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A potential method to improve the in vitro cytotoxicity of half-sandwich Os(II) complexes against A2780 cells

The result's identifiers

  • Result code in IS VaVaI

    <a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61989592%3A15310%2F18%3A73591077" target="_blank" >RIV/61989592:15310/18:73591077 - isvavai.cz</a>

  • Result on the web

    <a href="https://pubs.rsc.org/en/content/articlepdf/2018/dt/c8dt00193f" target="_blank" >https://pubs.rsc.org/en/content/articlepdf/2018/dt/c8dt00193f</a>

  • DOI - Digital Object Identifier

    <a href="http://dx.doi.org/10.1039/c8dt00193f" target="_blank" >10.1039/c8dt00193f</a>

Alternative languages

  • Result language

    angličtina

  • Original language name

    A potential method to improve the in vitro cytotoxicity of half-sandwich Os(II) complexes against A2780 cells

  • Original language description

    The [Os((6)-pcym)(dpa)(VP)]PF6 (1-VP) complex contains the histone deacetylase (HDAC) inhibitor valproate (2-propylpentanoate; VP) as a monodentate O-donor ligand and shows ca. 3-fold higher in vitro cytotoxicity against A2780 human ovarian carcinoma cells than its chlorido analogue [Os((6)-pcym)(dpa)Cl]PF6 (1-Cl); pcym = 1-methyl-4-(propan-2-yl)benzene (p-cymene), dpa = 2,2-dipyridylamine. The complex 1-VP showed promising selectivity towards the A2780 ovarian carcinoma cell line (IC50 = 20.9 M) over normal human hepatocytes (IC50 &gt; 200.0 M). Moreover, the complex 1-VP was found to be inactive against MCF-7 (breast adenocarcinoma), PANC-1 (pancreatic adenocarcinoma) and HT-29 (colon carcinoma) up to a concentration of 100 M. Detailed flow cytometry studies indicated that treatment of A2780 cells with complex 1-VP led to induction of apoptosis, production of reactive oxygen species (ROS) and superoxide (SO) anion radicals, as well as mitochondrial membrane potential depletion and cell cycle perturbations. The microscopic assessment (standard hematoxylin/eosin staining) revealed signs of morphological changes associated with the progression of apoptosis in A2780 cells treated with the IC50 concentration of the complex 1-VP. Consistent with the intracellular production of ROS and SO, the complex 1-VP induced hydroxyl radical formation, as proved by EPR spin trapping experiments. This case study suggests that replacement of the chlorido ligand of half-sandwich Os(ii) complexes by a releasable monodentate biologically active ligand (e.g., VP used in this study) is an effective strategy for the development of novel non-platinum cytotoxic agents.

  • Czech name

  • Czech description

Classification

  • Type

    J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database

  • CEP classification

  • OECD FORD branch

    10402 - Inorganic and nuclear chemistry

Result continuities

  • Project

    Result was created during the realization of more than one project. More information in the Projects tab.

  • Continuities

    P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Others

  • Publication year

    2018

  • Confidentiality

    S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Data specific for result type

  • Name of the periodical

    DALTON TRANSACTIONS

  • ISSN

    1477-9226

  • e-ISSN

  • Volume of the periodical

    47

  • Issue of the periodical within the volume

    16

  • Country of publishing house

    GB - UNITED KINGDOM

  • Number of pages

    11

  • Pages from-to

    5714-5724

  • UT code for WoS article

    000430802500027

  • EID of the result in the Scopus database

    2-s2.0-85045958670