ABSTRACT
A fluorescent analog of cis-diamminedichloroplatinum(II), cis-bis(6-aminoquinoline)dichloroplatinum(II), was prepared from K2[PtCl4] and 6-aminoquinoline (AQL). HPLC of the thiourea derivative of the new complex showed that it has the cis-configuration. The Pt-AQL complex and the parent ligand AQL were evaluated for biological activity and cellular uptake, using the ciliate Tetrahymena pigmentosa. The complex was relatively nontoxic at the tested levels below 5 x 10(-4) M, but did exhibit inhibition of culture growth at 5 x 10(-4) M. Measurement of cellular uptake of the Pt-AQL complex demonstrated incorporation into the cell, with localization primarily within the vacuoles of the cells. Comparable measurement of the parent ligand AQL showed little measurable cellular uptake.
Subject(s)
Cisplatin/analogs & derivatives , Organoplatinum Compounds/metabolism , Animals , Cell Division , Chemical Phenomena , Chemistry, Physical , Cisplatin/chemistry , Cisplatin/metabolism , Cisplatin/toxicity , Organoplatinum Compounds/chemistry , Organoplatinum Compounds/toxicity , Tetrahymena/metabolismABSTRACT
The effects of two chemical radiation protectors, WR-1065 and WR-151326, were characterized in V79 Chinese hamster cells after either cobalt-60 (60Co) gamma or fission spectrum neutron irradiation. Each protector was administered at a concentration of 4 mM to exponentially growing cultures for 30 min prior to and during irradiation with either 60Co gamma or JANUS fission spectrum neutrons. After irradiation the cells were either plated immediately for survival or returned to the incubator and assayed for cell progression. Aliquots of cells were removed at selected times, counted, fixed and stained with 4'6-diamidino-2-phenylindole (DAPI). Analysis of DNA histograms indicate that the presence of the protector during irradiation reduced the division delay experienced at the G2-M interface. Implications of these effects are discussed.
