MUTAGENIC ACTIVITIES INVITRO AND INVIVO OF 5 ANTISCHISTOSOMAL COMPOUNDS

  • 1 January 1977
    • journal article
    • research article
    • Vol. 200  (1) , 1-9
Abstract
Five antischistosomal compounds, hycanthone, its 2 chloroindazole analogs (IA-4 and IA-4 N-oxide), oxamniquine and metrifonate, were tested for mutagenic activity, using Salmonella typhimurium strains TA 98 and TA 100 under in vitro and in vivo (host-mediated) conditions. In all assay systems hycanthone exhibited by far the highest mutagenic potency. Although oxamniquine and metrifonate had low mutagenic activity in vitro and although their administration resulted in urine of low mutagenic activity, their host-mediated mutagenic activities on strain TA 100 were fairly high. Confirming earlier studies with a less sensitive Salmonella strain, TA 1535, IA-4 N-oxide was found to be less mutagenic than IA-4. Orally administered IA-4 and IA-4 N-oxide were less mutagenic under in vivo conditions than an equal dose administered i.m. The antischistosomal activity of a given dose of each compound was the same, regardless of which of these 2 routes was used, suggesting that mutagenic and antischistosomal effects are produced by different metabolites. Mutagenic activities apparently can be dissociated from desired chemotherapeutic effects by suitable structural modifications.

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