ABSTRACT
The dual inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) is considered as an important strategy for the treatment of Alzheimer's disease. In this study, we applied the bioguided fractionations of Ocotea daphinifolia ethyl acetate active extract to furnish a fraction with high inhibitory activity for AChE and BuChE (82% and 92%, respectively). High-performance liquid chromatography semipreparative purification of this fraction provided two new natural products: 1-ß-D-galactopyranosyl-glycerol-2,3-heptanedionate, (1) whose complete chemical structural elucidation was made with spectrometric analysis (MS, 1D, and 2D NMR) and its minor derivative 1-ß-D-gulopyranosyl-glycerol-2,3-heptanedionate; (2) which could be characterized by 2D 1 H-13 C heteronuclear single-quantum correlation spectra analysis. Investigation of the intermolecular interactions with cholinesterases was carried out by molecular docking studies, and results suggested that both compounds are capable to interact with the catalytic site of both enzymes. Compounds 1 and 2 interact with residues of catalytic domains and the peripheral anionic binding site of AChE and BuChE. The results are comparable to those achieved with rivastigmine and galantamine. Thus, this study provides evidence for consideration of the glycosylglycerol from O. daphnifolia as new valuable dual cholinesterases inhibitor.
Subject(s)
Alzheimer Disease , Ocotea , Cholinesterase Inhibitors/chemistry , Butyrylcholinesterase/chemistry , Molecular Docking Simulation , Acetylcholinesterase/metabolism , Ocotea/metabolism , Glycerol , Magnetic Resonance SpectroscopyABSTRACT
ABSTRACT: The goal of the present study was to evaluate the germination, initial growth, and in vitro co-cultivation of Comanthera curralensis Moldenke, a "sempre viva" native of the Chapada Diamantina state of Bahia. Full strength (MS) and half-strength MS (MS1/2) growth media supplemented with two different sucrose concentrations (15 and 30g L-1) were tested for germination and initial plant growth. Three different plant densities were tested by in vitro culture (8, 10 and 12 plants per container). MS1/2 medium with 15g L-1 sucrose resulted in a higher percentage of germination and plant growth for the in vitro establishment of C. curralensis. The use of 12 plants per container is indicated for cost reduction in C. curralensis in vitro production.
RESUMO: Este trabalho teve como objetivo avaliar a germinação, o crescimento inicial e o co-cultivo in vitro de Comanthera curralensis Moldenke, uma "sempre viva" nativa da Chapada Diamantina-BA. Para germinação e crescimento inicial, foram testados os meios de cultura MS completo e MS1/2 suplementados com duas concentrações de sacarose (15 e 30gL-1); no cultivo in vitro, foram testadas três quantidades de plantas por recipiente (8,10 e 12). A utilização do meio MS1/2 com 15gL-1 de sacarose proporcionou maiores porcentagem de germinação crescimento das plantas no estabelecimento in vitro de C. curralensis , e o uso de 12 plantas por recipiente é indicado para a redução de custos na produção in vitro da espécie.
ABSTRACT
A conservação in vitro é uma estratégia de conservação ex situ que garante a manutenção da integridade genética e biológica das espécies. O objetivo deste estudo foi avaliar o efeito de agentes osmóticos e temperatura na conservação in vitro de Syngonanthus mucugensis Giul. subsp. mucugensis. Os brotos foram inoculados em meio de cultura MS ½ contendo 7g L-1 de ágar e suplementado com 60g L-1 de sacarose, e com as concentrações de sacarose 15, 30 e 45g L-1 combinados com 0 e 15g L-1 de sorbitol ou manitol. As culturas foram mantidas em duas temperaturas (18 e 25°C). A porcentagem de sobrevivência das plantas foi avaliada mensalmente e ao final de 180 dias foram analisados o comprimento da parte aérea e da raiz, a porcentagem de folhas verdes, a porcentagem de explantes com brotos, o número de brotos por explante e o comprimento dos brotos. Os agentes osmóticos promoveram um decréscimo no crescimento das plantas, no entanto reduziram a sua viabilidade. Os resultados observados nos experimentos mantidos a 18°C foram significativamente superiores aos encontrados a 25°, para todas as variáveis analisadas. A conservação de S. mucugensis subsp. mucugensis pode ser feita à 18°C em meio de cultura MS ½ contendo 15g L-1 de sacarose, por até 180 dias, sem subcultivo.
The in vitro conservation is an ex situ conservation strategy that ensures the maintenance of genetic and biological integrity of species. The present study evaluated the effects of, osmotic agents and different temperature regimes on the in vitro conservation of Syngonanthus mucugensis Giul. subsp. mucugensis. The shoots were inoculated into half salt strength Murashige and Skoog culture medium (MS ½) containing 7g L-1 of agar. The culture medium was supplemented with 60gL-1 sucrose and with the sucrose concentrations 15, 30 and 45g L-1 combined with 0 and 15g L-1 of sorbytol or mannitol. Two different temperatures were used in these experiments (18 and 25°C). The percentage of plant survival was evaluated monthly and at 180 days were analyzed length of shoot and root, the percentage of green leaves, the percentage of explants with shoots and number of shoots per explants and shoot length. The addition of osmotic agents resulted in decreased growth of the plants and therefore reduced their viability. The averages observed in the experiments undertaken at 18°C were significantly superior to those observed at 25°C for all of the variables analyzed. S. mucugensis subsp. mucugensis can be cultured at 18°C in MS½ culture medium containing 15g L-1 of sucrose, for up to 180 days, without subculturing.
