Fungal phenalenones inhibit HIV-1 integrase

Kazuro Shiomi; Ryosuke Matsui; Miki Isozaki; Harumi Chiba; Takahiro Sugai; Yuichi Yamaguchi; Rokuro Masuma; Hiroshi Tomoda; Tomoko Chiba; Hua Yan; Yoshihiro Kitamura; Wataru Sugiura; Satoshi Omura; Haruo Tanaka

doi:10.1038/ja.2005.8

Fungal phenalenones inhibit HIV-1 integrase

J Antibiot (Tokyo). 2005 Jan;58(1):65-8. doi: 10.1038/ja.2005.8.

Authors

Kazuro Shiomi¹, Ryosuke Matsui, Miki Isozaki, Harumi Chiba, Takahiro Sugai, Yuichi Yamaguchi, Rokuro Masuma, Hiroshi Tomoda, Tomoko Chiba, Hua Yan, Yoshihiro Kitamura, Wataru Sugiura, Satoshi Omura, Haruo Tanaka

Affiliation

¹ School of Pharmaceutical Sciences, Kitasato University, Minato-ku, Tokyo 108-8641, Japan.

PMID: 15813183
DOI: 10.1038/ja.2005.8

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).

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Antifungal Agents / chemistry
Antifungal Agents / pharmacology*
Enzyme Inhibitors / chemistry
Enzyme Inhibitors / pharmacology*
HIV Integrase / drug effects*
Ketones / chemistry
Ketones / pharmacology*
Naphthalenes / chemistry
Naphthalenes / pharmacology*
Phenalenes / chemistry*
Phenalenes / pharmacology
Polycyclic Compounds / chemistry
Polycyclic Compounds / pharmacology*
Structure-Activity Relationship

Substances

Antifungal Agents
Enzyme Inhibitors
Ketones
Naphthalenes
Phenalenes
Polycyclic Compounds
atrovenetinone
funalenone
phenalen-1-one
HIV Integrase