
| DOI | 2672 |
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