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Ampelopsin, a Small Molecule Inhibitor of HIV-1 Infection Targeting HIV Entry 被引量:13
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作者 DE-YULIU JIAN-TAOYE +3 位作者 WEN-HUIYANG JINYAN CHANG-HONGZENG sazeng 《Biomedical and Environmental Sciences》 SCIE CAS CSCD 2004年第2期153-164,共12页
Objective To investigate the anti-HIV effects of ampelopsin and its interaction with HIV-1 coreceptor CXCR4. Methods Through anti-virus experiments in vitro, the inhibitory effect of ampelopsin on HTV-1 infection was ... Objective To investigate the anti-HIV effects of ampelopsin and its interaction with HIV-1 coreceptor CXCR4. Methods Through anti-virus experiments in vitro, the inhibitory effect of ampelopsin on HTV-1 infection was verified. Chemotaxis assay was performed to show the ability to induce PBMCs migration by ampelopsin, RANTES and SDF-la. 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. Results Ampelopsin could protect sensitive cells against HTV-1 infection and dramatically reduce HIV-1 antigen P24 expression. HTV-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. Conclusion Ampelopsin displays a strong inhibitive role during HIV-1 absorption, incubation and acute infection. These results are coincident with its immune enhancement. 展开更多
关键词 AMPELOPSIN HTV-1 Chemokine receptors Cellular immunity
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