Saz H J, Dunbar G A
J Parasitol. 1975 Oct;61(5):794-801.
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.
三价有机锑化合物,如胺苯硫脲,已被用于治疗血吸虫病和丝虫感染。研究了胺苯硫脲对成年卡里尼丝虫、维氏双瓣线虫(= 维氏丝虫)和彭亨布鲁线虫的作用。在体外,锑化合物显著抑制了乳酸积累,同时也抑制了匀浆中的磷酸果糖激酶活性。将丝虫与胺苯硫脲一起孵育并测定己糖磷酸的内部浓度,也表明磷酸果糖激酶活性降低。此外,还观察到胺苯硫脲对醛缩酶的第二种抑制作用,这种作用似乎是胺苯硫脲特有的,酒石酸锑钾没有这种作用。这两种抑制活性可能都有助于胺苯硫脲的化疗效果。除了血吸虫和丝虫外,胺苯硫脲在低浓度时也能抑制蛔虫和微小膜壳绦虫的磷酸果糖激酶,而此时对相应的哺乳动物肝脏酶没有抑制作用。