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Steroid dimers-In vitro cytotoxic and antimicrobial activities

Authorized Users Only
2014
Authors
Krstić, Natalija
Matić, Ivana Z.
Juranić, Zorica
Novaković, Irena
Sladić, Dušan
Article (Published version)
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Abstract
The in vitro cytotoxic activity of previously synthesized steroid dimers with different spacer group (sulfide, trithiolane ring or phosphorotrithioate) and the substituent at C-17 position was tested for their possible effects against following human tumor cell lines: cervical adenocarcinoma (HeLa), chronic myelogenous leukemia (K562) and two human breast cancer cell lines (MDA-MB-361 and MDA-MB-453). These compounds, applied at micromolar concentrations, exhibited cytotoxic activity of different intensity (compared with cisplatin as a control), modality and selectivity in these malignant cell lines. The best activity against all four cell cancer lines was exhibited by dimer-sulfides. All screened compounds exerted concentration-dependent cytotoxic activity against leukemia K562 cells. The compounds which exerted the most pronounced cytotoxic action exhibited notably higher cytotoxic activities against K562, HeLa and MDA-MB-453 cells in comparison to resting and PHA-stimulated PBMC, po...inting to a significant selectivity in their antitumor actions. Examination of the mechanisms of cytotoxicity on leukemia K562 cells revealed pro-apoptotic action of each of the investigated compounds applied at concentrations 2IC(50). The most prominent pro-apoptotic action was exhibited by dimer-sulfide of cholest-4-en-3-one. Furthermore, almost all of the tested compounds at IC50 concentrations induced G1 phase cell cycle arrest in K562 cells. Antimicrobial activity against Gram-positive, Gram-negative bacteria and fungal cells, and toxicity to brine shrimp Artemia sauna, were evaluated. There was no antibacterial activity. The best antifungal activity was exhibited against Saccharomyces cerevisiae by dimers linked with trithiolane ring, indicating a selective activity of investigated compounds.

Keywords:
Steroid dimers / cytotoxic activity / Cell death / Cell cycle analysis / Caspase / Antimicrobial activity
Source:
Journal of Steroid Biochemistry and Molecular Biology, 2014, 143, 365-375
Publisher:
  • Pergamon-Elsevier Science Ltd, Oxford
Projects:
  • Interactions of natural products, their derivatives and coordination compounds with proteins and nucleic acids (RS-172055)
  • Biological response modifiers in physiological and pathological conditions (RS-175011)

DOI: 10.1016/j.jsbmb.2014.06.005

ISSN: 0960-0760

PubMed: 24923733

WoS: 000341465500040

Scopus: 2-s2.0-84902667382
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URI
http://cer.ihtm.bg.ac.rs/handle/123456789/1409
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