RESUMEN
The use of natural products in therapeutics has been growing over the years. Lignans are compounds with large pharmaceutical use, which has aroused interest in the search for new drugs to treat diseases. The present study evaluated the cytotoxicity of (-)-trachelogenin, a dibenzylbutyrolactone type lignan isolated from Combretum fruticosum, against several tumor and non-tumor cell lines using the MTT assay and its possible mechanism of action. (-)-Trachelogenin showed IC50 values ranging of 0.8-32.4µM in SF-295 and HL-60 cell lines, respectively and IC50 values >64µM in non-tumor cell lines. (-)-trachelogenin persistently induced autophagic cell death, with cytoplasmic vacuolization and formation of autophagosomes mediated by increasing LC3 activation and altering the expression levels of Beclin-1.
Asunto(s)
4-Butirolactona/análogos & derivados , Antineoplásicos Fitogénicos/farmacología , Autofagia/efectos de los fármacos , Neoplasias del Colon/tratamiento farmacológico , Combretum/química , Descubrimiento de Drogas , Tallos de la Planta/química , 4-Butirolactona/efectos adversos , 4-Butirolactona/química , 4-Butirolactona/aislamiento & purificación , 4-Butirolactona/farmacología , Antineoplásicos Fitogénicos/efectos adversos , Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/aislamiento & purificación , Autofagosomas/efectos de los fármacos , Autofagosomas/patología , Beclina-1/agonistas , Beclina-1/metabolismo , Brasil , Línea Celular , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , Neoplasias del Colon/patología , Combretum/crecimiento & desarrollo , Etnofarmacología , Células HCT116 , Humanos , Concentración 50 Inhibidora , Medicina Tradicional , Proteínas Asociadas a Microtúbulos/agonistas , Proteínas Asociadas a Microtúbulos/metabolismo , Estructura Molecular , Proteínas de Neoplasias/agonistas , Proteínas de Neoplasias/metabolismo , Tallos de la Planta/crecimiento & desarrollo , Vacuolas/efectos de los fármacos , Vacuolas/patologíaRESUMEN
O objetivo deste trabalho foi avaliar a correlação entre o conteúdo de fenóis de extratos de 18 plantas medicinais comuns nas Farmácias Vivas com a atividade sequestradora do radical livre DPPH e com a inibição da enzima acetilcolinesterase. Maiores conteúdos de fenóis totais foram encontrados nas plantas: Eugenia uniflora, Lippia alba, Lippia microphylla, Mentha x villosa, Ocimum gratissimum e Ocimum selloi. As espécies que apresentaram maior atividade antioxidante, semelhante a quercetina, foram: Spondias mombim, Malphigia glabra, L. alba e Croton zenhtneri,. As plantas Cecropia pachystachia, L. alba, L. microphylla, M. glabra, O. gratissimum e Plectranthus ornatus mostraram maiores halos de inibição da enzima acetilcolinesterase. Combinando as duas ações, as plantas mais ativas foram a M. glabra e a L. alba e somente a segunda correlaciona-se diretamente com o maior teor de fenóis totais. Através deste estudo, M. glabra e L. alba foram consideradas as plantas mais promissoras para estudos subsequentes a fim de encontrar novos compostos com ação potencial contra a doença de Alzheimer.
The purpose of this study was to evaluate the phenolic content of 18 medicinal plant extracts of "Live Pharmacies" and correlate them with their free radical scavenging activity and inhibition of the acetylcholinesterase enzyme. Higher amounts of phenolic compounds were found in the following plants: Eugenia uniflora, Lippia alba, Lippia microphylla, Mentha x villosa, Ocimum gatissimum, and Ocimum selloi. The species that showed higher anti-radical activity were Croton zenhtneri, Lippia alba, Malphigia glabra, and Spondias mombim, similar to quercetin. The plants Cecropia pachystachia, L. alba, L. microplylla, M. glabra, O. gratissimum, and Plectranthus ornatus showed larger inhibition zones of the acetylcholinesterase enzyme. By correlating the two actions L. alba and M. glabra are common as more active to both tests and only L. alba correlates directly with the phenolic content. Through this study, L. alba and M. glabra are considered the most promising plants for further studies to find new compounds with potential action against Alzheimer's disease.