Principle and applications of fluorescent probes for intracellular redox detection / 上海交通大学学报（医学版）

Redox state indicated by reactive oxygen species (ROS) level is a cellular physiological feature.Redox status is exactly controlled by conserved system.Its alterations consequently modulate various biological activities and play important roles in cells and organism under physiological and pathological conditions.Hence detection of redox state is deemed as an important technique both in basic and clinical researches.The present article reviews the principle and current applications of fluorescent probes or sensors for redox detection.With comparison of properties of various probes,especially genetic coding fluorescence probes,much understanding will be gained.And the review helps us to understand how to apply the redox probes on the biological and clinical researches and eventually look forward to new applications in the cell and whole animal level.

Design, synthesis and evaluation of new L-proline derivatives as acetylcholinesterase inhibitors / 药学学报

In this paper, fourteen new L-proline derivatives were designed and synthesized, and their acetlcholinesterase (AChE) inhibitory activities were also investigated in vitro. New L-proline derivatives were prepared from substituted 2-bromo-1-acetophenones through four-step reaction; and their bioactivities as AChE inhibitors were measured by Ellman spectrophotometry. The results showed that the target compounds had a certain AChE inhibitory activity to in vitro. The bioactivity of compound 8b was the best of them, and its IC50 value was 5.45 µmol.L-1, which was better than that of rivastigmine. So the acetylcholinesterase inhibitory activities of new L-proline derivatives were worth to be further studied.

Design, synthesis and evaluation of 5-aminobenzimidazolone derivatives as acetylcholinesterase inhibitors / 药学学报

The target compounds were prepared from 5-aminobenzimidazolone by two steps reaction, and their AChE inhibitory activities were measured by Ellman method in vitro. The AChE inhibitory activity of compound 4d is the best of them, and its IC50 value is equal to 7.2 μmol·L(-1), which is better than that of rivastigmine; moreover the 4d had no inhibitory activities to BuChE. Therefore, the inhibitory activities of 5-aminobenzimidazolone derivatives to acetylcholinesterase are worth further researching.