3D-QSAR analysis of a new type of acetylcholinesterase inhibitors.

Acetylcholinesterase (AChE) inhibitors are an important class of medicinal agents used for the treatment of Alzheimer's disease. A screening model of AChE inhibitor was used to evaluate the inhibition of a series of phenyl pentenone derivatives. The assay result showed that some compounds displayed higher inhibitory effects.

Protections of pinocembrin on brain mitochondria contribute to cognitive improvement in chronic cerebral hypoperfused rats.

To study effects of pinocembrin, a natural compound extracted from propolis, on cognitive ability impaired by chronic cerebral hypoperfusion in rats, and if it did so, to investigate its effects on brain mitochondria. Rat chronic cerebral hypoperfusion was achieved by permanent bilateral common carotid arteries ligation, with regional cerebral blood flow evaluated. Cognitive ability was tested by Morris water maze task.

High-throughput screening for monoamine oxidase-A and monoamine oxidase-B inhibitors using one-step fluorescence assay.

Aim: To develop high-throughput screening (HTS) assays for monoamine oxidase (MAO)-A and MAO-B inhibitors.

Methods: A fluorescence probe based method measuring MAO-A and MAO-B activity was established and optimized, with its sensitivity, stability and specificity evaluated. Reaction conditions including enzyme sources, substrate concentrations, incubation volume and reaction time in 384-well format were optimized to achieve sensitive and low consumptive goal.

Protective effects of hydroxyethylpuerarin on cultured bovine cerebral microvascular endothelial cells damaged by hydrogen peroxide.

Aim: To observe the damages induced by hydrogen peroxide in cultured bovine cerebral microvascular endothelial cells (BCMEC) and evaluate the protective effects of hydroxyethylpuerarin on hydrogen peroxide-injured BCMEC.

Methods: BCMEC were cultured and transferred into modified Eagle medium (MEM). The viability of cells was detected by MTT assay.