Chloroquine is one of a series of 4-amiinoquinoline antimalarial compounds whose biology and chemistry were studied extensively during and immediately following World War II.'-3 Early investigations by Parker and Irvin4 demonstrated the ability of chloroquine to bind to both DNA and RNA in vitro, suggesting a possible mechanism by which this drug might interfere with cellular processes in malarial parasites. Subsequently, chloroquine has been found to be effective in controlling infestations by other species of parasites,5 and recently effects of this compound on the metamorphosis of tadpoles,6 and on cell division in tissue culture7 have been reported. The mechanism of action of chloroquine is not known, although effects on various enzyme systems have been described.8' Several years ago, it was demonstrated that chloroquinle can inhibit incorporation of radioactively labeled nucleic acid precursors in DNA and RNA of intact Plasmodium gallinaceunii and P. bergheij0 and more recently it has been shown that hydroxychloroquiine, a closely related analogue, has a similar effect on L-fibroblasts growing in tissue culture.1' The observations that, the binding of chloroquine to DNA can alter the biological'2 and physical'3 properties of the DNA helix suggests that this inhibition of cellular processes might indeed result from complex forma-Downloaded by guest on August 5, 2020
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