Enzymatic basis for the lack of oxamniquine activity in Schistosoma haematobium infections

• Published in: Parasitology research (1987) Vol. 83; no. 7; pp. 687 - 689
• Main Authors: PICA-MATTOCCIA, L, NOVI, A, CIOLI, D
• Format: Journal Article
• Language: English
• Published: Berlin Springer 1997
• Subjects: Animals; Antibiotics. Antiinfectious agents. Antiparasitic agents; Antiparasitic agents; Biological and medical sciences; Biotransformation; Hycanthone - pharmacology; Macromolecular Substances; Male; Medical sciences; Oxamniquine - metabolism; Oxamniquine - pharmacology; Pharmacology. Drug treatments; Schistosoma haematobium - drug effects; Schistosoma haematobium - enzymology; Schistosoma mansoni - drug effects; Schistosomicides - metabolism; Species Specificity; Anthelmintic; Schistosoma haematobium; Enzyme; Trematode disease; Plathelmintha; Parasite; Activation; Parasitosis; Helminthiasis; Trematoda; Infection; Schistosomiasis; Chemotherapy; Parasiticid; Helmintha; Oxamniquine; Invertebrata; Mechanism of action; Negative therapeutic reaction
• ISSN: 0932-0113; 1432-1955
• DOI: 10.1007/s004360050320

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.