Design, synthesis and application of AIE fluorescent probe for lipid raft / 中国药科大学学报

@#Lipid rafts composed of saturated phospholipids,sphingomyelin,and cholesterol are usually defined as liquid ordered microdomains located in the cell membrane. Lipid rafts are involved in many physiological and pathological processes of cells. Based on the difference in composition and distribution between lipid raft and non-raft domains,a lipid raft probe with aggregation-induced emission (AIE),cholesterol-triethylene glycol-tetraphenylethylene (TCHS-TPE),was designed and synthesized for convenient and specific imaging of lipid raft domains on cell membranes in this study. In this paper,TCHS-TPE was successfully synthesized,and the photophysical properties of TCHS-TPE were measured to evaluate its AIE characteristics. And finally the specific imaging of TCHS-TPE on the lipid raft region of B16F10 melanoma cell membrane was studied using confocal laser scanning microscopy. Compared with the existing lipid raft probe cholera toxin B (CTxB),the TCHS-TPE lipid raft probe has the advantages of simple operation and high specificity. The successful synthesis of the fluorescent probe will provide a useful tool for studying the physiological and pathological processes related to lipid raft domains,and offer a theoretical basis for the design of imaging probes for other lipid raft domains.

Synthesis and in vitro bioIogicaI activity of 3-phenyI-3-pyrroIyIpentane deriva-tives / 中国药科大学学报

A new series of 3-phenyl-3-pyrrolylpentane derivatives are synthesized through modifying the structure of lead compound LG19055,a nonsecosteroidal vitamin D receptor(VDR)agonist.The VDR-agonistic ability of target compounds was measured indirectly by evaluating the differentiation ability of HL-60 cell.The results showed that compounds 13a,13c,13d,13h,13i,13j have excellent VDR-agonistic ability(EC50 <50 μmol /L), especially for compound 13j (EC50 =0.10 μmol /L),which was more potential than that of lead compound LG190155.Their proliferation inhibitory activities in vitro were evaluated by MTT assay in MCF-7,PC-3,Caco-2, HepG2 and L02 cell lines.Compound 13a exhibited significant inhibitory effects on HepG2 cell line(IC50 =0.11μmol /L).Moreover,the inhibitory effect of compound 13a on non-tumor liver L02 cell line was relatively weak (IC50 =15.24 μmol /L ),suggesting that compound 13a has selective inhibitory effects on liver cancer cells.Additionally,HL-60 cell differentiation-inducing activity and the inhibitory effect of cancer cells were posi-tively related.