ABSTRACT
cis-bis(3-aminoflavone)dichloroplatinum(II) [cis-Pt(II) complex of 3-aminoflavone] is an analog of cis-DDP characterized by low cytotoxicity and anticancer properties in vivo. In order to evaluate genotoxic properties of this chemical compound, the comet assay in human lymphocytes was used. The analysis of DNA damage after 1-h cell incubation with cis-Pt(II) complex of 3-aminoflavone and cis-DDP was carried out, and DNA repair kinetics were evaluated after 0.5-h, 1-h, and 1.5-h postexposure incubation. It has been shown that cis-Pt(II) complex of 3-aminoflavone causes the increase in tail moments in comparison with cis-DDP. On the other hand, the decrease in these values caused by cis-DDP was connected mainly with the presence of DNA and DNA-protein crosslinks. The decrease in tail moments after cis-Pt(II) complex of 3-aminoflavone lymphocyte treatment was already observed after 0.5-h postexposure incubation, whereas in the variant with hydrogen peroxide application these values after cis-Pt(II) complex of 3-aminoflavone addition were higher in comparison with cis-DDP. Results obtained on the basis of the comet assay could confirm the occurrence of DNA breaks and cross-links induced by cis-Pt(II) complex of 3-aminoflavone.
Subject(s)
Cisplatin/toxicity , DNA Damage , DNA Repair , Lymphocytes/drug effects , Mutagens/toxicity , Organoplatinum Compounds/toxicity , Cell Survival/drug effects , Cells, Cultured , Comet Assay , Female , Humans , Lymphocytes/metabolismABSTRACT
Phosphorohydrazines and phosphorohydrazones of benzopyran-2,4-dione as well as the phosphorohydrazone of 4-hydroxycoumarine were tested for antitumor activity in lymphatic leukemia L1210 bearing mice.
Subject(s)
Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/pharmacology , Chromones/chemical synthesis , Chromones/pharmacology , Hydrazines/chemical synthesis , Hydrazines/pharmacology , Leukemia L1210/drug therapy , Organophosphorus Compounds/chemical synthesis , Organophosphorus Compounds/pharmacology , Animals , Antineoplastic Agents/toxicity , Chromones/toxicity , Hydrazines/toxicity , Lethal Dose 50 , Leukemia L1210/pathology , Mice , Mice, Inbred BALB C , Mice, Inbred DBA , Neoplasm Transplantation , Organophosphorus Compounds/toxicityABSTRACT
The X-ray structure analysis of [Ni(C(5)H(8)N(2))(4)(H(2)O)(2)]Cl(2) was undertaken to elucidate the geometry around the Ni(2+) ion. The molecule lies on a twofold axis which runs through the O-Ni-O atoms. The geometry around the Ni(2+) ion is best described as slightly distorted tetragonal bipyramidal.
Subject(s)
Nickel/chemistry , Organometallic Compounds/chemistry , Pyrazoles/chemistry , Crystallography, X-Ray , Molecular StructureSubject(s)
Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/pharmacology , Flavonoids/pharmacology , Organometallic Compounds/pharmacology , Palladium/chemistry , Palladium/pharmacology , Platinum Compounds/chemical synthesis , Platinum Compounds/pharmacology , Animals , Flavonoids/chemical synthesis , Leukemia L1210/drug therapy , Male , Mice , Mice, Inbred BALB C , Mice, Inbred DBA , Organometallic Compounds/chemical synthesisSubject(s)
Antineoplastic Agents/pharmacology , Cisplatin/pharmacology , Organophosphonates/pharmacology , Thymine/pharmacology , Uracil/pharmacology , Animals , Drug Interactions , Leukemia L1210/drug therapy , Leukemia L1210/pathology , Male , Mice , Thymine/analogs & derivatives , Tumor Cells, Cultured , Uracil/analogs & derivativesABSTRACT
The alkylating ability of alpha,beta-unsaturated amidoesters 1a-8d, diethyl pyridylmethylphosphonate esters and their cis-platinum(II) complexes has been investigated based on the test with 4-(4'-nitrobenzyl)pyridine (NBP) (Preussmann Test). Of the compounds tested for alkylating activity, only cis-platinum(II) phosphonate complexes were found to possess activity. The highest activity was found for CiS-[PtCl2(4-pmpe)2] where 4-pmpe is diethyl 4-pyridylmethylphosphonate. The results show a correlation between alkylating activity in vitro and cytotoxic activity in vivo for platinum(II) complexes.
Subject(s)
Amides/chemical synthesis , Antineoplastic Agents, Alkylating/chemical synthesis , Esters/chemical synthesis , Organophosphonates/chemical synthesis , Organoplatinum Compounds/chemical synthesis , Amides/pharmacology , Animals , Antineoplastic Agents, Alkylating/pharmacology , Drug Screening Assays, Antitumor , Esters/pharmacology , Indicators and Reagents , Leukemia L1210/drug therapy , Mice , Organophosphonates/pharmacology , Organoplatinum Compounds/pharmacology , Pyridines/chemistry , Sarcoma 180/drug therapySubject(s)
Antineoplastic Agents/pharmacology , Cisplatin/analogs & derivatives , Cisplatin/pharmacology , Platelet Aggregation Inhibitors/pharmacology , Platelet Aggregation/drug effects , Adenosine Diphosphate/antagonists & inhibitors , Adenosine Diphosphate/pharmacology , Animals , Humans , In Vitro Techniques , SwineABSTRACT
We investigated the effect of two cis-platinum (II) complexes, cis-[PtCl2(NH3)2] (cisplatin) and cis-[PtCl2(4-pmpe)2] (4-pmpe stands for diethyl 4-pyridylmethylphosphonate), which was recently synthetized in our laboratory, on murine mast cells. We noticed that both tested compounds were able to evoke histamine release from murine mast cells. The histamine secretion was dependent on the concentration of compound and on the time and temperature of the reaction. It was also dependent on metabolic energy (the reaction was diminished in a medium without glucose and abolished in the presence of 2-deoxyglucose). The results indicate that cis-platinum (II) complexes activate mast cells to secrete histamine via a non-cytotoxic, active secretory process.
