Результаты исследований: Научные публикации в периодических изданиях › статья › Рецензирование
Design of the New Closo-Dodecarborate-Containing Gemcitabine Analogue for the Albumin-Based Theranostics Composition. / Raskolupova, Valeria I; Wang, Meiling; Dymova, Maya A и др.
в: Molecules (Basel, Switzerland), Том 28, № 6, 2672, 15.03.2023.Результаты исследований: Научные публикации в периодических изданиях › статья › Рецензирование
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TY - JOUR
T1 - Design of the New Closo-Dodecarborate-Containing Gemcitabine Analogue for the Albumin-Based Theranostics Composition
AU - Raskolupova, Valeria I
AU - Wang, Meiling
AU - Dymova, Maya A
AU - Petrov, Gleb O
AU - Shchudlo, Ivan M
AU - Taskaev, Sergey Yu
AU - Abramova, Tatyana V
AU - Godovikova, Tatyana S
AU - Silnikov, Vladimir N
AU - Popova, Tatyana V
N1 - Funding: This research was funded by the Russian Science Foundation (grant № 19-74-20123).
PY - 2023/3/15
Y1 - 2023/3/15
N2 - 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 closo-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 closo-dodecaborate, and a 5'-hydroxy group was used to tether maleimide moiety through an acid-labile phosphamide linker. The N-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 (IC50) 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.
AB - 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 closo-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 closo-dodecaborate, and a 5'-hydroxy group was used to tether maleimide moiety through an acid-labile phosphamide linker. The N-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 (IC50) 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.
KW - BORON NEUTRON CAPTURE THERAPY
KW - BORON DELIVERY AGENTS
KW - GEMCITABINE ANALOGUE
KW - BORONATED ALBUMIN THERANOSTIC CONJUGATE
KW - CELL VIABILITY AND PROLIFERATION
KW - CLONOGENIC ASSAY
UR - https://www.scopus.com/record/display.uri?eid=2-s2.0-85151113824&origin=inward&txGid=45840cc3a87183778a618d3bab16989b
UR - https://elibrary.ru/item.asp?id=50498118
UR - https://www.mendeley.com/catalogue/6d44dd1b-893b-3906-b9cd-bf3bead65374/
U2 - 10.3390/molecules28062672
DO - 10.3390/molecules28062672
M3 - Article
C2 - 36985644
VL - 28
JO - Molecules
JF - Molecules
SN - 1420-3049
IS - 6
M1 - 2672
ER -
ID: 46103373