Inhibition of DNA and RNA Polymerase Reactions by Trypanocidal Drugs. Effect of Aromatic Diamidine and Phenanthridinium Compounds

摘要

Several trypanocidal drugs were tested for possible inhibitory activity towards DNA (pol. I) and RNA polymerase. These chemotherapeutically active agents are throught to inhibit nucleic acid syntheses in African bloodstream trypanosomes. In the isolated DNA and RNA reactions those compounds that were most inhibitory include Isometamidium, Berenil (diminazene) and Hydroxystilbamidine. In some cases inhibition of the DNA polymerase reaction could be relieved by the input of additional enzyme and/or template-primer. RNA polymerase activity appeared to be inhibited in direct proportion to the amount of drug bound to the template. (Author)