title: Fungal phenalenones inhibit HIV-1 integrase.
abstract: A phenalenone compound, atrovenetinone methyl acetal, was isolated from a culture broth of Penicillium sp. FKI-1463 as an HIV-1 integrase inhibitor, and it showed anti-HIV activity in vitro. HIV-1 integrase inhibition and anti-HIV activity of two other natural phenalenones were also studied. Among the tested compounds, funalenone inhibited HIV-1 integrase with an IC50 value of 10 microM and showed the best selectivity (anti-HIV, IC50=1.7 microM; cytotoxicity, IC50=87 microM).
authors.affiliation: School of Pharmaceutical Sciences, Kitasato University, Minato-ku, Tokyo 108-8641, Japan.
authors.forename: Kazuro
authors.initials: K
authors.lastname: Shiomi
authors.forename: Ryosuke
authors.initials: R
authors.lastname: Matsui
authors.forename: Miki
authors.initials: M
authors.lastname: Isozaki
authors.forename: Harumi
authors.initials: H
authors.lastname: Chiba
authors.forename: Takahiro
authors.initials: T
authors.lastname: Sugai
authors.forename: Yuichi
authors.initials: Y
authors.lastname: Yamaguchi
authors.forename: Rokuro
authors.initials: R
authors.lastname: Masuma
authors.forename: Hiroshi
authors.initials: H
authors.lastname: Tomoda
authors.forename: Tomoko
authors.initials: T
authors.lastname: Chiba
authors.forename: Hua
authors.initials: H
authors.lastname: Yan
authors.forename: Yoshihiro
authors.initials: Y
authors.lastname: Kitamura
authors.forename: Wataru
authors.initials: W
authors.lastname: Sugiura
authors.forename: Satoshi
authors.initials: S
authors.lastname: Omura
authors.forename: Haruo
authors.initials: H
authors.lastname: Tanaka
mesh_terms: D000935:Antifungal Agents / Q000737:chemistry / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D019427:HIV Integrase / Q000187:drug effects*; D007659:Ketones / Q000737:chemistry / Q000494:pharmacology*; D009281:Naphthalenes / Q000737:chemistry / Q000494:pharmacology*; D043803:Phenalenes / Q000737:chemistry* / Q000494:pharmacology; D011083:Polycyclic Compounds / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000935:Antifungal Agents; D004791:Enzyme Inhibitors; D007659:Ketones; D009281:Naphthalenes; D043803:Phenalenes; D011083:Polycyclic Compounds; C095644:atrovenetinone; C405054:funalenone; C038036:phenalen-1-one; D019427:HIV Integrase