Antiproliferative activity of some cis-/trans-platinum(II) complexes on HeLa cells.
Purpose of this work was to synthesize several cis-/trans- isomer pairs of the platinum(II) complexes, and study the extent and the mode of their antiproliferative activity on HeLa cells. Six platinum(II) isomer pairs have a general formula cis-/trans-[PtA2X2], where A is ligand: ammonia (NH3), pyridine (Py); and X is ligand: chloride ion (Cl-), bromide ion (Br-), iodide ion (I-), thiocyanato ion (SCN-); four compounds have different structural formulas, and these are cis-/trans-[Pt(NH2OH)2(NH3)2]Cl2, and cis-/trans-Pt(Gly)2, where Gly is bidentate glycinato ligand. Results of the MTT assay, showed that six cis- and one trans-platinum(II) complexes exhibited cytotoxicity (IC50) ranging between 5 and 33 microM. Most of the cis-platinum(II) isomers caused significant alteration of cell cycle phases progression, and induced apoptosis in degree that varied among different compounds, as evaluated using flowcytometry and morphological study. Spectrophotometric analysis (AAS) indicated that there is no correlation between intracellular platinum(II) accumulation and cytotoxicity of tested complexes.
Arandjelovic
S
S
Laboratory for experimental pharmacology, National Cancer Research Centre, Belgrade, Yugoslavia.
Tesic
Z
Z
Juranic
Z
Z
Radulovic
S
S
Vrvic
M
M
Potkonjak
B
B
Ilic
Z
Z
D000970:Antineoplastic Agents / Q000737:chemistry / Q000493:pharmacokinetics / Q000633:toxicity; D001692:Biological Transport; D002453:Cell Cycle / Q000187:drug effects; D002455:Cell Division / Q000187:drug effects*; D002470:Cell Survival / Q000187:drug effects; D002945:Cisplatin / Q000737:chemistry / Q000493:pharmacokinetics / Q000633:toxicity*; D006367:HeLa Cells; D006801:Humans; D008968:Molecular Conformation; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; C034697:transplatin; D002945:Cisplatin