RESUMEN
Leishmaniasis is an infectious disease caused by protozoan parasites of the genus Leishmania. The treatment of all forms of leishmaniasis relies on first-line drug, pentavalent antimonial, and in cases of drug failure, the second-line drug amphotericin B has been used. Besides the high toxicity of drugs, parasites can be resistant to antimonial in some areas of the World, making it necessary to perform further studies for the characterization of new antileishmanial agents. Thus, the aim of the present work was to evaluate the leishmanicidal activity of tolnaftate, a selective reversible and non-competitive inhibitor of the fungal enzyme squalene epoxidase, which is involved in the biosynthesis of ergosterol, essential to maintain membrane physiology in fungi as well as trypanosomatids. Tolnaftate eliminated promastigote forms of L. (L.) amazonensis, L. (V.) braziliensis and L. (L.) infantum (EC50 ~ 10 µg/mL and SI ~ 20 for all leishmanial species), and intracellular amastigote forms of all studied species (EC50 ~ 23 µg/mL in infections caused by dermatotropic species; and 11.7 µg/mL in infection caused by viscerotropic species) with high selectivity toward parasites [SI ~ 8 in infections caused by dermatotropic species and 17.4 for viscerotropic specie]. Promastigote forms of L. (L.) amazonensis treated with the EC50 of tolnaftate displayed morphological and physiological changes in the mitochondria and cell membrane. Additionally, promastigote forms treated with tolnaftate EC50 reduced the level of ergosterol by 5.6 times in comparison to the control parasites. Altogether, these results suggest that tolnaftate has leishmanicidal activity towards Leishmania sp., is selective, affects the cell membrane and mitochondria of parasites and, moreover, inhibits ergosterol production in L. (L.) amazonensis.
Asunto(s)
Antifúngicos/uso terapéutico , Antiprotozoarios/uso terapéutico , Ergosterol/antagonistas & inhibidores , Leishmania/efectos de los fármacos , Leishmaniasis/tratamiento farmacológico , Tolnaftato/uso terapéutico , Animales , Antifúngicos/farmacología , Antiprotozoarios/farmacología , Supervivencia Celular , Humanos , Ratones , Tolnaftato/farmacologíaRESUMEN
We report and eight years old boy presenting with a pyogenic granuloma of the scalp, generalized alopecia, descamative plates in the neck, trunk and limbs and nail involvement. Cultures for fungus of all these lesions disclosed Microspore canis. The patient was treated with oral griseofulvin, miconazole and topical tolnaftate. Five years later and after several incomplete treatments, the patient returns with a fistulous mass of 12 x 8 cm in the dorsal area whose culture revealed Microspore canis. The mass was excised and oral ketoconazole was indicated. After three months of follow up, the patient was lost from control
Asunto(s)
Humanos , Masculino , Niño , Micetoma/microbiología , Microsporum/patogenicidad , Tolnaftato/uso terapéutico , Gentamicinas/uso terapéutico , Cloxacilina/uso terapéutico , Alopecia/microbiología , Griseofulvina/uso terapéutico , Micetoma/terapia , Miconazol/uso terapéutico , Granuloma Piogénico/cirugíaRESUMEN
Vinte e oito pacientes com diagnóstico clínico e laboratorial de dermatofitose foram aleatoriamente divididos em dois grupos. Um grupo foi tratado com creme de oxiconazol a 1%. O outro grupo foi tratado com creme de tolnaftato. A medicaçäo em ambos os grupos foi aplicada duas vezes ao dia por 40 dias. Em uma segunda fase foram estudados 19 pacientes com diagnóstico clínico e laboratorial de dermatofitose, tratados com uma única aplicaçäo diária de creme de oxiconazol a 1% por 40 dias. O creme de oxiconazol a 1% foi täo eficaz quanto o creme de tolnaftato e causou menor incidência de efeitos colaterais. uma única aplicaçäo diária de creme de oxiconazol a 1% levou à cura micológica em 94,7% dos pacientes após 40 dias
Asunto(s)
Niño , Adolescente , Adulto , Persona de Mediana Edad , Humanos , Masculino , Femenino , Dermatomicosis , Imidazoles/uso terapéutico , Tolnaftato/uso terapéuticoRESUMEN
A 17-year-old boy with chronic papules of the scrotum showed no improvement after topical therapy. A skin biopsy specimen showed Schistosoma mansoni eggs. No evidence of bladder or bowel involvement was found. No treatment is necessary for schistosomal infections without severe symptoms or excessive egg production.