Study on preparation of ampelopsin liposomes / 中国中药杂志

<p><b>OBJECTIVE</b>To study the formulation and preparation of ampelopsin liposomes and evaluate their quality.</p><p><b>METHOD</b>The liposomes were prepared by a film-ultrasonic dispersion technique. Served as quota with the entrapment ratio and appearance and diameter of the liposomes, the optimal formulation and preparation were selected by means of an uniform design test. The appearance of liposomes was observed by micrography. The diameter and electric charge of surface were determined by granularity mensuration instrument. The entrapment ratio and the leakage rate of ampelopsin liposome were determined by means of dialyze. The content of ampelopsin was determined by UV.</p><p><b>RESULT</b>The result of electron micrography and the size distribution showed that the liposomes were similar to spherical small unilamellar vesicles. The mean diameter was (258.2 +/- 51.2) nm and the electric charge of surface is 19.0 mV. The entrapment ratio of ampelopsin liposomes was 62. 3% and the lecithoid oxidative rate was 0.83% (n = 3).</p><p><b>CONCLUSION</b>The selected formulation and preparation of ampelopsin liposomes is efficient and practicable.</p>

Ampelopsin, a small molecule inhibitor of HIV-1 infection targeting HIV entry / 生物医学与环境科学（英文）

<p><b>OBJECTIVE</b>To investigate the anti-HIV effects of ampelopsin and its interaction with HIV-1 coreceptor CXCR4.</p><p><b>METHODS</b>Through anti-virus experiments in vitro, the inhibitory effect of ampelopsin on HIV-1 infection was verified. Chemotaxis assay was performed to show the ability to induce PBMCs migration by ampelopsin, RANTES and SDF-1alpha. Fluorescence labelling monoclonal antibody was utilized to observe the interaction of ampelopsin and CXCR4. Mice immunosuppressant model was also established to detail the role ampelopsin played in regulating cellular immunological functions.</p><p><b>RESULTS</b>Ampelopsin could protect sensitive cells against HIV-1 infection and dramatically reduce HIV-1 antigen P24 expression. HIV-1SF33 attaching to MT-4 cells was interfered by ampelopsin, and the EC50 was 0.175 mg/mL for cellular protection and 0.024 mg/mL for P24 inhibition. At co-cultivating phase, EC50 was 0.229 mg/mL and 0.197 mg/mL respectively. Furthermore, the EC50 was 0.179 mg/mL and 0.348 mg/mL in acute infection. Human PBMCs migration was induced after being challenged with ampelopsin or chemokines, and synergistic action was observed during co-treatment. Ampelopsin alone resulted in maximal chemotaxis at 1 mg/mL. HIV-1 co-receptor CXCR4 on the surface of PBMCs was decreased by internalization, which indicated the effect of ampelopsin on CXCR4. About 70% CXCR4 was reduced by ampelopsin at 1 mg/mL. Ampelopsin also augmented cellular immunological functions in immunosuppressive mice.</p><p><b>CONCLUSION</b>Ampelopsin displays a strong inhibitive role during HIV-1 absorption, incubation and acute infection. These results are coincident with its immune enhancement.</p>