Cellular uptake and toxicity study of cis-bis(6-aminoquinoline) dichloroplatinum(II)

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 × 10-4 M, but did exhibit inhibition of culture growth at 5 × 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. © 1991.