Recent advances in screening of enzymes inhibitors based on capillary electrophoresis / 药物分析学报

Capillary electrophoresis with many advantages plays an important role in pharmaceutical analysis and drug screening. This review gives an overview on the recent advances in the developments and applications of capillary electrophoresis in the field of enzyme inhibitor screening. The period covers 2013 to 2017. Both the pre-capillary enzyme assays and in-capillary enzyme assays which include electrophoretically mediated microanalysis (EMMA) and immobilized enzyme microreactor (IMER) are summarized in this article.

Study on preparation of immobilized acetylcholinesterase microreactor and its application in CMM inhibitors screening / 中草药

Objective To prepare an immobilized acetylcholinesterase (AChE) microreactor and establish a rapid screening method for Chinese materia medica (CMM) acetylcholinesterase inhibitors (AChEIs). Methods A novel immobilized AchE microreactor was prepared by crosslinking with glutaraldehyde, using aminated magnetic microspheres as carrier. The characterizations were conducted by physicochemical properties and chromatographic performance. The immobilized AChE reactor was used to screen AChEIs from the Huperzia Serratum extracts. Results In the enzyme reaction system, the optimum substrate concentration was 50 μmol/L, and the incubation time was 5 min, respectively. IR characterization, specificity verification, enzyme kinetics, and stability study results all demonstrated the effectiveness of the enzyme reactor. The CMM AChEI, huperzine A, was obtained from the screening of H. Serratum extracts. Conclusion A high throughput screening method for AChEIs is established in this paper, which will be further applied and popularized.

Manufacture and application of a microfluidic chip-based 18F microreactor / 中华核医学与分子影像杂志

Objective To develop a polydimethylsiloxane (PDMS) microfluidic chip-based 18F microreactor for the preparation of 18F-labeled probes.Methods The 18F microreactor was composed of PDMS microfluidic chip and customized glass microvessel integrating with stainless capillary tube (D 0.6 mm) as heater/cooler.PDMS chips were fabricated by silk-screen printing technology,a traditional and easily accessible process.18F-FDG and 18F-fluoroacetate(FAC) were synthesized using the 18F microreactor.TLC was applied to measure the 18F-labeling yield and the radiochemical purity of 18F-FDG and 18F-FAC.Results The size of PDMS chip was 40.0 mm (l)×30.0 mm (w)×6.0 mm(h) and the liquid/gas inside channel was 0.3 mm (w)×50.0 μm (h).The customized glass microvessel was about 4.0 mm (D) ×30.0 mm (h) with 200 μl of reaction volume.The capillary tube which wrapped around the microvessel functioned as a heater when electric current was provided,while as a cooler when compressed air went through.The integrated 18F microreactor with a total size of 40.0 mm (l) ×30.0 mm (w) ×15.0 mm (h) was successfully used to prepare 18F-FDG and 18F-FAC,whose radiochemical purity were both higher than 96％ and 18F-labeling yield was 92.5％ and 90.0％ respectively in the first fluorination step.Conclusions A PDMS microfluidic chip-based 18F microreactor is developed and successfully applied to prepare 18F-FDG and 18F-FAC.It has the dual advantages of both microfluidc chip and traditional synthesis module and features of high integration,small total size and low consumption of labeling precursor.