Contact photodermatitis due to bithionol and related compounds.
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Anti-Infective Agents, Local↗
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[Immunoelectrophoresis For Anthelmintics Evaluation Against Experimental Paragonimiasis]
Paragonimiasis is one of the most important endemic diseases in Korea. However, recognition of the limitation of microscopic examination of sputum and feces for Paragonimus eggs has led to the investigation of immunoserological techniques for paragonimiasis. The other hand, bithionol preparation has been used as a drug of choice in paragonimiasis but recently niclofolan preparation has introduced as a new agent. By the time, the authors attempted the evaluation of above both agents against experimental rat paragonimiasis by immunoelectrophoresis and Ouchterlony test. The immunoeletrophoresis and Ouchterlony tests were performed according to the method Tsuji and Grabar et Williams respectively, with antigen extracted from lyophilized worm of P. westermani with 0.1 per cemt saline solution. Meanwhile, rats were infected with per os 20 metacercariae of P. westermani above two kinds of serologic tests and were undertaken at biweekly intervals. Then, bithionol was administered every other day for 5 successively for 2 weeks or 6 weeks after infection. Another groups, niclofolan was administered per os single dose same as above. 1. The sera from the rats infected with P. westermani, after treatment with bithionol or niclofolan preparations began to show the precipitin bands against P. westermani antigen 8 weeks after the infection in immunoelectrophoresis and Ouchterlony test, but from 10 or 12 weeks after infection, the number of bands were decreased or disappeared gradually. 2. In genera1, the sera from the rats treated with bithionol or niclofolan showed the precipitin bands delaying 2 weeks than control rat groups. 3. The sera from the rats administered with hydrocortisone showed precipitin bands neither in immunoelectrophoresis nor in Ouchterlony test.
Journal Article↗
Induction of keratinocyte apoptosis by photosensitizing chemicals plus UVA.
BACKGROUND: The capacity of photosensitizing chemicals with ultraviolet A light (UVA) to induce apoptosis is one of the methods to assess their phototoxic and potentially photoallergic properties, since apoptotic cells may be easily presented by antigen-presenting cells. OBJECTIVES: We examined the photoaggravated ability to induce keratinocyte apoptosis of various chemicals that are known as causative agents of photocontact dermatitis and drug photosensitivity involving photoallergic and/or phototoxic mechanisms. METHODS: HaCaT keratinocytes were incubated with 3,3',4',5-tetrachlorosalicylanilide (TCSA), bithionol, diphenylhydramine, chlorpromazine, 6-methylcoumarin, sparfloxacin, and enoxacin at 10(-7) to 10(-4)M and irradiated with UVA at 4J/cm(2). As positive control, 8-methoxypsoralen (8-MOP) was also tested. Apoptosis and necrosis were evaluated by flow cytometric enumeration of annexin V(+) 7-AAD(-) and annexin V(+) 7-AAD(+) cells, respectively. The expression of apoptosis-related molecules, caspase-3 and poly (ADP-ribose) polymerase (PARP), was tested by flow cytometric and Western blotting analyses. RESULTS: In a comparison with non-irradiated cells, significant apoptosis was found in TCSA, bithionol, chlorpromazine, sparfloxacin and enoxacin at 10(-4) or 10(-5)M as well as 8-MOP as assessed by both annexin V and active caspase-3 stainings, while necrosis occurred in most of these chemicals at 10(-4)M. Neither apoptosis nor necrosis was seen in diphenylhydramine or 6-methylcoumarin. PARP were activated in HaCaT cells phototreated with TCSA, bithionol and chlorpromazine. CONCLUSIONS: We suggest that our method is useful for in vitro assessment of phototoxicity and potential photoallergenicity of chemicals.
Anesthetics, Local↗
Synthetic polymers as drugs.
Biologically active compounds have been incorporated into synthetic polymers. Bithionol, a well-known and potent antibacterial agent, has been used as bisphenol monomers for polyesters, polyphosphates, and phosphonates; the bischloroformate of bithionol has been converted into copolycarbonates and polyurethanes. The copolycarbonates of bithionol, optimally designed polymer structures with poly(ethylene oxide) glycols as the other comonomer, have been hydrolyzed under physiological conditions at a degradation rate of about 1% per day. Primaquine, an antimalarial, and amantadine, an antiviral agent, when reacted with isocyanates gave polymeric biurets as do other primary aliphatic amines. Primaquine also underwent nucleophilic substitution reactions on polyepichlorohydrin. 3-Vinyl-, 4-vinyl-, and 5-vinylsalicylic acids have been synthesized, polymerized, and copolymerized to polymeric antibacterials. Copolymers of vinylsalicylic acid can be selective in their activity, depending on the comonomer. Selectivity can also be achieved by derivation of the poly(vinylsalicylic acid).
Anti-Bacterial Agents↗
Fasciola hepatica infection: clinical and computerized tomographic findings of ten patients.
BACKGROUND/AIMS: Fasciola hepatica is the cause of liver infection, fascioliasis. Although rare, it is still a problem even in developed countries. In this study, the clinical and computerized tomographic findings of 10 patients diagnosed with fascioliasis are summarized. METHODS: The medical records of the patients with fascioliasis were retrospectively examined. Clinical, laboratory findings and computerized tomographic results were recorded. RESULTS: Abdominal pain, fever, eosinophilia and abnormal liver function tests were the most commonly encountered symptoms and signs. One patient was human immunodeficiency virus -positive with active tuberculosis. Serologic test for fasciola hepatica was positive in all patients. Nodular masses without prominent enhancement, and branching low-attenuated tubular lesions were the most commonly seen tomographic findings and were supportive for the diagnosis. All except the HIV-positive patient received bithionol therapy; six patients responded well, two lost contact with the clinic and one patient who was unresponsive to bithionol therapy received triclabendazole. During follow-up of the six patients who responded, all the clinical and radiological findings regressed. CONCLUSION: In any patient with peripheral eosinophilia, abdominal pain and elevated liver enzymes, especially when CT reveals tubular and nodular hypodense lesions particularly in subcapsular area, F. hepatica infection should be considered. Either triclabendazole or bithionol can be used effectively for the treatment.
Abdominal Pain↗
Treatment of human taeniasis in the Philippines: a review.
Studies relating to the treatment of human taeniasis in the Philippines using Atabrine, bithionol, and mebendazole are reviewed. Cure rates of 93.7% for Atabrine, 85%-100% for bithionol, and 84.62% for mebendazole are reported. Aside from these studies, recent experience in the treatment of Taenia saginata infections at the Department of Parasitology, College of Public Health, is also reported. Twenty patients referred to the department were treated, 3 with bithionol, 17 with praziquantel. Of the 17 patients treated with praziquantel, the study reported cure rates of 47-88.24%.
Bithionol↗
Mass Chemotherapy In The Control Of Paragonimiasis.
Among 11,005 inhabitants(61% of total population) surveyed in 13 villages of Che Ju Island in 1964, were identified as paragonimiasis patients, of these 1,355 were treated with 40 mg/kg body weight of bithionol for 10~15 doses. The purpose of the study was to test whether mass chemotherapy of the human host may provie an answer for the control of paragonimiasis in an area where the human host is main source of infection to the intermediate hosts. The efficacy of the mass chemotherapy as control program was measured by the acceptance of the survey and treatment by the inhabitants, the efficacy and the toxicity of the drug applied, and the influence of the infection rates of the intermediate hosts. The acceptance of the survey and the treatment was not entirely satisfactory: an estimate based on data suggests that only fifty to sixty percent of all cases infected were detected, and 93% of detected cases were treated in the primary program. All cases detected during the follow up survey, which could not cover whole population, were treated. The efficacy of bithionol was excellent when the treatment was completed. 40 mg/kg body weight for 10~15 doses was sufficient to turn the sputum egg-negative except in a few cases infected heavily that needed 20 doses. Side reactions were generally mild; the most frequent reaction was gastrointestinal; which spontaneously subsided within a few to several days. The infection rate of intermediate hosts started to decrease from the third year of the mass treatment with a pattern of gradual drop. Follow up studies on general population in three and four years of the mass treatment also showed markedly decreased prevalence of paragonimiasis by intradermal test and sputum examination. It is concluded that a complete mass chemotherapy with bithionol in an area where human is the main source of infection to the intermediate hosts can be the answer for control of paragonimiasis.
Journal Article↗
Pulmonary paragonimiasis: clinical features, diagnosis and treatment of 39 cases in Manipur.
Thirty-nine cases of pulmonary paragonimiasis due to Paragonimus westermani were identified in Manipur, India. Recurrent haemoptysis, often increased on exertion, was the most common symptom. The clinical features and radiological appearances simulated pulmonary tuberculosis and 23 cases were treated for tuberculosis for varying periods before the final diagnosis. Young males aged 11 to 30 years comprised two-thirds of the cases. The disease was acquired by eating raw or improperly cooked crabs (Potamon deham). Intradermal tests (IDT) employing a saline extract of adult Paragonimus were a simple and reliable method of detecting present or past infection. Erythema of large size even without wheal and pseudopodia may indicate a positive IDT. Charcot-Leyden crystals (CLC) were detected in all sputum samples positive for Paragonimus ova. In patients (four) presenting with pleural effusion, Paragonimus ova were not present in the sputum, stool or pleural fluid. Bithionol (2,2'-thiobis [4,6-dichlorophenol]) orally, 40 mg/kg body-weight/day, 10 to 25 doses, cured all cases and, except in one, side effects were minimal. Relapse in one patient after six months' treatment was apparently cured by a second course of Bithionol.
Adolescent↗
Pharmacological activation and inhibition of Slack (Slo2.2) channels.
The Slack (Sequence like a calcium-activated K channel) (Slo2.2) gene is abundantly expressed in the mammalian brain and encodes a sodium-activated K+ (KNa) channel. Although the specific roles of Slack channel subunits in neurons remain to be identified, they may play a role in the adaptation of firing rate and in protection against ischemic injury. In the present study, we have generated a stable cell line expressing the Slack channel, and have analyzed the pharmacological properties of these channels in these cells and in Xenopus oocytes. Two known blockers of KNa channels, bepridil and quinidine, inhibited Slack currents in a concentration-dependent manner and decreased channel activity in excised membrane patches. The inhibition by bepridil was potent, with an IC50 of 1.0 microM for inhibition of Slack currents in HEK cells. In contrast, bithionol was found to be a robust activator of Slack currents. When applied to the extracellular face of excised patches, bithionol rapidly induced a reversible increase in channel opening, suggesting that it acts on Slack channels relatively directly. These data establish an important early characterization of agents that modulate Slack channels, a process essential for the experimental manipulation of Slack currents in neurons.
Animals↗
The induction of photocontact sensitivity in guinea pigs without UVB radiation.
Allergic photocontact sensitization could be induced in guinea pigs with 3,3',4',5-tetrachlorosalicylanilide (TCSA), 3,4',5-tribromosalicylanilide (TBS), and bithionol using pretreatment with sodium lauryl sulfate (SLS) and long-wave ultraviolet (UVA) radiation. Mid-wave ultraviolet below 320 nm (UVB) was not necessary for the induction of sensitization. Combined use of SLS pretreatment with UVA radiation resulted in more effective sensitization than combined UVB and UVA radiation. Higher sensitization rates to TCSA and TBS were achieved by allowing rest periods between each of 5 2-hr exposures to UVA than by daily 1-hr exposures for 10 consecutive days. The opposite result was obtained with bithionol. Although UVB has been customarily used in the past for induction of photosensitivity, its role is only to irritate the site of induction.
Animals↗
Experimental chemotherapy of paragonimiasis. A review.
The ideal type of an anthelmintic drug should be effective against the parasite and not toxic to the host. In early studies of this disease in Japan, a large number of different drugs was tested, none of which was promising enough. In 1956, an in vitro screening method for effective drugs against Paragonimus westermani was established. It was also found (1961) that rats experimentally infected with P. ohirai can be successfully employed for chemotherapeutic studies of paragonimiasis in place of dogs and cats infected with P. westermani. Thus, bithionol has been found to have a strong therapeutic effect against pulmonary paragonimiasis and is now used not only for individual treatment but also for mass treatment in endemic areas. However, it proved difficult to administer bithionol over 20 days because of reduced patient compliance, especially in patients of population based chemotherapy. To ensure good patient compliance and easy administration in such campaigns for disease control, treatment must be simple and given over a minimum period of time. Praziquantel (2-cyclohexylcarbonyl-1,2,3,6,7,11b-hexahydro-4H-pyrazino[2,1-a]++ +isoquinolin- 4-one, EMBAY 8440, Biltricide) is a recently introduced drug that has the unique characteristic of being effective in the treatment of infections with all schistosome species pathogenic to man and many other human trematode and cestode infections, and it has to be given on 1 to 2 days only. In this paper, the effects of praziquantel against Paragonimus in vitro using metacercariae of P. ohirai and rats experimentally infected with P. ohirai are described.
Animals↗
A predictive mouse ear-swelling model for investigating topical photoallergy.
The photoallergic potential of various compounds was assessed using a mouse ear-swelling model, which offers the advantage of being quantifiable and more objective than models based on subjective evaluation of erythematous skin reactions. Cyclophosphamide pretreated BALB/c mice were induced by topical treatment of the dorsal skin surface on 3 consecutive days and challenged on the ears 5 days after the last induction. For each induction and challenge treatment, mice were consecutively irradiated with ultraviolet (UV) A (10 J/cm2) and UVB (45 mJ/cm2) radiation 30 min to 1 hr after test material application. The photoallergic response to musk ambrette, a known human photoallergen, was significantly augmented when three consecutive induction exposures were used as compared with one or two inductions. The photoallergic potential of nine other known human photoallergens (tetrachlorosalicylanilide, bithionol, 6-methylcoumarin, chlorpromazine, sodium omadine, bisphenol A, sulphanilamide, fentichlor and p-aminobenzoic acid) was successfully detected using the mouse model. In each experiment, the ear thickness changes observed in the photoallergy test mice were significantly greater than the changes observed in the contact allergy, vehicle/radiation and phototoxicity control mice. Coumarin and homosalate, two agents not traditionally associated with causing photoallergy in humans or animals, did not demonstrate contact photoallergy using this model. With three of the photoallergens, musk ambrette, bithionol and tetrachlorosalicylanilide, the ear swelling response obtained was due to photoallergy alone and not due to the co-existence of both contact photoallergy and contact allergy. In addition, irradiating mice 24 hr, rather than 1 hr, following application of the test material during the induction phase resulted in a significantly reduced photoallergic response with both musk ambrette and tetrachlorosalicylanilide. These results indicate that the mouse ear-swelling model is a potentially useful model for investigative and predictive photoallergy testing.
Administration, Topical↗
[Fasciola hepatica. study of a series of 37 patients].
BACKGROUND: To analyze the clinical, bacteriologic, diagnostic and therapeutic features of patients with Fasciola hepatica (FH) in our hospital. PATIENTS AND METHOD: We reviewed all the patients with a diagnosis of fascioliasis from 1975 to 1999 in the Aranzazu Hospital in San Sebastián (Guipúzcoa, Spain). Diagnosis was made by direct vision of adult parasites during surgery and/or the presence of ova in stool examinations and/or positive serologic tests in patients with symptoms consistent with parasitosis. RESULTS: Thirty-seven patients were included (23 men and 14 women), aged 19 to 71 years. Ingestion of watercress was confirmed in 27. Seven cases occurred as part of familiar outbreaks. Thirty-two were in the liver invasive stage and in 5 the biliary tree was invaded. The most common features were eosinophilia (91.8%), malaise and weight loss (75.6%), elevated alkaline phosphatase (74.2%), and abdominal pain (72.9%). Adult worms in the biliary ducts were observed in 3 patients and ova in feces were observed in 6. In 13 of 27 patients indirect hemagglutination test was ( 1/1,280. Data significant to confirmation of liver involvement were provided by laparoscopy in 12 of 13 patients and by imaging techniques in 13 of 31 patients. Four patients had cholelithiasis and of these, 2 also showed adult parasites in the common bile duct. Three patients underwent surgery. Therapy with dehydroemetine and/or bithionol was followed by complete remission in 30 patients, although 6 required repeat treatment cycles. The remaining 4 patients were cured by praziquantel. CONCLUSIONS: Most of the patients in these series reported consumption of watercress and all patients showed the symptoms typical of parasite disease. Imaging techniques proved to be of great utility in confirming the diagnosis of hepato-biliary disease. In most of the patients therapy with dehydroemetine and/or bithionol (in one or several cycles) was followed by complete remission.
Adult↗
Identification of a 17-kilodalton Fasciola hepatica immunodiagnostic antigen by the enzyme-linked immunoelectrotransfer blot technique.
Sera obtained from human patients, calves, sheep, and rabbits infected with Fasciola hepatica were tested by the Falcon assay screening test enzyme-linked immunosorbent assay (FAST-ELISA) and the enzyme-linked immunoelectrotransfer blot (EITB) techniques with Fasciola hepatica excretory-secretory antigens in order to evaluate their immunodiagnostic potential. The study included sera from 13 patients infected with F. hepatica or a history suggesting fascioliasis, 5 patients infected and treated with bithionol or praziquantel (3 were cured with bithionol), 10 patients infected with Schistosoma mansoni, 6 infected with Trichinella spiralis, and 13 controls and sera from calves, sheep, and rabbits with a primary F. hepatica infection. By FAST-ELISA with F. hepatica excretory-secretory antigens, the serum samples from fascioliasis patients gave the highest absorbance values, and the schistosomiasis patient sera gave intermediate values compared with a normal human serum control. Also by FAST-ELISA, the values for serum from patients with fascioliasis decreased steadily after cure, reaching normal levels 20 to 47 weeks postcure. In contrast, the serum from two patients who had been treated but were not yet cured had high levels of antibodies for up to 3 years of infection. By EITB, the serum samples from humans, rabbits, cattle, and sheep with fascioliasis recognized two antigenic polypeptides of 17 and 63 kilodaltons (kDa) in the form of sharp bands. For humans, this recognition lasted for at least 3 years of infection. Sera from individuals with schistosomiasis mansoni or trichinosis or from normal controls did not recognize the 17-kDa F. hepatica antigenic polypeptide. However, serum from one human with S. mansoni and one with T. spiralis infection has slight bands in the 63-kDa region, suggesting cross-reactivity. Reactivity to the 17-kDa polypeptide was absent in fascioliasis patients at 1 year postcure. Reactivity to the 63-kDa polypeptide was significantly diminished in fascioliasis patients at 1 year postcure. The sera from rabbits with a primary F. hepatica infection also recognized both the 17- and 63-kDa antigenic polypeptides by week 4 of infection. Reactivity to both antigens diminished significantly 6 weeks postcure and disappeared by 8 weeks postcure. The sera from infected cattle and sheep recognized these two antigenic polypeptides by week 8 of infection. These studies suggest that the 17-kDa F. hepatica excretory secretory antigen is an excellent candidate for the immunodiagnosis of acute and chronic fascioliasis. Purification of this antigen and its application to quantitative serologic tests will permit further analysis of its predictive value to evaluate cure.
Animals↗
[Anthelmintic Effects Of Various Drugs Against Metagonimiasis]
The infection of Metagonimus yokogawai has been known to be present nationwidely and endemic in some parts in Korea. In order to select a highly effective compound against Metagonimus infections, the therapeutic effects were observed in 156 cases who were treated with several anthelmintic i.e. bithionol, niclosamide, niclofolan and praziquantel. All of the above drugs showed highly effective to the treatment of metagonimiasis by a single or two medication days. The egg reduction rates were in the range of 80.2 to 100 per cent. However, relatively low cure rates(8.3 to 37.5%) were observed in the groups treated by two doses of 30 mg/kg of bithionol, a single day treatment with 100 mg/kg of niclosamide and two doses of 1.0 mg/kg of niclofolan. On the other hand, the high cure rates were observed at the following dose rates of each drugs, i.e. the cure rate of 66.7% was obtained at two doses of 100 mg/kg of niclosamide, 88.9% of cure rate was observed at two doses of 2.0 mg/kg of niclofolan and a single dose of 10 and 20 mg/kg of praziquantel were shown as 85.0% and 88.0% of cure rates respectively. But the complete radical cure was obtained in the group treated by two doses of 20 mg/kg of praziquantel in 10 metagonimiasis cases. From the above results praziquantel was shown as the most highly effective against metagonimiasis and it was well tolerated without any side effect. Therefore, praziquantel is a very promising drug for mass treatment against metagonimiasis.
Journal Article↗
[In Vitro Activities Of Various Drugs Against Adult Worms Of Clonorchis Sinensis]
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 degrees 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.
Journal Article↗
Antiprotozoals effective in vitro against the scuticociliate fish pathogen Philasterides dicentrarchi.
The histophagous ciliate Philasterides dicentrarchi causes fatal scuticociliatosis in farmed turbot Scophthalmus maximus and sea bass Dicentrarchus labrax. The present study screened 52 candidate antiprotozoals for activity against this pathogen in vitro. Of these compounds, 14 were effective (i.e. killed all ciliates within a 24 h assay period). In descending order of efficacy (minimum lethal concentration 100 to 0.8 ppm), these were niclosamide, oxyclozanide, bithionol sulfoxide, toltrazuril, N-(2'-hydroxy-5'-chloro-benzoyl) 2-chloro-4-nitroaniline, furaltadone, doxycycline hyclate, formalin, albendazole, carnidazole, pyrimethamine, quinacrine hydrochloride and quinine sulfate. Administration in filtered seawater rather than phosphate-buffered saline inactivated doxycycline hyclate and albendazole, and markedly reduced that of bithionol sulfoxide and toltrazuril, suggesting that these compounds may not be effective in bath administration. In view of these findings, we discuss the potential utility of chemotherapy as a strategy for the control of scuticociliatosis in farmed turbot and sea bass.
Animals↗
Trichomonas species: homocysteine desulphurase and serine sulphydrase activities.
Homocysteine desulphurase (EC 4.4.1.2) and serine sulphydrase (EC 4.2.1.22) activities in various lines of Trichomonas vaginalis, both metronidazole resistant and sensitive, and other trichomonad species were assessed. T. vaginalis contained the highest homocysteine desulphurase and serine sulphydrase activities of all the species. Although the levels of the enzyme activity in T. vaginalis isolates differed, no correlation between the activities and sensitivity to metronidazole was apparent. T. vaginalis homocysteine desulphurase catalysed both the hydrolysis of homocysteine to hydrogen sulphide, ammonia, and 2-oxoacid, and an exchange reaction between homocysteine and 2-mercaptoethanol. Homocysteine desulphurase was detected as a single enzyme band on isoelectric focusing, whereas several isoenzymes of serine sulphydrase were found. There were large differences in serine sulphydrase isoenzyme patterns between T. vaginalis lines and between species. Several isoenzymes were amplified in cells grown with 10(-5) M DL-propargylglycine for 24 hr. T. vaginalis homocysteine desulphurase and serine sulphydrase activities were inhibited by bithionol, hexachlorophene, and dichlorophene. These compounds also inhibited growth in vitro of T. vaginalis at concentrations similar to those that inhibited the enzymes.
Alkynes↗