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Baicalein iud Baicalin as Inhibitors of HIV-1 Integrase
YAKHAK HOEJI 2003;47(1):46-51
Published online February 28, 2003
© 2003 The Pharmaceutical Society of Korea.

이민전(Min Jun Lee);김미라(Mi Ra Kim);이용섭(Yong Sup Lee);신차균(Cha Gyun Shin)
Abstract
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.
Keywords : HIV-1;integrase;baicalein;baicalin.


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