RESUMEN
Schistosomiasis is a neglected tropical disease that affects millions of people around the world. Currently, the only drug available for the treatment of this disease is praziquantel, which has low efficacy against immature helminth stages and there are reports of drug resistance. In this study, the chemical composition and the in vitro effect of essential oils (EOs) and major compounds from Lippia gracilis and Lippia alba against schistosomula and adult Schistosoma mansoni worms were evaluated. Adult S. mansoni worms cultured for 8h in the presence of L. gracilis EO (50 and 100 µg/mL) or for 2h with its major compound, carvacrol (100 µg/mL), had a 100% reduction in viability. After interaction with L. alba EO (100µg/mL), there was a reduction of approximately 60% in the viability of adult worms after 24 hours of exposure; citral (50 and 100 µg/mL), its major compound, reduced the viability after 24 hours by more than 75%. Treatment of schistosomula with 100 µg/mL of L. gracilis or L. alba EOs for 6h led to a reduction in parasite viability of 80% and 16% respectively. Both EOs and their major compounds significantly reduced the oviposition of adult worms exposed to a non-lethal concentration (5 µg/mL). In addition, morphological changes such as the destruction of the tegument and disorganization of the reproductive system of male and female worms were visualized. Both EOs showed low cytotoxicity at a concentration of 50 µg/mL. The results encourage further investigation of these plants as a potential source of bioactive compounds against S. mansoni.
Asunto(s)
Lippia , Aceites Volátiles , Animales , Femenino , Humanos , Lippia/química , Masculino , Aceites Volátiles/farmacología , Oviposición , Praziquantel/farmacología , Schistosoma mansoniRESUMEN
Trypanosomiases are diseases caused by parasitic protozoan trypanosomes of the genus Trypanosoma. In humans, this includes Chagas disease and African trypanosomiasis. There are few therapeutic options, and there is low efficacy to clinical treatment. Therefore, the search for new drugs for the trypanosomiasis is urgent. This review describes studies of the trypanocidal properties of essential oils, an important group of natural products widely found in several tropical countries. Seventy-seven plants were selected from literature for the trypanocidal activity of their essential oils. The main chemical constituents and mechanisms of action are also discussed. In vitro and in vivo experimental data show the therapeutic potential of these natural products for the treatment of infections caused by species of Trypanosoma.
Asunto(s)
Enfermedad de Chagas/tratamiento farmacológico , Aceites Volátiles/uso terapéutico , Animales , Humanos , Extractos Vegetales/uso terapéutico , Tripanocidas/uso terapéutico , Trypanosoma brucei brucei/efectos de los fármacos , Trypanosoma brucei brucei/patogenicidad , Trypanosoma cruzi/efectos de los fármacos , Trypanosoma cruzi/patogenicidad , Tripanosomiasis Africana/tratamiento farmacológicoRESUMEN
INTRODUCTION: Carbapenem-resistant Klebsiella pneumoniae infection lacks treatment options and is associated with prolonged hospital stays and high mortality rates. The production of carbapenemases is one of the most important factors responsible for this multi-resistance phenomenon. METHODS: In the present study, we analyzed the presence of genes encoding carbapenemases in K. pneumoniae isolates circulating in one of the public hospitals in the city of Aracaju, Sergipe, Brazil. We also determined the best combination of drugs that display in vitro antimicrobial synergy. First, 147 carbapenem-resistant K. pneumoniae isolates were validated for the presence of blaKPC, bla GES, bla NDM, bla SPM, bla IMP, bla VIM, and bla OXA-48 genes using multiplex polymerase chain reaction. Thereafter, using two isolates (97 and 102), the role of double and triple combinational drug therapy as a treatment option was analyzed. RESULTS: Seventy-four (50.3%) isolates were positive for bla NDM, eight (5.4%) for bla KPC, and one (1.2%) for both bla NDM and bla KPC. In the synergy tests, double combinations were better than triple combinations. Polymyxin B and amikacin for isolate 97 and polymyxin B coupled with meropenem for isolate 102 showed the best response. CONCLUSIONS: Clinicians in normal practice use multiple drugs to treat infections caused by multi-resistant microorganism; however, in most cases, the benefit of the combinations is unknown. In vitro synergistic tests, such as those described herein, are important as they might help select an appropriate multi-drug antibiotic therapy and a correct dosage, ultimately reducing toxicities and the development of antibiotic resistance.
Asunto(s)
Antibacterianos/farmacología , Proteínas Bacterianas/genética , Infecciones por Klebsiella/microbiología , Klebsiella pneumoniae/efectos de los fármacos , beta-Lactamasas/genética , Brasil , ADN Bacteriano , Farmacorresistencia Bacteriana Múltiple/genética , Humanos , Klebsiella pneumoniae/genética , Klebsiella pneumoniae/aislamiento & purificación , Pruebas de Sensibilidad Microbiana , Reacción en Cadena de la Polimerasa , PrevalenciaRESUMEN
Abstract INTRODUCTION: Carbapenem-resistant Klebsiella pneumoniae infection lacks treatment options and is associated with prolonged hospital stays and high mortality rates. The production of carbapenemases is one of the most important factors responsible for this multi-resistance phenomenon. METHODS: In the present study, we analyzed the presence of genes encoding carbapenemases in K. pneumoniae isolates circulating in one of the public hospitals in the city of Aracaju, Sergipe, Brazil. We also determined the best combination of drugs that display in vitro antimicrobial synergy. First, 147 carbapenem-resistant K. pneumoniae isolates were validated for the presence of blaKPC, bla GES, bla NDM, bla SPM, bla IMP, bla VIM, and bla OXA-48 genes using multiplex polymerase chain reaction. Thereafter, using two isolates (97 and 102), the role of double and triple combinational drug therapy as a treatment option was analyzed. RESULTS: Seventy-four (50.3%) isolates were positive for bla NDM, eight (5.4%) for bla KPC, and one (1.2%) for both bla NDM and bla KPC. In the synergy tests, double combinations were better than triple combinations. Polymyxin B and amikacin for isolate 97 and polymyxin B coupled with meropenem for isolate 102 showed the best response. CONCLUSIONS: Clinicians in normal practice use multiple drugs to treat infections caused by multi-resistant microorganism; however, in most cases, the benefit of the combinations is unknown. In vitro synergistic tests, such as those described herein, are important as they might help select an appropriate multi-drug antibiotic therapy and a correct dosage, ultimately reducing toxicities and the development of antibiotic resistance.
Asunto(s)
Humanos , Proteínas Bacterianas/genética , beta-Lactamasas/genética , Infecciones por Klebsiella/microbiología , Klebsiella pneumoniae/efectos de los fármacos , Antibacterianos/farmacología , Brasil , ADN Bacteriano , Pruebas de Sensibilidad Microbiana , Reacción en Cadena de la Polimerasa , Prevalencia , Farmacorresistencia Bacteriana Múltiple/genética , Klebsiella pneumoniae/aislamiento & purificación , Klebsiella pneumoniae/genéticaRESUMEN
Amoebic keratitis and granulomatous amoebic encephalitis are caused by some strains of free-living amoebae of the genus Acanthamoeba. In the case of keratitis, one of the greatest problems is the disease recurrence due to the resistance of parasites, especially the cystic forms, to the drugs that are currently used. Some essential oils of plants have been used as potential active agents against this protist. Thus, the aim of this study was to determine the amebicidal activity of essential oils from plants of the genus Lippia against Acanthamoeba polyphaga trophozoites. To that end, 8 × 10(4) trophozoites were exposed for 24 h to increasing concentrations of essential oils from Lippia sidoides, Lippia gracilis, Lippia alba, and Lippia pedunculosa and to their major compounds rotundifolone, carvone, and carvacrol. Nearly all concentrations of oils and compounds showed amebicidal activity. The IC50 values for L. sidoides, L. gracilis L. alba, and L. pedunculosa were found to be 18.19, 10.08, 31.79, and 71.47 µg/mL, respectively. Rotundifolone, carvacrol, and carvone were determined as the major compounds showing IC50 of 18.98, 24.74, and 43.62 µg/mL, respectively. With the exception of oil from L. alba, the other oils evaluated showed low cytotoxicity in the NCI-H292 cell line. Given these results, the oils investigated here are promising sources of compounds for the development of complementary therapy against amoebic keratitis and granulomatous amoebic encephalitis and can also be incorporated into cleaning solutions to increase their amebicidal efficiency.