RESUMEN
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.
Asunto(s)
Benzoatos/aislamiento & purificación , Epilobium/microbiología , Alcoholes del Azúcar/aislamiento & purificación , Talaromyces/química , Benzoatos/química , China , Endófitos/química , Estructura Molecular , Alcoholes del Azúcar/químicaRESUMEN
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.
Asunto(s)
Inhibidores Enzimáticos/química , Inhibidores Enzimáticos/farmacología , Compuestos de Espiro/química , Talaromyces/química , Inhibidores de la Colinesterasa/química , Inhibidores de la Colinesterasa/farmacología , Dicroismo Circular , Evaluación Preclínica de Medicamentos , Endófitos/química , Inhibidores Enzimáticos/aislamiento & purificación , Espectroscopía de Resonancia Magnética , Estructura Molecular , Inhibidores de la Monoaminooxidasa/química , Inhibidores de la Monoaminooxidasa/farmacología , Inhibidores de las Quinasa Fosfoinosítidos-3/química , Inhibidores de las Quinasa Fosfoinosítidos-3/farmacología , Compuestos de Espiro/aislamiento & purificación , Compuestos de Espiro/farmacologíaRESUMEN
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.