Fungal phenalenones inhibit HIV-1 integrase.
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).
Shiomi
Kazuro
K
School of Pharmaceutical Sciences, Kitasato University, Minato-ku, Tokyo 108-8641, Japan.
Matsui
Ryosuke
R
Isozaki
Miki
M
Chiba
Harumi
H
Sugai
Takahiro
T
Yamaguchi
Yuichi
Y
Masuma
Rokuro
R
Tomoda
Hiroshi
H
Chiba
Tomoko
T
Yan
Hua
H
Kitamura
Yoshihiro
Y
Sugiura
Wataru
W
Omura
Satoshi
S
Tanaka
Haruo
H
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
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