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1.
Molecules ; 29(10)2024 May 10.
Artigo em Inglês | MEDLINE | ID: mdl-38792102

RESUMO

This study investigates the chemical composition of the essential oil obtained from the leaves of Bocageopsis multiflora (Mart.) R.E.Fr (Annonaceae), examining its effectiveness in combating both the larvae and adult forms of Aedes aegypti mosquitoes. Additionally, for a deeper understanding of the insecticidal activity, toxicity properties and molecular docking calculations were conducted using the main compounds of this essential oil. GC/MS analysis revealed the presence of 26 constituents, representing 95.2% of the essential oil, with the major components identified as the sesquiterpenes α-selinene, ß-selinene, and ß-elemene. Larvicidal assays demonstrated potent activity of this essential oil with significant LC50 values of 40.8 and 39.4 µg/mL at 24 and 48 h, respectively. Adulticidal assessments highlighted strong efficacy with LC50 of 12.5 µg/mL. Molecular docking analysis identified optimal interaction activities of α-selinene and ß-selinene with key Aedes proteins. The in silico studies comparing synthetic insecticides with the major sesquiterpenes of the essential oil revealed that ß-selinene exhibited a significantly higher binding affinity compared to the other two sesquiterpenes. Also, ADMET studies of the three main sesquiterpenes indicated acceptable drug-like properties. In these findings, safety evaluations showed low toxicity and skin sensitization for the main sesquiterpenes, contrasting with commercial synthetic insecticides. Therefore, in silico analyses suggest promising interactions with Aedes proteins, indicating its potential as an effective alternative to conventional insecticides These results show the larvicidal and adulticidal potential of the essential oil from Bocageopsis multiflora against Aedes aegypti, supported by its predominant constituents, α-selinene, ß-selinene and ß-elemene.


Assuntos
Aedes , Inseticidas , Larva , Simulação de Acoplamento Molecular , Óleos Voláteis , Animais , Aedes/efeitos dos fármacos , Óleos Voláteis/farmacologia , Óleos Voláteis/química , Inseticidas/química , Inseticidas/farmacologia , Larva/efeitos dos fármacos , Folhas de Planta/química , Sesquiterpenos/farmacologia , Sesquiterpenos/química , Cromatografia Gasosa-Espectrometria de Massas
2.
Mem. Inst. Oswaldo Cruz ; 117: e220089, 2022. tab, graf
Artigo em Inglês | LILACS-Express | LILACS | ID: biblio-1406000

RESUMO

BACKGROUND Black fungi of the Herpotrichiellaceae family are agents of chromoblastomycosis and phaeohyphomycosis. There are few therapeutic options for these infections and it is common to associate antifungal drugs in their treatment. OBJECTIVES To investigate the Medicines for Malaria Venture (MMV) Pathogen Box® for possible compounds presenting synergism with antifungal drugs used to treat black fungal infections. METHODS An initial screening of the Pathogen Box® compounds was performed in combination with itraconazole or terbinafine at sub-inhibitory concentrations against Fonsecaea pedrosoi. Hits were further tested against eight Herpotrichiellaceae using the checkerboard method. FINDINGS No synergism was observed with terbinafine. MMV687273 (SQ109) and MMV688415 showed synergism with itraconazole against F. pedrosoi. Synergism of these compounds was confirmed with some black fungi by the checkerboard method. SQ109 and itraconazole presented synergism for Exophiala dermatitidis, F. pedrosoi, F. monophora and F. nubica, with fungicidal activity for F. pedrosoi and F. monophora. MMV688415 presented synergism with itraconazole only for F. pedrosoi, with fungicidal activity. The synergic compounds had high selectivity index values when combined with itraconazole. MAIN CONCLUSIONS These compounds in combination, particularly SQ109, are promising candidates to treat Fonsecaea spp. and E. dermatitidis infections, which account for most cases of chromoblastomycosis and phaeohyphomycosis.

3.
Molecules ; 24(14)2019 Jul 10.
Artigo em Inglês | MEDLINE | ID: mdl-31295880

RESUMO

The difficulties encountered and the numerous side effects present in the treatment of cutaneous leishmaniasis have encouraged the research for new compounds that can complement or replace existing treatment. The growing scientific interest in the study of plants, which are already used in folk remedies, has led our group to test Endlicheria bracteolata essential oil against Leishmania amazonensis. Several species of the Lauraceae family, or their compounds, have relevant antiprotozoal activities Therefore, the biological potential on L. amazonensis forms from the essential oil of Endlicheria bracteolata leaves was verified for the first time in that work. The antileishmanial activity was evaluated against promastigotes and intracellular amastigotes, and cytotoxicity were performed with J774.G8, which were incubated with different concentrations of E. bracteolata essential oil. Transmission electron microscopy and flow cytometry were performed with E. bracteolata essential oil IC50. Promastigote forms showed E. bracteolata essential oil IC50 of 7.945 ± 1.285 µg/mL (24 h) and 6.186 ± 1.226 µg/mL (48 h), while for intracellular amastigote forms it was 3.546 ± 1.184 µg/mL (24 h). The CC50 was 15.14 ± 0.090 µg/mL showing that E. bracteolata essential oil is less toxic to macrophages than to parasites. Transmission electron microscopy showed that E. bracteolata essential oil treatment is capable of inducing mitochondrial damage to promastigote and intracellular amastigote forms, while flow cytometry showed ΔÑ°m disruption in treated parasites. These results could bring about new possibilities to develop products based on E. bracteolata essential oil to treat cutaneous leishmaniasis, especially for people who cannot receive the conventional therapy.


Assuntos
Antiprotozoários/farmacologia , Leishmania mexicana/química , Leishmania/efeitos dos fármacos , Óleos Voláteis/farmacologia , Animais , Antiprotozoários/química , Cromatografia Gasosa-Espectrometria de Massas , Macrófagos/efeitos dos fármacos , Macrófagos/parasitologia , Macrófagos/patologia , Macrófagos/ultraestrutura , Camundongos , Óleos Voláteis/química , Testes de Sensibilidade Parasitária
4.
PLoS One ; 12(10): e0187380, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-29088304

RESUMO

Copaifera oleoresin is one of the most used natural products in popular medicine all over the world. Among other effects (i.e., anti-inflammatory, antinociceptive, microbicidal) one of the most well-known is its wound healing capacity. However, the mechanism by which the oleoresin presents its effect is still not clear. In this study, our aim was to evaluate the wound healing capacity of oleoresin obtained from Copaifera paupera, its mechanism of action and identify its major components. For these purposes, diabetic Swiss Webster mice were topically treated with oleoresin (100, 150 or 200 mg/kg) for 14 consecutive days after an excision was performed in the back of the mice. Cytokines, wound retraction and histological evaluation were conducted at 3, 7 and 10 days (for cytokines); 0, 3, 7, 10 and 14 days (for wound retraction); and 7 and 14 days (for histological evaluation). Our data indicate that oleoresin significantly reduced production of MCP-1 and TNF-α at days 7 and 10 post-excision and increased IL-10 production at both days. All treatments demonstrated an effect similar or higher to that in collagenase-treated mice. Histological evaluations demonstrated that higher dose treatment resulted in better resolution and closure of the wound and higher levels of collagen deposition and indexes of re-epithelialization even when compared with the collagenase-treated group. The treatment with oleoresin from Copaifera paupera demonstrated that it is even better than an ointment routinely used for improvement of wound healing, suggesting this oleoresin as an option for use in diabetic patients.


Assuntos
Fabaceae/química , Extratos Vegetais/farmacologia , Cicatrização/efeitos dos fármacos , Animais , Quimiocina CCL2/metabolismo , Cromatografia Gasosa-Espectrometria de Massas , Masculino , Camundongos , Fator de Necrose Tumoral alfa/metabolismo
5.
CoDAS ; 27(6): 541-549, nov.-dez. 2015. tab, graf
Artigo em Inglês | LILACS | ID: lil-770524

RESUMO

RESUMO Objetivos: Verificar se há concordância entre fonoaudiólogos e nutricionistas na classificação de consistências alimentares utilizadas em hospitais e as opiniões sobre as possíveis consequências das divergências nessa classificação. Métodos: Estudo descritivo transversal com 30 fonoaudiólogos e 30 nutricionistas que trabalhavam em 14 hospitais da rede pública e/ou privada de Belo Horizonte. Os profissionais responderam um questionário elaborado pelas pesquisadoras e classificaram cinco alimentos, com e sem direcionamento teórico. Empregaram-se os testes estatísticos Exato de Fisher e Z para comparação de proporções, com nível de significância de 5%. Resultados: Tanto fonoaudiólogos (100%) quanto nutricionistas (90%) percebem divergência nas classificações, sendo que, respectivamente, 86,2% e 100% acreditam que essa divergência pode prejudicar a recuperação dos pacientes. O risco de aspiração de alimento foi o prejuízo mais citado. Para a classificação geral das consistências alimentares, a maior parte dos profissionais (88,5%) sugeriu de quatro a seis termos. Quanto à terminologia utilizada na classificação dos alimentos apresentados sem direcionamento teórico, os profissionais citaram 49 termos e concordaram apenas na classificação do sólido e do líquido. Com o direcionamento teórico, os profissionais concordaram também na classificação do pastoso grosso e do pastoso fino. Conclusão: Tanto fonoaudiólogos quanto nutricionistas reconhecem divergências na classificação das consistências alimentares e o consequente risco de prejuízos à recuperação do paciente. A utilização do direcionamento teórico aumentou a concordância entre os profissionais.


ABSTRACT Purpose To verify if there is an agreement between speech-language pathologists and nutritionists about the classification of food textures used in hospitals and their opinions about the possible consequences of differences in this classification. Methods This is a descriptive, cross-sectional study with 30 speech-language pathologists and 30 nutritionists who worked in 14 hospitals of public and/or private network in Belo Horizonte, Brazil. The professionals answered a questionnaire, prepared by the researchers, and classified five different foods, with and without theoretical direction. The data were analyzed using Fisher's exact and Z -tests to compare ratios with a 5% significance level. Results Both speech-language therapists (100%) and nutritionists (90%) perceive divergence in the classification and, 86.2% and 100% of them, respectively, believe that this difference may affect the patients' recovery. Aspiration risk was the most mentioned problem. For the general classification of food textures, most of the professionals (88.5%) suggested four to six terms. As to the terminology used in the classification of food presented without theoretical direction, the professionals cited 49 terms and agreed only in the solid and liquid classifications. With theoretical direction, the professionals also agreed in the classification of thick and thin paste. Conclusion Both the professionals recognized divergences in the classification of food textures and the consequent risk of damage to patient's recovery. The use of theoretical direction increased the agreement between these professionals.


Assuntos
Humanos , Serviço Hospitalar de Nutrição , Alimentos/classificação , Ciências da Nutrição/normas , Patologia da Fala e Linguagem/normas , Terminologia como Assunto , Brasil , Estudos Transversais , Transtornos de Deglutição/dietoterapia , Dieta/normas , Nutricionistas , Fatores de Risco , Inquéritos e Questionários
6.
Rev Bras Parasitol Vet ; 24(1): 36-44, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-25909251

RESUMO

Essential oil of Cymbopogon citratus collected from Brazil and Cuba was tested to a chemical characterization and then was tested on the post-embryonic development of Musca domestica. The chemical composition analysis by GC-MS of the oils from Brazil/Cuba allowed the identification of 13 and 12 major constituents respectively; nine of them common to both. In the both oils, the main components were the isomers geranial and neral, which together form the compound citral. This corresponds to a total of 97.92%/Brazil and 97.69%/Cuba of the compounds identified. The monoterpene myrcene, observed only in the sample of Cuba, presented a large relative abundance (6.52%). The essential oil of C. citratus (Brazil/Cuba) was dissolved in DMSO and tested at concentrations of 5, 10, 25, 50, 75 and 100% and citral was prepared by mixing 16.8 mg with 960 µL DMSO. Both essential oils and monoterpene citral were applied topically to newly-hatched larvae (1µL/larva). The results showed a lethal concentration (LC50) of 4.25 and 3.24% for the Brazilian and Cuban essential oils, respectively. Mortalities of larval and newly-hatched larvae to adult periods were dose-dependent for the two both oils as for monoterpene citral, reaching 90%. Both essential oils and citral caused morphological changes in adult specimens.


Assuntos
Cymbopogon , Moscas Domésticas/efeitos dos fármacos , Inseticidas , Óleos Voláteis/química , Óleos Voláteis/farmacologia , Animais , Brasil , Cuba
7.
Rev. bras. parasitol. vet ; 24(1): 36-44, Jan-Mar/2015. tab, graf
Artigo em Inglês | LILACS | ID: lil-744658

RESUMO

Essential oil of Cymbopogon citratus collected from Brazil and Cuba was tested to a chemical characterization and then was tested on the post-embryonic development of Musca domestica. The chemical composition analysis by GC-MS of the oils from Brazil/Cuba allowed the identification of 13 and 12 major constituents respectively; nine of them common to both. In the both oils, the main components were the isomers geranial and neral, which together form the compound citral. This corresponds to a total of 97.92%/Brazil and 97.69%/Cuba of the compounds identified. The monoterpene myrcene, observed only in the sample of Cuba, presented a large relative abundance (6.52%). The essential oil of C. citratus (Brazil/Cuba) was dissolved in DMSO and tested at concentrations of 5, 10, 25, 50, 75 and 100% and citral was prepared by mixing 16.8 mg with 960 µL DMSO. Both essential oils and monoterpene citral were applied topically to newly-hatched larvae (1µL/larva). The results showed a lethal concentration (LC50) of 4.25 and 3.24% for the Brazilian and Cuban essential oils, respectively. Mortalities of larval and newly-hatched larvae to adult periods were dose-dependent for the two both oils as for monoterpene citral, reaching 90%. Both essential oils and citral caused morphological changes in adult specimens.


O óleo essencial de Cymbopogon citratus, coletado no Brasil e em Cuba, foi caracterizado quimicamente e testado no desenvolvimento pós-embrionário de Musca domestica. A análise da composição química dos óleos essenciais (Brasil/Cuba), por Cromatografia Gasosa acoplada ao espectrômetro de massa (GC-EM), permitiu a identificação de 13 e 12 componentes principais, respectivamente; nove deles comuns aos dois. Em ambos os óleos, os principais componentes foram os isômeros geranial e neral, que, juntos, formam o composto citral. Esse corresponde a um total de 97,92%/Brasil e 97,69%/Cuba dos compostos identificados. O monoterpeno mirceno, observado na amostra cubana, apresentou grande abundância relativa (6,52%). O óleo de C. citratus (Brasil/Cuba) foi dissolvido em DMSO, obtendo–se as concentrações de 5, 10, 25, 75 e 100%; e o citral (16,8 mg) foi misturando com 960mL de DMSO. Tanto o óleo essencial como o monoterpeno citral foram aplicados topicamente nas neolarvas (1µL/larva). Os resultados mostraram uma concentração letal (CL50) de 4,25% e 3,24% para o óleo essencial brasileiro e cubano, respectivamente. As mortalidades do período larval e o de neo-larva a adulto foram dose-dependentes, tanto para os óleos como para o monoterpeno citral, podendo chegar a 90%. Ambos os óleos essenciais e citral causaram alterações morfológicas nos espécimes adultos.


Assuntos
Animais , Óleos Voláteis/farmacologia , Óleos Voláteis/química , Cymbopogon , Moscas Domésticas/efeitos dos fármacos , Inseticidas , Brasil , Cuba
8.
Exp Parasitol ; 148: 66-72, 2015 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-25448354

RESUMO

Current treatments for leishmaniasis present some difficulties due to their toxicity, the use of the intravenous route for administration and therapy duration, which may lead to treatment discontinuation. The aim of this study is to investigate new treatment alternatives to improve patients well being. Therefore, we evaluated the inhibitory effect of (-)α-bisabolol, a sesquiterpene alcohol found in various essential oils of different plant species, against the promastigotes and intracellular amastigotes forms of Leishmania amazonensis, as well as the cytotoxic, morphological and ultrastructural alterations of treated cells. Promastigotes forms of L. amazonensis were incubated with (-)α-bisabolol to determine the antileishmanial activity of this compound. The cytotoxicity effect was evaluated by testing against J774.G8 cells. After these tests, the infected and uninfected cells with L. amazonensis were used to determine if the (-)α-bisabolol was able to kill intracellular parasites and to cause some morphological changes in the cells. The (-)α-bisabolol compound showed significant antileishmanial activity against promastigotes with a 50% effective concentration of 8.07 µg/ml (24 h) and 4.26 µg/ml (48 h). Against intracellular amastigotes the IC50 (inhibitory concentration) of (-)α-bisabolol (24 h) was 4.15 µg/ml. The (-)α-bisabolol also showed a cytotoxic effect against the macrophage strain J774.G8. The value of 50% cytotoxic concentration was 14.82 µg/ml showing that (-)α-bisabolol is less toxic to macrophages than to the parasite. Ultrastructural studies of treated promastigotes and amastigotes showed several alterations, such as loss of cytoplasmic organelles, including the nucleus, and the presence of lipid inclusions. This study showed that (-)α-bisabolol has promising antileishmanial properties, as it can act against the promastigote forms and is able to penetrate the cell, and is also active against the amastigote forms. About 69% of the promastigotes forms suffered mitochondrial membrane damage after treatment with IC50 of (-)α-bisabolol, suggesting inhibition of the metabolic activity of parasites. These results open new prospects for research that can contribute to the development of products based on essential oils or isolated compounds from plants for the treatment of cutaneous leishmaniasis.


Assuntos
Antiprotozoários/farmacologia , Leishmania mexicana/efeitos dos fármacos , Sesquiterpenos/farmacologia , Animais , Antiprotozoários/toxicidade , Linhagem Celular , Citometria de Fluxo , Humanos , Concentração Inibidora 50 , Leishmania mexicana/crescimento & desenvolvimento , Leishmania mexicana/ultraestrutura , Macrófagos/efeitos dos fármacos , Camundongos , Camundongos Endogâmicos BALB C , Microscopia Eletrônica de Transmissão , Sesquiterpenos Monocíclicos , Sesquiterpenos/toxicidade
9.
Acta amaz ; 37(1): 119-122, 2007. ilus, tab
Artigo em Inglês | LILACS | ID: lil-459259

RESUMO

The main iridoids from the bark and latex of Himatanthus sucuuba were isolated and characterised by spectroscopic methods. HPLC was used for the quantitative analyses of these iridoids and the chromatograms of bark and latex showed a similar iridoid composition. Both parts of the plant are used in folk medicine for the treatment of various ailments.


Os iridóides principais das cascas e látex de Himatanthus sucuuba foram isolados e caracterizados por métodos espectroscópicos. CLAE foi utilizada para a análise quantitativa desses iridóides e os cromatogramas da casca e do látex apresentaram uma composição semelhante de iridóides. Ambas as partes da planta são utilizadas na medicina popular para o tratamento de várias doenças.


Assuntos
Cromatografia Líquida de Alta Pressão , Apocynaceae , Iridoides , Estudos de Avaliação como Assunto
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