면역결핍바이러스 인테그라제 억제제로서 Baicalein과 Baicalin

Baicalein iud Baicalin as Inhibitors of HIV-1 Integrase

Baicalein and baicalin are flavonoid compounds isolated from medicinal herb Scutellaria baicalensis Georgi (Labiatae) and have been known to possess antiviral activities. In the present study; we investigated the in vitro effects of baicalein and baicalin on the three distinctive enzymatic activities of the human immunodeficlency virus type-1 (HIV-1) integrase - endonucleolytic, integration, and disintegration activities. Both compounds inhibited the three enzymatic activities in a dose-dependent manner The 50% inhibitory concentrations of baicalein and baicalin for endonucleolytic activities of HIV-1 integrase were 4.4 +/- 3.3 and 25.9 +/- 4.0μM, respectivel. In general, baicalein exhibited nearly 6- to 10-fold stronger inhibition than baicalin for the three enzymatic activities. These data demonstrate that baicalein or baicalin can be used as a leading compound to develop anti-AIDS chemotherapeutic agents targeting to the HIV-1 integrase.