Naslov
Organometallic ruthenium complexes with triphenylphosphane amino acid bioconjugates as possible anticancer compounds

Autori
Pernar, Margareta ; Kokan, Zoran ; Matković, Marija ; Piantanida, Ivo ; Polančec, Denis ; Turel, Iztok ; Kirin, Srećko I. ; Brozović, Anamaria

Vrsta, podvrsta i kategorija rada
Sažeci sa skupova, sažetak, znanstveni

Izvornik
Libri oncologici : Croatian journal of oncology (0300-8142) XLIV (2016), 1 ; 47-47 / - Zagreb, 2016, 47-47

Skup
HDIR-4: "From Bench to Clinic"- Fourth Meeting of the Croatian Association for Cancer Research with International Participation

Mjesto i datum
Zagreb, Hrvatska, 03.11.2016. - 04.11.2016

Vrsta sudjelovanja
Poster

Vrsta recenzije
Nije recenziran

Ključne riječi
cancer ; organometallic ruthenium complexes ; cell death ; triphenylphosphane amino acid bioconjugates ; anticancer compounds

Sažetak
Cytotoxic activity of newly synthesized (p-cymene)-ruthenium complexes 1 and 2, bearing phosphane ligands substituted with chiral or non-chiral amino acid esters was investigated on human cervix carcinoma cell line (HeLa) using MTT assay. Four (2pG, 2pA, 2mG and 2mA) out of six synthesized metallated biconjugates showed significant toxicity, with IC50 values of 5 to 30 μM. 2mG compound with average value of IC50 16 μM was selected for further biological characterisation. The higher level of toxicity towards tumour compared to normal cell lines indicates its selective activity, important characteristic for potential medical use. Further, it was detected that 2mG causes dose- and time-dependent increase of SubG1 cell population, suggesting its ability to induce apoptosis and stop cells in G1/S phase of cell cycle. Moreover, the role of glutathione in HeLa cells response to investigated organometallic ruthenium complexes was confirmed by using specific regulators of GSH synthesis, buthionine sulfoximine and N-acetyl-cysteine. Pre-treatment of cells with ethacrynic acid and probenecid emphasizes role of GSH in detoxification of 2mG compound. We speculate that ruthenium complexes bind protein-based biomolecules triggering further cell death. Based on the gained knowledge, the synthesis and development of more tumour-specific ruthenium-based complexes as potential anticancer drugs is expected.

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Biologija

POVEZANOST RADA