Lamb, David C.; Warrilow, Andrew G. S.; Rolley, Nicola J.; Parker, Josie E.; Nes, W. David; Smith, Stephen N; Kelly, Diane E.; Kelly, Steven L.
In this study, we investigate the amebicidal activities of the pharmaceutical triazole CYP51 inhibitors fluconazole, itraconazole, and voriconazole against Acanthamoeba castellanii and Acanthamoeba polyphaga and assess their potential as therapeutic agents against Acanthamoeba infections in humans. Amebicidal activities of the triazoles were assessed by in vitro minimum inhibition concentration (MIC) determinations using trophozoites of A. castellanii and A. polyphaga. In addition, triazole e...
Full Text Available 328.1474 D02480.gif Antiprotozoal, Amebicide [DS:H00360] Same as: C07637 ATC code: P01AC01 Anatomical Thera... Antiparasitics Agents against Amebiasis and other antiprotozoals Dichloroacetamide derivatives Diloxanide [
Chloroquine phosphate is in a class of drugs called antimalarials and amebicides. It is used to prevent and treat ... Chloroquine phosphate comes as a tablet to take by mouth. For prevention of malaria in adults, one dose is ...
Full Text Available D07353 Drug Secnidazole (INN); Secnidal (TN) C7H11N3O3 185.08 185.1805 D07353.gif Antiprotozoa...l, amebicide; Antiprotozoal, trichomonacidal ATC code: P01AB07 Anatomical Therapeutic Chemical (A...nst Amebiasis and other antiprotozoals Nitroimidazole derivatives Secnidazole [ATC:P01AB07] D07353 Secnidazo
Lin, J. Y.; Seguin, R; K. Keller; Chadee, K
Nitric oxide (NO measured as nitrite, NO2-) is the major effector molecule produced by activated macrophages for in vitro cytotoxicity against Entamoeba histolytica trophozoites. In this study, we determine whether tumor necrosis factor alpha (TNF-alpha) produced by activated bone marrow-derived macrophages (BMM) is involved in the induction of the inducible NO synthase gene (mac-NOS) for NO-dependent amebicidal activity. TNF-alpha alone did not directly induce macrophage NO2- production to k...
Iasmine A.B.S. Alves; Henrique M. Miranda; Luiz A. L. Soares; Karina P. Randau
The Simaroubaceae family includes 32 genera and more than 170 species of trees and brushes of pantropical distribution. The main distribution hot spots are located at tropical areas of America, extending to Africa, Madagascar and regions of Australia bathed by the Pacific. This family is characterized by the presence of quassinoids, secondary metabolites responsible of a wide spectrum of biological activities such as antitumor, antimalarial, antiviral, insecticide, feeding deterrent, amebicid...
Lamb, David C; Warrilow, Andrew G S; Rolley, Nicola J; Parker, Josie E; Nes, W David; Smith, Stephen N; Kelly, Diane E; Kelly, Steven L
In this study, we investigate the amebicidal activities of the pharmaceutical triazole CYP51 inhibitors fluconazole, itraconazole, and voriconazole against Acanthamoeba castellanii and Acanthamoeba polyphaga and assess their potential as therapeutic agents against Acanthamoeba infections in humans. Amebicidal activities of the triazoles were assessed by in vitro minimum inhibition concentration (MIC) determinations using trophozoites of A. castellanii and A. polyphaga. In addition, triazole effectiveness was assessed by ligand binding studies and inhibition of CYP51 activity of purified A. castellanii CYP51 (AcCYP51) that was heterologously expressed in Escherichia coli. Itraconazole and voriconazole bound tightly to AcCYP51 (dissociation constant [Kd] of 10 and 13 nM), whereas fluconazole bound weakly (Kd of 2,137 nM). Both itraconazole and voriconazole were confirmed to be strong inhibitors of AcCYP51 activity (50% inhibitory concentrations [IC50] of 0.23 and 0.39 μM), whereas inhibition by fluconazole was weak (IC50, 30 μM). However, itraconazole was 8- to 16-fold less effective (MIC, 16 mg/liter) at inhibiting A. polyphaga and A. castellanii cell proliferation than voriconazole (MIC, 1 to 2 mg/liter), while fluconazole did not inhibit Acanthamoeba cell division (MIC, >64 mg/liter) in vitro. Voriconazole was an effective inhibitor of trophozoite proliferation for A. castellanii and A. polyphaga; therefore, it should be evaluated in trials versus itraconazole for controlling Acanthamoeba infections. PMID:26014948
Iasmine A.B.S. Alves
Full Text Available The Simaroubaceae family includes 32 genera and more than 170 species of trees and brushes of pantropical distribution. The main distribution hot spots are located at tropical areas of America, extending to Africa, Madagascar and regions of Australia bathed by the Pacific. This family is characterized by the presence of quassinoids, secondary metabolites responsible of a wide spectrum of biological activities such as antitumor, antimalarial, antiviral, insecticide, feeding deterrent, amebicide, antiparasitic and herbicidal. Although the chemical and pharmacological potential of Simaroubaceae family as well as its participation in official compendia; such as British, German, French and Brazilian pharmacopoeias, and patent registration, many of its species have not been studied yet. In order to direct further investigation to approach detailed botanical, chemical and pharmacological aspects of the Simaroubaceae, the present work reviews the information regarding the main genera of the family up to 2013.
Full Text Available Although amebic liver abscess can be a cause of significant morbidity and mortality in all ages, there are few reports dealing with this entity in children. Twenty-four children with amebic liver abscess. Ages ranging between 8 weeks and 14.5 years were managed at the Tehran university hospital of children, Iran, between November 1987, and October 2001. The most frequency presentation was high-grade fever and right upper quadrant pain, associated with tender hepatomegaly, leukocytosis and an elevated erythrocyte sedimentation rate. The diagnosis was confirmed by elevated indirect hemagglutination titers and ultrasonograpy of the liver. Unlike the experience in adult patients, none of the patients had concomitant jaundice and significant derangement of liver enzymes. The abscesses were likely to be solitary (22 of 24 patients. There were 17 males and 7 females. Most patients (80% were between 8 weeks to 14.5 years of age. In five patients possible predisposing factors were tuberculosis, chickenpox, tetralogy of fallot and thalassemia major. All patients received metronidazole (50 mg/kg/day, followed by a therapeutic course of a luminal amebicide. There was no death despite a mean delay of 15 days before presentation to our hospital. In conclusion a high index of suspicion, early institution of metronidazole therapy and aspiration of abscesses with potential to rupture are believed to have contributed to the better outcome in these children when compared with results in previous reports.
Avaliação do extrato hidroalcoólico de Mentha crispa sobre a performance reprodutiva em ratos Wistar Evaluation of the hydroalcoholic extract of Mentha crispa on the reproductive performance in Wistar rats
Gustavo Santiago Dimech
Full Text Available A Mentha crispa (Lamiaceae é conhecida popularmente como hortelã-da-folha-miúda. O extrato hidroalcoólico (EHA de Mentha crispa, obtido do caule e da folha, possui atividade amebicida (Entamoeba histolytica e giardicida (Giardia lamblia e é explorado comercialmente na produção do fitoterápico Giamebil plus®. Os efeitos da administração oral subcrônica do EHA de Mentha crispa foram investigados sobre a performance reprodutiva em ratos Wistar adultos. Três grupos de ratos machos (n=6-12/grupo foram tratados durante 30 dias consecutivos com EHA por via oral nas doses de 0,5 e 1,0 g/kg de peso ou água destilada (grupo controle. Em seguida, foram determinados os índices reprodutivos, massa dos órgãos e análise morfológica do testículo, epidídimo e ducto deferente. Os resultados mostram que, durante o período de tratamento, não se observaram sinais de toxicidade ou morte dos animais. Os índices reprodutivos, assim como a massa e as morfologias macro e microscópica dos órgãos não foram modificados pela administração subcrônica do EHA. Dessa forma, conclui-se que a administração subcrônica do extrato hidroalcoólico de Mentha crispa (Giamebil plus® não possui atividade contraceptiva sobre o sistema reprodutor de ratos Wistar.Mentha crispa (Lamiaceae is commonly known as "hortelã-da-folha-miúda". The hydroalcoholic extract (HAE from the leaves and stem of Mentha crispa possesses amebicidal (Entamoeba histolytica and giardicidal (Giardia lamblia activity and it is commercially used in the production of the phytoterapic Giamebil plus®. The effects of the subchronic administration of the HAE of Mentha crispa were investigated on reproductive performance in adult Wistar rats. Three groups of male rats (n=6-12/group were orally treated daily for 30 consecutive days with the HAE at doses of 0.5 and 1.0 g/kg or distilled water (control group. Then, the reproductive indices, the organ weight and the morphologic analysis of