Schistosomicidal Activity of Lucanthone Hydrochloride, Hycanthone and Their Metabolites in Mice and Hamsters

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Abstract
The schistosomicidal activities of hycanthone, the hydroxymethyl analog and the most active metabolite of lucanthone, and several human liver microsomal conversion metabolites of both compounds were tested against experimentally induced Schistosoma mansoni infection in mice and hamsters. The compounds were administered intragastrically (twice daily for 5 days) to groups of infected animals. Lucanthone, hycanthone, and two of the salts of hycanthone were also administered parenterally (single dose medication). Hycanthone was the most active metabolite of lucanthone. On an equal weight basis the schistosomicidal activity of intragastrically administered hycanthone was 9 times greater in hamsters and 3 times greater in mice than that of lucanthone. Desethyl analogs and the sulfoxides of both compounds were less active than either parent compound. When adminstered parenterally lucanthone was inactive whereas hycanthone was highly schistosomicidal. The activity of a single dose of a hycanthone administered parenterally was equal to that obtained by a 5-day regimen administered intragastrically, and the activity was maximal when given intravenously.