Jincai Wang

The pharmacokinetic properties of drugs are significantly influenced by their interactions with cell membranes. Phosphatidylserine (PS) as one of the crucial membrane phospholipids is present abundantly in biological cells. In this study, a PS‐mimicking phospholipid membrane polymer monolithic column was developed using the synthetic compound 2‐methylacryloxydodecyl phosphatidylserine (MDPS). The physicochemical properties and chromatographic performance of the poly(MDPS‐co‐ethylene dimethacrylate (EDMA)) monolithic column were evaluated through scanning electron microscopy (SEM) and nano‐high‐performance liquid chromatography (HPLC). The retention mechanism was investigated by eluting the acidic, neutral, and basic compounds under the same gradient conditions, and the performance of the poly(MDPS‐co‐EDMA) monolithic column was compared with that of a poly(12‐methacryloyl n‐dodecylphosphocholine (MDPC)‐co‐EDMA) monolithic column. The poly(MDPS‐co‐EDMA) column demonstrated effective separation capabilities for small peptides, protein enzymatic hydrolysis polypeptides, and pharmaceutical compounds. Furthermore, the column was also employed to predict the blood–brain barrier (BBB) permeability of drugs, and the correlation coefficient of 0.73 indicates the promising potential of poly(MDPS‐co‐EDMA) monolithic column for predicting the ability of drugs to cross the BBB.

Background: Although molecularly imprinted polymers (MIPs) have now been widely utilized for the sample pretreatment, chromatography separation and removal of pollutants, conventional MIPs are still lack of satisfactory compatibility with water, thus leading to poor molecular recognition for target analytes in aqueous solutions. This aim of study was to prepare the watercompatible MIPs. Methods: The zwitterionic MMIPs were synthesized on vinyltrimethoxysilane-coated Fe₃O₄ (Fe₃O₄-VTMS) through a surface imprinting process by using levofloxacin (LEV) as a template, [2-(methacryloyloxy) ethyl] dimethyl-(3-sulfopropyl) ammonium hydroxide (SPE) as a functional monomer, N, N-methylene-bis-acrylamide (MBA) as a crosslinker and potassium persulfate as an initiator. Results: The prepared zwitterionic LEV-MMIPs were characterized by Fourier transform infrared spectrometry, X-ray diffraction, vibrating sample magnetometry, scanning electron microscopy and water contact angle test. The characterization results showed that zwitterionic LEV-MMIPs exhibited good magnetic responsiveness and super-hydrophilicity (the contact angle is 0°). The optimum pH for binding LEV was found to be 6.0 and the binding isotherm followed the Langmuir isotherm model of monolayer adsorption. The binding process was very fast and the pseudo-second-order model fitted well with the kinetic data. The adsorption capacity of these zwitterionic MMIPs was 54.30 mg g^-1 with a selectivity factor of 1.6 compared to the magnetic non-imprinted polymers (MNIPs). Their feasibility for removing fluoroquinolones (FQs) from the environmental sample was demonstrated using pearl river water spiked with LEV, gatifloxacin, ciprofloxacin and lomefloxacin. The zwitterionic LEV-MMIPs could be reused at least five times with a removal efficiency of more than 80% for the selected FQs. Conclusion: The prepared zwitterionic LEV-MMIP is a promising sorbent for rapid, selective and efficient removal of fluoroquinolones from aqueous medium.

Strigolactones (SLs) are a novel class of plant hormones with enormous potential for the prevention and treatment of inflammation. To further investigate the anti-inflammatory activities of SLs, a representative SL, GR24, and the reductive products of its D-ring were synthesized and their anti-inflammatory activities were fully evaluated on both in vitro and in vivo models. Among these compounds, the two most active optical isomers (2a and 6a) demonstrated strong inhibitory activity on the release of inflammatory cytokines, including nitric oxide (NO), tumor necrosis factor-alpha (TNF-α), and interleukin-6 (IL-6) by blocking the nuclear factor kappa B (NF-κB) and mitogen-activated protein kinase (MAPK) signaling pathways; they also greatly inhibited the migration of neutrophils and macrophages in fluorescent protein labeled zebrafish larvae. These results identified the promising anti-inflammatory effects of SLs, and suggested that both the absolute configuration of SL and the α,β-unsaturated D-ring structure are essential for the observed anti-inflammatory activity.