Cellular uptake and toxicity study of cis-bis(6-aminoquinoline) dichloroplatinum (II).
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.
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Department of Biology, University of Northern Iowa, Cedar Falls 50614.
Chang
J C
JC
Bergquist
B L
BL
D000818:Animals; D002455:Cell Division; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D002945:Cisplatin / Q000031:analogs & derivatives* / Q000737:chemistry / Q000378:metabolism / Q000633:toxicity; D009944:Organoplatinum Compounds / Q000737:chemistry / Q000378:metabolism* / Q000633:toxicity; D013768:Tetrahymena / Q000378:metabolism
D009944:Organoplatinum Compounds; C070611:bis(6-aminoquinoline)dichloroplatinum(II); D002945:Cisplatin