RESUMO
A norbisabolane and an arabitol benzoate, Talaromarnine A (1), Talaromarnine B (2), together with eight known compounds were obtained from cultures of Talaromyces marneffei, an endophytic fungus of Epilobium angustifolium. Their structures were elucidated by IR, MS, 1D and 2D NMR spectra, and their absolute configuration was determined by single-crystal X-ray diffraction and molecular computation. These compounds were tested for monoamine oxidase, acetylcholinesterase and PI3K inhibitory activity, but no compounds exhibited significant activities.
Assuntos
Benzoatos/isolamento & purificação , Epilobium/microbiologia , Álcoois Açúcares/isolamento & purificação , Talaromyces/química , Benzoatos/química , China , Endófitos/química , Estrutura Molecular , Álcoois Açúcares/químicaRESUMO
Two new compounds Talaromycin A (1) and Talaromycin B (2) were isolated from a liquid culture of Talaromyces aurantiacus. The structures of 1 and 2 were elucidated by IR, MS, 1D and 2D NMR spectra and comparison of the experimental and calculated electronic circular dichroism spectra. Additional known compounds (3-6) were also isolated. These compounds were tested for monoamine oxidase, acetylcholinesterase and PI3K inhibitory activity, but showed only weak activity.
Assuntos
Inibidores Enzimáticos/química , Inibidores Enzimáticos/farmacologia , Compostos de Espiro/química , Talaromyces/química , Inibidores da Colinesterase/química , Inibidores da Colinesterase/farmacologia , Dicroísmo Circular , Avaliação Pré-Clínica de Medicamentos , Endófitos/química , Inibidores Enzimáticos/isolamento & purificação , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Inibidores da Monoaminoxidase/química , Inibidores da Monoaminoxidase/farmacologia , Inibidores de Fosfoinositídeo-3 Quinase/química , Inibidores de Fosfoinositídeo-3 Quinase/farmacologia , Compostos de Espiro/isolamento & purificação , Compostos de Espiro/farmacologiaRESUMO
It is well known that the isolation of monoamine oxidase (MAO) inhibitors from natural sources is an important strategy for drug development in the treatment of depression, Parkinson's disease and Alzheimer's disease. The present work describes developing a thin-layer chromatography (TLC) bioautographic method for detecting MAO inhibitors from plant extracts. The basic principle of the method is that the enzyme oxidises tryptamine into an aldehyde which in turn reacts with 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyltetrazolium bromide to form a blue formazan which makes a blue-coloured background on the TLC plates. Inhibitors of MAO produced white spots on the background. The new TLC bioautographic method has several advantages such as lower consumption of the enzyme, shorter experimental time, more easily observed background of TLC plate and better reproducibility. The detection limits were 10 ng for several known MAO inhibitors.