title: Inhibition of HIV-1 entry by the tricyclic coumarin GUT-70 through the modification of membrane fluidity.
abstract: 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 NF-κB, 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.
authors.affiliation: Division of Hematopoiesis, Center for AIDS Research, Kumamoto University, 2-2-1 Honjo, Chuo-ku, Kumamoto 860-0811, Japan.
authors.forename: Kouki
authors.initials: K
authors.lastname: Matsuda
authors.affiliation: Division of Hematopoiesis, Center for AIDS Research, Kumamoto University, 2-2-1 Honjo, Chuo-ku, Kumamoto 860-0811, Japan.
authors.forename: Shinichiro
authors.initials: S
authors.lastname: Hattori
authors.affiliation: Division of Hematopoiesis, Center for AIDS Research, Kumamoto University, 2-2-1 Honjo, Chuo-ku, Kumamoto 860-0811, Japan.
authors.forename: Ryusho
authors.initials: R
authors.lastname: Kariya
authors.affiliation: Division of Applied Life Science, Graduate School of Engineering, Sojo University, 4-22-1 Ikeda, Nishi-ku, Kumamoto 860-0082, Japan.
authors.forename: Yuji
authors.initials: Y
authors.lastname: Komizu
authors.affiliation: Division of Hematopoiesis, Center for AIDS Research, Kumamoto University, 2-2-1 Honjo, Chuo-ku, Kumamoto 860-0811, Japan.
authors.forename: Eriko
authors.initials: E
authors.lastname: Kudo
authors.affiliation: Division of Hematopoiesis, Center for AIDS Research, Kumamoto University, 2-2-1 Honjo, Chuo-ku, Kumamoto 860-0811, Japan.
authors.forename: Hiroki
authors.initials: H
authors.lastname: Goto
authors.affiliation: Division of Hematopoiesis, Center for AIDS Research, Kumamoto University, 2-2-1 Honjo, Chuo-ku, Kumamoto 860-0811, Japan.
authors.forename: Manabu
authors.initials: M
authors.lastname: Taura
authors.affiliation: Division of Applied Life Science, Graduate School of Engineering, Sojo University, 4-22-1 Ikeda, Nishi-ku, Kumamoto 860-0082, Japan.
authors.forename: Ryuichi
authors.initials: R
authors.lastname: Ueoka
authors.affiliation: Division of Hematology, Respiratory Medicine and Oncology, Department of Internal Medicine, Faculty of Medicine, Saga University, 5-1-1 Nabeshima, Saga 849-8501, Japan.
authors.forename: Shinya
authors.initials: S
authors.lastname: Kimura
authors.affiliation: Division of Hematopoiesis, Center for AIDS Research, Kumamoto University, 2-2-1 Honjo, Chuo-ku, Kumamoto 860-0811, Japan. Electronic address: okadas@kumamoto-u.ac.jp.
authors.forename: Seiji
authors.initials: S
authors.lastname: Okada
mesh_terms: D019380:Anti-HIV Agents / Q000494:pharmacology*; D015704:CD4 Antigens / Q000235:genetics; D002460:Cell Line; D003374:Coumarins / Q000494:pharmacology*; D015536:Down-Regulation / Q000187:drug effects; D015497:HIV-1 / Q000187:drug effects* / Q000502:physiology*; D054884:Host-Pathogen Interactions; D006801:Humans; D019169:Jurkat Cells; D008560:Membrane Fluidity / Q000187:drug effects; D019713:Receptors, CCR5 / Q000235:genetics; D019718:Receptors, CXCR4 / Q000235:genetics; D013601:T-Lymphocytes / Q000187:drug effects / Q000502:physiology / Q000821:virology; D053586:Virus Internalization / Q000187:drug effects*; D014779:Virus Replication / Q000187:drug effects
chemical_list: D019380:Anti-HIV Agents; C584933:CCR5 protein, human; D015704:CD4 Antigens; C527276:CXCR4 protein, human; D003374:Coumarins; C493688:GUT-70; D019713:Receptors, CCR5; D019718:Receptors, CXCR4
keywords: Cell fusion; GUT-70; HIV-1 infection; Membrane fluidity; Viral entry