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PubMed2003

[Light- and temperature-induced degradation of fumagillin].

The antibiotic fumagillin with amebicidal and fungicidal effects isolated from Aspergillus fumigatus is the only presently known agent for the treatment of life threatening serious microsporidiosis occurring in patients with AIDS. Fumagillin and its degradation products were measured by HPLC at given time intervals after storage under defined conditions (temperature, relative humidity). Significant degradation took place even in samples stored in freezer; therefore fumagillin drug substance should be stored below -60 degrees C. Light also induced a degradation process in fumagillin, thus it is proposed to be stored and transported in brown glass.

Amebicides↗
PubMed2002

In vitro effect of artesunate against Acanthamoeba spp.

The in vitro effects of artesunate, the antimalarial agent, and metronidazole against Acanthamoeba spp were studied. Acanthamoeba Group II and Acanthamoeba polyphaga-like were isolated from natural water courses in Buri Ram Province, northeastern Thailand. The trophozoites were axenically cultured in PPYG medium and treated with artesunate in a concentration of 5-700 microg/ml. Artesunate showed its ability to inhibit the growth of acanthamoeba trophozoites: 54% at 50 mg/ml (after six days of exposure) and 93.2% at 100 microg/ml (after two days). The 500-700 microg/ml concentration caused inhibition on the first day of more than 93.2%; excystation did not occur in drug-treated medium. The present study shows that artesunate is amebastatic rather than amebicidal in an axenic culture of trophozoites at the highest concentration of 100 microg/ml. Metronidazole, in concentrations of 5-1,000 microg/ml, had no effects on either trophozoites or cysts.

Acanthamoeba↗
PubMed2004

Common intestinal parasites.

Intestinal parasites cause significant morbidity and mortality. Diseases caused by Enterobius vermicularis, Giardia lamblia, Ancylostoma duodenale, Necator americanus, and Entamoeba histolytica occur in the United States. E. vermicularis, or pinworm, causes irritation and sleep disturbances. Diagnosis can be made using the "cellophane tape test." Treatment includes mebendazole and household sanitation. Giardia causes nausea, vomiting, malabsorption, diarrhea, and weight loss. Stool ova and parasite studies are diagnostic. Treatment includes metronidazole. Sewage treatment, proper handwashing, and consumption of bottled water can be preventive. A. duodenale and N. americanus are hookworms that cause blood loss, anemia, pica, and wasting. Finding eggs in the feces is diagnostic. Treatments include albendazole, mebendazole, pyrantel pamoate, iron supplementation, and blood transfusion. Preventive measures include wearing shoes and treating sewage. E. histolytica can cause intestinal ulcerations, bloody diarrhea, weight loss, fever, gastrointestinal obstruction, and peritonitis. Amebas can cause abscesses in the liver that may rupture into the pleural space, peritoneum, or pericardium. Stool and serologic assays, biopsy, barium studies, and liver imaging have diagnostic merit. Therapy includes luminal and tissue amebicides to attack both life-cycle stages. Metronidazole, chloroquine, and aspiration are treatments for liver abscess. Careful sanitation and use of peeled foods and bottled water are preventive.

Adult↗
PubMedDate not supplied

[Growth inhibition of Entamoeba histolytica and E. invadens produced by pomegranate root (Punica granatum L.)].

The purpose of the present work has been to evaluate the biological activity of alkaloids and tannins extracted from roots of Punica granatum L. on axenic cultures from Entamoeba histolytica and E. invadens, strains. Initially, the total aqueous extract and later some of its components obtained by thin layer chromatography were tested. These compounds were identified by chromatography as alkaloids or tannins. The density of amebic cultures was determined with a hemocytometer after 48 and 96 hours of incubation, which was calculated by the difference between number of trophozoites obtained at the times chosen and the number of amoebae inoculated. Two milliliters of aqueous extract had higher activity on cultures from E. histolytica than E. invadens strains, producing growth inhibitions of about 100 and 40 per cent respectively. Alkaloid concentrations of 1 mg/ml had no amebicide activity, however tannins at concentrations of 10 micrograms/ml for E. histolytica, and 100 micrograms/ml for E. invadens were sufficient to produce an growth inhibition about 100 per cent. Tannic acid was also tested on the cultures of E. histolytica observing an high inhibitory activity on the growth, this effect was produced at 0.01 mg/ml was similar to that observed with the tannins mixture.

Alkaloids↗
PubMed1987

[Pathology, diagnosis and therapy of liver abscess].

Bacterial hepatic abscesses are a rare but serious disease. They develop either secondary to injuries or ischemia of the liver, infections in the drainage area of the portal vein, systemic sepsis or biliary infections. An abscess secondary to injuries or ischemia of the liver or infections in the drainage area of the portal vein, is usually caused by a mixed flora consisting of gramnegative aerobes and anaerobic bacteria. Hepatic abscesses secondary to systemic sepsis contain Staphylococci or Streptococci, while in abscesses on the basis of biliary infections gramnegative organisms are found. Clinically, one can find signs of systemic sepsis, pain in the right upper quadrant and a tender enlarged liver. Jaundice is absent unless a biliary obstruction is present simultaneously. The diagnosis is confirmed by ultrasonography or computerized tomography. An uncertain diagnosis can be confirmed by aspiration under ultrasonographic or computertomographic guidance. The therapy consists of administration of antibiotics and surgical or percutaneous drainage. Surgical drainage via laparotomy is always mandatory if one suspects a primary infectious focus within the abdomen. The mortality of multiple liver abscesses is 20 per cent, that of single abscesses 10 per cent. Amebic abscesses have been observed in nonendemic regions sporadically after travel or spontaneously. Clinical and radiological manifestations are the same as for bacterial abscesses. They are differentiated from bacterial abscesses by positive serology for amebiasis or aspiration which yields the typical anchovy paste. Most important complications are hepato-bronchial fistulae, empyema and amebic pericarditis. The therapy consists of a nitroimidazole and a luminal amebicide. Except for diagnostic reasons aspiration is only indicated for large abscesses of the left lobe of the liver. Mortality of an uncomplicated amebic liver abscess should be under one per cent.

Amebicides↗
PubMed1982

[Amebiasis].

Infections with Entamoeba histolytica do not necessarily cause disease in those infected. The parasite may act as commensal (cysts living in the bowel) or it may cause a broad spectrum of clinical illness. Some of the factors causing overt disease are poorly understood. An acute amebic dysentery is accompanied by bloody stools, abdominal pain and indigestion. The most important extraintestinal complication of an amebic infection is a liver abscess causing severe pain, fever, nausea and vomiting. The diagnosis of an amebic infection is based upon isolation of the parasite from the stools. Extraintestinal amebiasis is diagnosed - apart from the clinical picture - by serology. For treatment of intestinal amebiasis so-called contact-amebicides can be recommended. An amebic abscess of the liver usually responds well to dehydroemetine, metronidazole or any other derivative or imidazole and chloroquine. Surgical treatment of amebic liver abscess is only required if complications arise.

Amebiasis↗
PubMed1983

Treatment of chronic amebiasis in pediatric patients with a suspension of quinfamide.

Quinfamide, a dichloroacetyl quinolol synthesized and tested at Sterling Winthrop Research Institute, is a potent luminal amebicide with potential utility for a one-day treatment of chronic and subacute amebiasis caused by Entamoeba histolytica. Previous studies demonstrated that quinfamide is a safe and efficacious drug for adult patients when given as a one-day treatment regimen of 300 mg taken in tablet form at a dosage of 100 mg every eight hours. To test the drug in suspension form in pediatric patients, 46 children from newborn to 12 years old, assigned to groups according to age, were administered quinfamide in doses ranging from 50 to 300 mg/day as either single or divided doses. In all age groups quinfamide suspension, given as multiple doses in a single day, was shown to be highly effective in eliminating trophozoites from the stool. Cure rates ranged from 77.8% to 100%.

Age Factors↗
PubMedDate not supplied

[Clinical trial of etophamide in the treatment of chronic intestinal amebiasis].

The author present the results obtained in the treatment of 100 patients suffering chronic intestinal amebiasis, employing a new drug--Etophamide, in a dose of 1,0 g per day, for three consecutive days. The tolerance of a new antiamebic drug was excellent in all patients, and the parasitological cure rate obtained was 92%. The author concluded that the new derivate amebicide used in this research is very effective for treatment of intestinal amebiasis infections.

Acetamides↗
PubMed1993

Correlation of phospholipid loss in goat whole blood with solvochromic properties of antiamebics like emetine, metronidazole and diloxanide furoate.

Phospholipid content of whole blood lipid decreases significantly when goat blood is incubated for different length of time with different amebicidal agents (e.g., emetine, metronidazole and diloxanide furoate). The plots of relative per cent phosphate loss against incubation period show biphasic nature and suggest that the rates of phospholipid loss bears some relation with the drug's lipophilicity (log P in 1 octanol/water system). The absolute phospholipid loss seems to be governed by the drug's aquasolubility. Implication of these finding were discussed in terms of their clinical profiles assuming that the loss of phospholipid is due to drug's binding with the phospholipid layer in amebic cyst-coat, being the first step which may trigger a chain of events leading to the onset of drug action.

Amebicides↗
PubMed1977

Synthesis of some quinoline derivatives of potential antiamebic activity.

New compounds derived from cinchoninic acid esters and amides were prepared. The esters are those derived from p-hydroxy-N-methyldichloroacetanilide (diloxanide) whereas the amides are from piperazine whose hydrogen is substituted by a dichloroacetyl group. The dichloroacetamido group is responsible for the amebicidal activity in several related compounds.

Amebicides↗
PubMed1996

Energy production in Entamoeba histolytica: new perspectives in rational drug design.

The amebicidal action of metronidazole is activated when the enzyme pyruvate:ferredoxin oxido-reductase transfers reducing equivalents to the nitro group of the drug. The enzyme is present in Entamoeba histolytica and other anaerobic parasites like Giardia and Trichomonas that lack mitochondria. The selectivity of the drug can be ascribed to the absence of the reductase in the human host. E. histolytica possesses other enzymes involved in glucose catabolism that are interesting for the rational design of new drugs. It has glycolytic enzymes that are important for the production of energy like phosphofructokinase, pyruvate phosphate dikinase, phosphoenolpyruvate carboxytransphosphorylase and acetate thiokinase, which use pyrophosphate as a phosphate donor and have no human counterparts. The first part of this article describes the reactions by which E. histolytica obtains energy from glucose degradation, and includes recent advances in the cloning of genes for the various participating enzymes. The second part shows an alternative view for the study of target enzymes that are unique to the parasite, and indicates their importance in therapeutic research.

Amebicides↗
PubMed1976

Clinical trial methodology in intestinal parasitic diseases.

The high prevalence of intestinal parasitic infections as an index of underdevelopment, especially in tropical countries, is related to poverty, poor housing, lack of sanitation, malnutrition, and ignorance. The effects are lowered work capacity, physical and mental retardation, leading to recurrences and exacerbations of the parasitism and malnutrition. The most prevalent parasites, methods of detection by specific tests in patients in clinical trials involving antiparasitic drugs are dealt with. How and by whom investigations of new drugs should be undertaken, the need for a basic knowledge of parasitology and techniques of the discipline, of biostatistics, and use of such controls as randomized allotment to treatment groups, placebo administration, and double-blind assessments are emphasized. The justification for undertaking an evaluation of an antiparasitic drug is predicated on the demonstration of safety in exhaustive in vitro and animal studies and of the drug's potential superiority as to efficacy and lower incidence of unwanted side effects, as compared with existing agents. Tolerance and dose-range studies should be conducted in male adult hospitalized patients under close supervision. The evaluation of amebicides in clinical trials, as well as of anthelmintics, is considered in terms of differentiation and reproductive habits of specific causative agents and tests for detecting their elimination to determine improvement under drug therapy. The problem of reinfection, particuarly of nonhospitalized patients under the adverse conditions of life, is stressed.

Amebiasis↗
PubMed1989

Human neutrophils activated by interferon-gamma and tumour necrosis factor-alpha kill Entamoeba histolytica trophozoites in vitro.

The interaction between cytokine-activated human neutrophils and Entamoeba histolytica trophozoites was studied as well as the mechanism(s) involved. Treatment of neutrophils with rIFN-gamma alone allowed them to kill 30% of E. histolytica trophozoites; however, rIFN-gamma and rTNF-alpha pretreatments in combination increased neutrophil killing to 70%. In the absence of direct contact between neutrophils and amebae, rIFN-gamma-treated neutrophils were shown to kill 70% of amebae, and rIFN-gamma- and rTNF-alpha-treated neutrophils killed 97% of amebae. Neutrophil enhancement of amebicidal activity following cytokine treatments was correlated with increased neutrophil resistance to amebic contact-dependent killing and was shown to be 73% H2O2 dependent.

Animals↗
PubMed1978

Experimental muscular amebiasis in hamsters as a biological model.

Trophozoites of Entamoeba histolytica maintained in vitro in Pavlova's medium were inoculated by deep intramuscular injection into the proximal left hindleg of hamsters. Thioglycollate medium was utilized as a successful vehicle to induce the infection. The invasion of the muscular tissue by the vegetative forms caused the formation of abscesses with great destruction of muscular fibers. The lesions were limited to the muscular tissue of the femoral area. The number of trophozoites, the medium of thioglycollate as a vehicle, the volume of the inoculum and the trauma caused by the needle were important elements in the evolution of the muscular amebic abscesses. A limited trial of the amebicidal activity of metronidazole utilizing the amebic intramuscular infection was also performed.

Abscess↗
PubMed1978

Amebic liver abscess: 1966-1976.

A 10-year retrospective analysis of 15 patients with amebic liver abscess is reviewed and represents a continuation of the previous 2-decade experience at our institution (37 patients). Records were studied to determine the population affected, presenting symptoms, physical and laboratory findings, type and response to therapy. Most patients were rural males of lower socioeconomic status in the third to fifth decade of life. They presened as a febrile illness with abdominal pain for an average of 2 1/2 months duration. Significanct physical abnormalities were tender hepatomegaly (93%), right-sided pulmonary changes (40%), and fever (66%). All patients had abnormal liver scan, positive amebic serology, and hypoalbuminemia. All patients promptly responded to amebicidal therapy except one whose therapy was delayed. Clinical suspicion, liver scanning, serologic testing, and response to therapy are the keys to diagnosis.

Adult↗
PubMed1981

Effect of exogenous iron on the viability of pathogenic Naegleria fowleri in serum.

When Naegleria fowleri (Lee) was incubated in newborn calf and human serum an amebicidal effect was observed. Heat inactivation of both sera resulted in the recovery of viable amebae after incubation in these sera. Exogenous iron added to non-heat inactivated calf serum improved viability slightly but was without effect when added to human serum not heat inactivated. Exogenous iron greatly enhanced growth and/or viability in heat inactivated calf serum. Viability of amebae also was considerably enhanced in human serum which was heat inactivated when pH was lowered in conjunction with iron supplements.

Amoeba↗
PubMed1994

Hepatic abscess caused by Salmonella typhi. A case report and review of the literature.

Salmonella typhi is a rare cause of liver abscess. We describe a 47-year-old African male with multiple liver abscesses due to S. typhi in an area where hepatic amebiasis is endemic. The patient did not respond appropriately to amebicidal therapy and culture of the liver aspirate on two occasions yielded S. typhi. The Widal test, initially negative, became positive on repeat testing 10 days later. Percutaneous aspiration combined with appropriate antibiotic therapy resulted in a complete recovery. No predisposing cause could be found. We report the clinical, radiological, and microbiological features of this case and review the literature on this rare but easily treatable condition.

Humans↗