4.6 Article

Inhibition of HIV-1 entry by the tricyclic coumarin GUT-70 through the modification of membrane fluidity

Journal

Publisher

ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bbrc.2014.12.102

Keywords

HIV-1 infection; Viral entry; Cell fusion; Membrane fluidity; GUT-70

Funding

  1. Health and Labour Sciences Research Grant from the Ministry of Health, Labour, and Welfare of Japan [H25-AIDS-I-002]
  2. Global CUE program, Global Education and Research Center Aiming at the Control of AIDS from the Ministry of Education, Science, Sports, and Culture of Japan [25114711]
  3. Graduate School of Medical Sciences, Kumamoto University, Japan
  4. Grants-in-Aid for Scientific Research [25420843] Funding Source: KAKEN

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Membrane fusion between host cells and HIV-1 is the initial step in HIV-1 infection, and plasma membrane fluidity strongly influences infectivity. In the present study, we demonstrated that GUT-70, a natural product derived from Calophyllum brasiliense, stabilized plasma membrane fluidity, inhibited HIV-1 entry, and down-regulated the expression of CD4, CCR5, and CXCR4. Since GUT-70 also had an inhibitory effect on viral replication through the inhibition of NE-kappa B, it is expected to be used as a dual functional and viral mutation resistant reagent. Thus, these unique properties of GUT-70 enable the development of novel therapeutic agents against HIV-1 infection. (C) 2015 Elsevier Inc. All rights reserved.

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