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At least 19 recordsLinked to original sources
PubMed1975

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.

Animals↗
PubMed1977

Post-kala-azar dermal leishmaniasis.

Ten patients with post-kala-azar dermal leishmaniasis (2 females, 8 males-aged 17-47 years) are described. Two of them had macular lesions in which very few Leishman-Donovan bodies were seen and who responded well to treatment with stibophen. Five patients had both macular and nodular lesions, Leishman-Donovan bodies being present in nodules but not in macules. Treatment with stibophen caused partial regression of nodules. Nodular lesions were found in three patients, who did not have macules. They contained numerous Leishman-Donovan bodies and treatment produced only temporary improvement. The variable response to treatment with stibophen may have been due to differences in parasitic load. The difficulty in distinguishing this disease from leprosy is discussed.

Adolescent↗
PubMed1965

Laboratory studies on the joint effects of certain tris (p-aminophenyl) carbonium salts and antimonials as antischistosomal drugs.

Tris (p-aminophenyl) carbonium (TAC) pamoate and antimonials, such as tartar emetic and stibophen, have broad antischistosomal activity in animals and man, but both groups have important limitations. Thus the slow-acting TAC pamoate must be given for several weeks to obtain a high degree of effect and the fast-acting antimonials have a narrow therapeutic index.This study deals with whether TAC pamoate and antimonials together have a useful degree of joint action against Schistosoma mansoni without commensurate joint toxicity for the host.A marked degree of synergism in antischistosomal activity occurred with relatively low amounts of TAC pamoate and tartar emetic or stibophen in vitro and in infected mice, particularly when TAC pamoate was started ahead of the antimonial. Moreover, neither TAC pamoate nor tartar emetic affected appreciably the gross toxicity of the other for normal mice. An encouraging degree of joint antischistosomal action by TAC pamoate and tartar emetic also occurred in infected rhesus monkeys.The results suggest that the use of TAC pamoate and antimonials together may avoid some of their main limitations when used alone.

Animals↗
PubMed1984

Cyclic AMP-dependent and independent protein kinases in Ascaridia galli.

The occurrence of multiple protein kinases, distinguished with respect to molecular weight and preference for acceptor proteins, was demonstrated in Ascaridia galli. The molecular weights of the cyclic AMP-dependent protein kinase and of phosvitin kinase I and II - both independent of cyclic AMP-were determined to be 160000, greater than 200000 and 40000, respectively. The cyclic AMP-dependent protein kinase preferred histones and kemptide as acceptor substrates; stimulation of enzyme activity was up to 4-fold by cyclic AMP. The activities of phosvitin kinase I and II were found to be effectively inhibited by suramin. The inhibition constants were calculated to be 2 microM and 5 microM, respectively. In addition, stibophen turned out to be a potent inhibitor of phosvitin kinase I; the inhibition constant was determined to be 10 microM.

Animals↗