The effects of stibophen on phosphofructokinases and aldolases of adult filariids.
Trivalent organic antimonials, such as stibophen, have been employed for the chemotherapy of schistosome and filariid infections. The effects of stibophen on adult Litomosoides carinii, Dipetalonema witei (= viteae), and Brugia pahangi were examined. In vitro, lactate accumulation was markedly inhibited by the antimonials as was phosphofructokinase activities in homogenates. Incubation of filariids with stibophen and determination of internal concentrations of hexose phosphate also indicated a decreased phosphofructokinase activity. In addition, a second inhibitory effect of stibophen on aldolase has been observed which appears to be specific for stibophen and is not displayed by potassium antimony tartrate. Both inhibitory activities may contribute to the chemotherapeutic effect of stibophen. In addition to the schistosomes and filariids, stibophen also inhibits Ascaris and Hymenolepis diminuta phosphofructokinases at low concentrations, where no inhibition of the corresponding mammalian liver enzyme was demonstrable.
D000818:Animals; D000966:Antimony Potassium Tartrate / Q000494:pharmacology; D001200:Ascaris / Q000201:enzymology; D001557:Benzenesulfonates / Q000494:pharmacology*; D002009:Brugia / Q000201:enzymology; D004153:Dipetalonema / Q000201:enzymology; D005370:Filarioidea / Q000201:enzymology*; D005634:Fructose-Bisphosphate Aldolase / Q000037:antagonists & inhibitors / Q000378:metabolism*; D005636:Fructosephosphates; D005947:Glucose; D005958:Glucosephosphates; D006925:Hymenolepiasis / Q000201:enzymology; D010732:Phosphofructokinase-1 / Q000037:antagonists & inhibitors / Q000378:metabolism*
D001557:Benzenesulfonates; D005636:Fructosephosphates; D005958:Glucosephosphates; D000966:Antimony Potassium Tartrate; D010732:Phosphofructokinase-1; D005634:Fructose-Bisphosphate Aldolase; D005947:Glucose