DC pole | Wartość | Język |
dc.contributor.author | Adamus‐Grabicka, Angelika A. | - |
dc.contributor.author | Daśko, Mateusz | - |
dc.contributor.author | Hikisz, Paweł | - |
dc.contributor.author | Kusz, Joachim | - |
dc.contributor.author | Malecka, Magdalena | - |
dc.contributor.author | Budzisz, Elżbieta | - |
dc.date.accessioned | 2022-05-30T09:51:32Z | - |
dc.date.available | 2022-05-30T09:51:32Z | - |
dc.date.issued | 2022 | - |
dc.identifier.citation | "International Journal of Molecular Sciences" (2022), Vol. 23, iss. 11, art. no. 6061 | pl_PL |
dc.identifier.issn | 1422-0067 | - |
dc.identifier.uri | http://hdl.handle.net/20.500.12128/23419 | - |
dc.description.abstract | In this study, we evaluated the antiproliferative potential, DNA damage, crystal structures,
and docking calculation of two spiropyrazoline derivatives. The main focus of the research
was to evaluate the antiproliferative potential of synthesized compounds towards eight cancer cell
lines. Compound I demonstrated promising antiproliferative properties, especially toward the
HL60 cell line, for which IC50 was equal to 9.4 μM/L. The analysis of DNA damage by the comet
assay showed that compound II caused DNA damage to tumor lineage cells to a greater extent than
compound I. The level of damage to tumor cells of the HEC‐1‐A lineage was 23%. The determination
of apoptotic and necrotic cell fractions by fluorescence microscopy indicated that cells treated with
spiropyrazoline‐based analogues were entering the early phase of programmed cell death. Compounds
I and II depolarized the mitochondrial membranes of cancer cells. Furthermore, we performed
simple docking calculations, which indicated that the obtained compounds are able to bind
to the PARP1 active site, at least theoretically (the free energy of binding values for compound I and
II were −9.7 and 8.7 kcal mol−1, respectively). In silico studies of the influence of the studied compounds
on PARP1 were confirmed in vitro with the use of eight cancer cell lines. The degradation
of the PARP1 enzyme was observed, with compound I characterized by a higher protein degradation
activity. | pl_PL |
dc.language.iso | en | pl_PL |
dc.rights | Uznanie autorstwa 3.0 Polska | * |
dc.rights.uri | http://creativecommons.org/licenses/by/3.0/pl/ | * |
dc.subject | flavonoid derivatives | pl_PL |
dc.subject | anticancer properties | pl_PL |
dc.subject | spiropyrazoline | pl_PL |
dc.subject | PARP1 | pl_PL |
dc.subject | DNA interaction | pl_PL |
dc.title | Biochemical, Structural Analysis, and Docking Studies of Spiropyrazoline Derivatives | pl_PL |
dc.type | info:eu-repo/semantics/article | pl_PL |
dc.identifier.doi | 10.3390/ijms23116061 | - |
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