RESUMO
In the present study, nine compounds (1-9) were isolated from Colletotrichum gloeosporioides (an endophytic fungus from Uncaria rhynchophylla) which was cultured in wheat bran medium. Their structures were elucidated as 4-Epi-14-hydroxy-10, 23-dihydro-24, 25-dehydroaflavinine (1), 10, 23-Dihydro-24,25 -dehydro-21-oxoaflavinine (2), Ergosterol (3), Ergosterol peroxide (4), Mellein (5), 4, 5-dihydroblumenol A (6), Colletotrichine A (7), Cyclo(L-leucyl-L-leucyl) (8), and Brevianamide F (9) based on NMR spectral data, as well as comparing with previous literature data. This is the first report about the isolation of compounds 1-2, 6, and 8-9 from Colletotrichum genus. All compounds were tested for their phosphoinositide 3-kinase (PI3Kα) inhibitory activity. Compounds 8 and 9 showed potent PI3K α inhibitory activity with IC50 values of 38.1 and 4.8 µM, respectively, while the other compounds showed very weak activity at a concentration of 20 µg/mL.
Assuntos
Colletotrichum/metabolismo , Inibidores Enzimáticos/química , Interações Hospedeiro-Patógeno , Inibidores de Fosfoinositídeo-3 Quinase , Uncaria/enzimologia , Uncaria/microbiologia , Colletotrichum/química , Endófitos/química , Endófitos/metabolismo , Inibidores Enzimáticos/isolamento & purificação , Concentração Inibidora 50 , Estrutura Molecular , Metabolismo SecundárioRESUMO
One new compound, colletotrichine B (1), was produced by the fungal Colletotrichum gloeosporioides GT-7. The structure of 1 was elucidated on the basis of spectroscopic analysis and X-ray crystallographic analysis. Monoamine oxidase (MAO), acetylcholinesterase (AChE) and phosphoinositide 3-kinase (PI3Kα) inhibitory activity of 1 was also evaluated. Compound 1 showed only AChE inhibiting activity with IC50 value of 38.0 ± 2.67 µg/mL.
Assuntos
Inibidores da Colinesterase/isolamento & purificação , Colletotrichum/química , Endófitos/química , Sesquiterpenos/isolamento & purificação , Uncaria/microbiologia , Inibidores da Colinesterase/química , Concentração Inibidora 50 , Estrutura Molecular , Inibidores da Monoaminoxidase/química , Inibidores da Monoaminoxidase/isolamento & purificação , Inibidores de Fosfoinositídeo-3 QuinaseRESUMO
One new compound, Colletotrichine A (1), was produced by the fungal Colletotrichum gloeosporioides GT-7. The structure was established by 1D and 2D NMR spectra. Monoamine oxidase (MAO) and acetylcholinesterase (AChE) inhibitory activity of 1 was also evaluated. Compound 1 showed AChE-inhibiting activity with IC50 value of 28 µg/mL.
Assuntos
Inibidores da Colinesterase/química , Colletotrichum/química , Inibidores da Monoaminoxidase/química , Sesquiterpenos/química , Uncaria/microbiologia , Inibidores da Colinesterase/farmacologia , Endófitos/química , Concentração Inibidora 50 , Inibidores da Monoaminoxidase/farmacologia , Sesquiterpenos/farmacologiaRESUMO
Four novel lactams, colletotrilactam A-D (1-4), along with six known compounds (5-10) were isolated from the culture broth of Colletotrichum gloeosporioides GT-7, a fungal endophyte of Uncaria rhynchophylla. The structures of these compounds were elucidated by comprehensive NMR spectroscopy. Isolates were tested for monoamine oxidase (MAO) inhibitory activity and compound 9 showed potent MAO inhibitory activity with IC50 value of 8.93±0.34µg/mL, when the IC50 value of iproniazid as a standard was 1.80±0.5µg/mL.
