Show simple item record

dc.creatorKrstić, Natalija
dc.creatorMatić, Ivana Z.
dc.creatorJuranić, Zorica
dc.creatorNovaković, Irena
dc.creatorSladić, Dušan
dc.date.accessioned2019-01-30T17:39:01Z
dc.date.available2019-01-30T17:39:01Z
dc.date.issued2014
dc.identifier.issn0960-0760
dc.identifier.urihttp://cer.ihtm.bg.ac.rs/handle/123456789/1409
dc.description.abstractThe 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, pointing 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.en
dc.publisherPergamon-Elsevier Science Ltd, Oxford
dc.relationinfo:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172055/RS//
dc.relationinfo:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/175011/RS//
dc.rightsrestrictedAccess
dc.sourceJournal of Steroid Biochemistry and Molecular Biology
dc.subjectSteroid dimersen
dc.subjectcytotoxic activityen
dc.subjectCell deathen
dc.subjectCell cycle analysisen
dc.subjectCaspaseen
dc.subjectAntimicrobial activityen
dc.titleSteroid dimers-In vitro cytotoxic and antimicrobial activitiesen
dc.typearticle
dc.rights.licenseARR
dcterms.abstractСладиц, Дусан М; Новаковић, Ирена; Јураниц, Зорица Д; Матиц, Ивана З; Крстић, Наталија;
dc.citation.volume143
dc.citation.spage365
dc.citation.epage375
dc.citation.other143: 365-375
dc.citation.rankM22
dc.identifier.pmid24923733
dc.identifier.doi10.1016/j.jsbmb.2014.06.005
dc.identifier.rcubConv_3214
dc.identifier.scopus2-s2.0-84902667382
dc.identifier.wos000341465500040
dc.type.versionpublishedVersion


Files in this item

Thumbnail

This item appears in the following Collection(s)

Show simple item record