ABSTRACT
The present study was undertaken to evaluate in vitro activities of following drugs against adult worms of Clororchis sinensis: i.e., stibnal, chloroquine diphosphate, Hetol (1,4-bis-trichloromethylbenzol), dehydroemetine 'Roche' (Ro 1-9334), niridazole (Ambilhar), bisbendazole, gentian violet, dithiazanine iodide, hexachlorophene, bithionol, niclofolan (Bilevon, Bayer 9015) and praziquantel (Embay 8440, Biltricide). After isolation from bile ducts of experimentally infected rabbits (3 months infection), the parasites were rinsed in sterilized Tyrode's solution and incubated for 24 hours at 37 C in TC 199 medium with Earle's balanced salt solution containing 0, 0.01, 0.1, 1.0, 10 and 100 microgram/ml concentrations of each above drugs. The activities of each concentrations with each drugs were evaluated by the motility of the worms in culture tubes observing at 15, 30, 60 minutes and 2, 4, 6, 12, 18 and 24 hours by stereomicroscope. In the results, no effect was found at the adult worms of C. sinensis in all concentrations with stibnal, chloroquine diphosphate, Hetol, dehydroemetine, niridazole and bisbendazole. However, moderate activities were observed in the concentrations of 1.0 and 0.1 microgram/ml of gentian violet, dithiazanine iodide, hexachlorophene and bithionol. The highest activities were observed in all concentrations of niclofolan and praziquantel.
Subject(s)
Clonorchis sinensis , Drug Therapy , In Vitro Techniques , Gentian Violet , Dithiazanine , Hexachlorophene , Bithionol , Niclofolan , PraziquantelABSTRACT
In order to find a highly efficient compound against Clonorchis infection, the anthelmintic activity of disophenol, Tremerad (SYD-230), dithiazanine iodide, dehydroemetine-late-release tablets(RO 1-9334/20), niridazole (Ambilhar), hexachlorophene (G-11), Hetol(1, 4-bis-trichloromethylbenzol) and Bilevon (niclofolan) was tested against Clonorchis sinensis experimentally infected rabbits. All drugs showed a progressive increase in efficacy as the dose rate. They were highly efficient against Clonorchis infection if sufficiently high, potentially toxic doses were given. The efficacy was evaluated by the number of detected worms with vital condition at autopsy after the treatment with above drugs. The high efficacy was observed at the following dose rates of each drugs, i.e. disophenol at a single dose of 30 mg/kg, Tremerad at the daily dose of 200 mg/kg for 10 consecutive days, dithiazanine iodide at the daily dose of 50 mg/kg for 6 consecutive days, dehydroemetine at the daily dose of 10 mg/kg for 10 consecutive days, hexachlorophene at the daily dose of 20 mg/kg for 10 to 15 consecutive days, Hetol at the daily doses from 50 to 100 mg/kg for 5 to 10 consecutive days, and Bilevon at a single dose of 8 mg/kg. Moderate effectiveness was shown in niridazole at the dose of 25 mg/kg for 10 days medication. The use of these anthelmintics for the clinical treatment of Clonorchis sinensis infection is discussed.
Subject(s)
DithiazanineABSTRACT
Authors carried out experimental study on chemotherapy with oral administration of Dithiazanine iodide (D.I.) and Bithionol sulfoxide(B.S.) in rabbit clonorchiasis. And the following result was obtained. In change of the E.P.G (eggs per gram feces) by D.I. administration, it was rather increased in early stage of the administration than prior to administration, and thereafter decreased gradually. In the change of the C.S. worm body by D.I. administration, there was not only prominent change of supporting tissue but also the change of reproductive organ was found. In considering the wormicidal effect of D.I. from detecting rate of survival worms, the effect was slight in group of 100 mg(80 mg/kg) per day dosage, but the effects were very excellent and almost complete by proper times of administration in groups of 200 mg (130 mg/kg) per day or higher dosage. But the side effect and intoxication sign of D.I. were appearent in groups of 200 mg or higher dosage. By B.S. administration, E.P.G. was decreased gradually. In changes of the C.S. worm body by B.S. administration, prominent inhibitory chnnge was seen in egg formation ability. Slight wormicidal effect of B.S. was observed in groups of 140 mg (100 mg/kg) per day or higher dosage. Side effect and intoxication sign of B.S. were found little in groups of 140 mg or lesser dosage.
Subject(s)
Clonorchis sinensis , Clonorchiasis , Drug Therapy , Dithiazanine , RabbitsABSTRACT
In the experimental rabbits which were previously infected with Clonorchis sinensis and were thereafter administered with Dithiazanine iodide, the patho-histological and some histochemical changes were observed in the healed liver(76 days after stoppage of egg excretion). And also, the patho-histological changes which appeared in the infected and healed livers respectively were compared from each other. The following results and conclusion were obtained. In the infected group, grossly the liver showed a considerable increase of its weight, an increased vascular marking of its surfaces and an increase in consistency and thickness of the bile ducts. However, the healed group grossly showed no remarkable changes in the liver. In the infected group, microscopically the liver showed a marked adenomatous hyperplasia of bile ducts, proliferation of bile ductules and marked periductal and periductular fibrosis with infiltration of chronic inflammatory cells in portal spaces. A histochemical study showed that the increased fibrous tissue consists largely with collagenous fibers and partly with reticulum fibers. In the group with healed liver microscopically the liver showed much improvement in the histopathological changes compared to those of the infected group. In the healed lover there remained only slight histopathological changes mainly in portal spaces of the liver, such as considerably diminished periductal and periductular fibrosis. The slightly increased fibrous tissue consists largely with reticulum fibers and partly with collagen fibers.