Caracterização química e atividades biológicas dos óleos essenciais de Protium heptaphyllum, Hedyosmum brasiliense, Blepharocalyx salicifolius, Baccharis dracunculifolia e Nectandra megapotamica
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Data
2018-04-13
Autores
Furtado, Fabiana Barcelos
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Editor
Universidade Estadual Paulista (Unesp)
Resumo
Espécies vegetais são fontes de moléculas biologicamente ativas que têm um importante papel no desenvolvimento de novos fármacos e, portanto, suas propriedades merecem ser investigadas. Apesar de serem espécies aromáticas e apresentarem um potencial farmacológico, algumas atividades biológicas dos óleos essenciais das folhas de Protium heptaphyllum, Hedyosmum brasiliense, Blepharocalyx salicifolius, Baccharis dracunculifolia e Nectandra megapotamica ainda não foram avaliadas. O objetivo deste trabalho foi verificar a ação citotóxica, antileishmania e antimicrobiana destes óleos essenciais com o intuito de estabelecer espécies vegetais com potencial uso na elaboração de fármacos ou como terapias complementares aos tratamentos convencionais de doenças de impacto em saúde pública. Os óleos essenciais foram obtidos por destilação de folhas frescas por arraste de vapor, a composição química determinada por análises de cromatografia gasosa/espectrometria de massas, as atividades biológicas testadas utilizando o método de microdiluição e a verificação dos mecanismos de morte celular feita por citometria de fluxo. B. salicifolius e B. dracunculifolia apresentaram elevado rendimento (0,86% e 0,89% respectivamente) quando comparado aos demais óleos essenciais avaliados. H. brasiliense e B. salicifolius apresentaram resultados promissores sobre linhagens tumorais Ehrlich (51,59 e 42,04 μg mL-1) e MDA-MB-231 (62,40 e 46,60 μg mL-1), com maior ação seletiva para estes tipos celulares se comparado a célula normal de mama MCF-10A (>512 e 314,44 μg mL-1). Os resultados de citometria de fluxo mostraram que o óleo de B. salicifolius não atua por indução de morte celular mas sim causando um prejuízo no metabolismo, especificamente em células tumorais. Já o tratamento com o óleo de H. brasiliense induziu morte celular principalmente por necrose em células tumorais de mama, mas não em células normais. Além disto, H. brasiliense, B. salicifolius e N. megapotamica apresentaram ação inibidora sobre Paracoccidioides brasiliensis (234,37; 156,25; 468,75 μg mL-1), mostrando assim potencial no tratamento da paracoccidioidomicose. Contra espécies de Candida, Cryptococcus neoformans, Trichophyton mentagrophytes e Microsporum canis não foram observados resultados relevantes. Os óleos de B. salicifolius e B. dracunculifolia, ainda que tenham apresentado ação sobre Leishmania amazonensis, foram citotóxicos para macrófagos, uma de suas principais células hospedeiras, sendo assim pouco interessante a investigação destes voláteis frente à forma amastigota. Os óleos essenciais avaliados, nas suas presentes constituições químicas, foram ineficazes contra Staphylococcus aureus meticilina resistente e meticilina sensível, Escherichia coli e Pseudomonas aeruginosa. Para Staphylococcus aureus meticilina sensível o óleo essencial de H. brasiliense atuou em sinergismo com as drogas cefalotina e oxacilina, já para E. coli, a droga gentamicina atuou de forma sinérgica com os óleos essenciais de P. heptaphyllum, H. brasiliense, B. salicifolius, e N. megapotamica, levando as drogas a apresentarem seus efeitos bactericidas a ¼ da concentração de suas doses efetivas. Em conclusão, alguns dos resultados aqui destacados, sobretudo para óleos de H. brasiliense e B. salicifolius, sugerem que nestas espécies há a presença de moléculas potencialmente ativas que podem servir como protótipos para o desenvolvimento de novos fármacos.
lant species are sources of biologically active molecules that play an important role in the development of new drugs, and therefore, their properties deserve to be investigated. In this regard, Protium heptaphyllum, Hedyosmum brasiliense, Blepharocalyx salicifolius, Baccharis dracunculifolia and Nectandra megapotamica are aromatic species with pharmacological potential, producing essential oils whose biological activities had not yet been investigated. The aim of this work was to assess any cytotoxic, antileishmania, or antimicrobial action of these essential oils to determine those plant species with potential in the elaboration of drugs or in complementary treatments of diseases with an impact on public health. Essential oils were obtained from fresh leaves by steam distillation. Chemical composition was determined by gas chromatography/mass spectrometry. Biological activities were assessed using the microdilution method while cell death was checked by flow cytometry. B. salicifolius and B. dracunculifolia presented high yields (0.86% and 0.89%, respectively) relative to the other species assessed. H. brasiliense and B. salicifolius showed promising action on Ehrlich (at 51.59 and 42.04 μg mL-1 concentration respectively) and MDA-MB-231 tumor lines (at 62.40 and 46.60 μg mL-1 concentration respectively), with less selective action against normal MCF-10A breast cells (at > 512 and 314.44 μg mL-1 concentration respectively). Flow cytometry results showed that B. salicifolius oil does not induce cell death but rather acts causing metabolic impairment, specifically in tumor cells. Essential oil from H. brasiliense induced cell death in breast tumor cells, mainly due to necrosis, but not in normal cells. In addition, H. brasiliense, B. salicifolius, and N. megapotamica, presented inhibitory action on Paracoccidioides brasiliensis (at 234.37, 156.25, and 468.75 μg mL-1 concentration respectively), thus showing potential in the treatment of paracoccidioidomycosis. Significant action was not observed against Candida species, Cryptococcus neoformans, Trichophyton mentagrophytes and Microsporum canis. The oils of B. salicifolius and B. dracunculifolia did present action against Leishmania amazonensis but were also cytotoxic to macrophages, one of its main host cells, therefore not being of interest against the amastigote form of the parasite. The essential oils studied here were ineffective against Staphylococcus aureus (whether resistant or sensitive to methicillin), Escherichia coli, and Pseudomonas aeruginosa. On methicillin-sensitive Staphylococcus aureus though, the action of H. brasiliense essential oil was synergistic with that of drugs cefalotin and oxacillin. On E. coli, use of the drug gentamicin benefitted from the synergistic action of essential oils from P. heptaphyllum, H. brasiliense, B. salicifolius, and N. megapotamica, which made the drug effective at 1/4 lower doses. In conclusion, some of the results highlighted here, especially for H. brasiliense and B. salicifolius, show that essential oils in these species include active molecules having potential in the development of new drugs.
lant species are sources of biologically active molecules that play an important role in the development of new drugs, and therefore, their properties deserve to be investigated. In this regard, Protium heptaphyllum, Hedyosmum brasiliense, Blepharocalyx salicifolius, Baccharis dracunculifolia and Nectandra megapotamica are aromatic species with pharmacological potential, producing essential oils whose biological activities had not yet been investigated. The aim of this work was to assess any cytotoxic, antileishmania, or antimicrobial action of these essential oils to determine those plant species with potential in the elaboration of drugs or in complementary treatments of diseases with an impact on public health. Essential oils were obtained from fresh leaves by steam distillation. Chemical composition was determined by gas chromatography/mass spectrometry. Biological activities were assessed using the microdilution method while cell death was checked by flow cytometry. B. salicifolius and B. dracunculifolia presented high yields (0.86% and 0.89%, respectively) relative to the other species assessed. H. brasiliense and B. salicifolius showed promising action on Ehrlich (at 51.59 and 42.04 μg mL-1 concentration respectively) and MDA-MB-231 tumor lines (at 62.40 and 46.60 μg mL-1 concentration respectively), with less selective action against normal MCF-10A breast cells (at > 512 and 314.44 μg mL-1 concentration respectively). Flow cytometry results showed that B. salicifolius oil does not induce cell death but rather acts causing metabolic impairment, specifically in tumor cells. Essential oil from H. brasiliense induced cell death in breast tumor cells, mainly due to necrosis, but not in normal cells. In addition, H. brasiliense, B. salicifolius, and N. megapotamica, presented inhibitory action on Paracoccidioides brasiliensis (at 234.37, 156.25, and 468.75 μg mL-1 concentration respectively), thus showing potential in the treatment of paracoccidioidomycosis. Significant action was not observed against Candida species, Cryptococcus neoformans, Trichophyton mentagrophytes and Microsporum canis. The oils of B. salicifolius and B. dracunculifolia did present action against Leishmania amazonensis but were also cytotoxic to macrophages, one of its main host cells, therefore not being of interest against the amastigote form of the parasite. The essential oils studied here were ineffective against Staphylococcus aureus (whether resistant or sensitive to methicillin), Escherichia coli, and Pseudomonas aeruginosa. On methicillin-sensitive Staphylococcus aureus though, the action of H. brasiliense essential oil was synergistic with that of drugs cefalotin and oxacillin. On E. coli, use of the drug gentamicin benefitted from the synergistic action of essential oils from P. heptaphyllum, H. brasiliense, B. salicifolius, and N. megapotamica, which made the drug effective at 1/4 lower doses. In conclusion, some of the results highlighted here, especially for H. brasiliense and B. salicifolius, show that essential oils in these species include active molecules having potential in the development of new drugs.
Descrição
Palavras-chave
Paracoccidioides brasiliensis, MDA-MB-231, Ehrlich, MCF-10A, Óleos essenciais, Tumor de mama, Citometria de fluxo, Essencial oils, Breast tumor, Flow cytometry