Enzymatic basis for the lack of oxamniquine activity in Schistosoma haematobium infections.
The notion that oxamniquine is active against Schistosoma mansoni but inactive against S. haematobium was confirmed using in vitro cultures of adult worms. Since oxamniquine and hycanthone have been shown to become effective upon activation by a schistosome enzyme, enzymatic tests were carried out to detect possible differences between the enzyme of S. mansoni and that of S. haematobium. It was found that the S. mansoni enzyme could activate hycanthone and, to a lesser extent, oxamniquine. The S. haematobium enzyme, on the other hand, was capable of activating hycanthone but virtually incapable of activating oxamniquine. It is concluded that the different activity of oxamniquine in the two species is due to differences in the drug-activating enzyme.
Pica-Mattoccia
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Institute of Cell Biology, Rome, Italy.
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D000818:Animals; D001711:Biotransformation; D006826:Hycanthone / Q000494:pharmacology; D046911:Macromolecular Substances; D008297:Male; D010073:Oxamniquine / Q000378:metabolism / Q000494:pharmacology*; D012548:Schistosoma haematobium / Q000187:drug effects* / Q000201:enzymology; D012550:Schistosoma mansoni / Q000187:drug effects; D012556:Schistosomicides / Q000378:metabolism*; D013045:Species Specificity
D046911:Macromolecular Substances; D012556:Schistosomicides; D010073:Oxamniquine; D006826:Hycanthone