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KMID : 0370220030470010046
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Yakhak Hoeji
2003 Volume.47 No. 1 p.46 ~ p.51
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Baicalein iud Baicalin as Inhibitors of HIV-1 Integrase
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이민전 (Min Jun Lee ) 김미라 (Mi Ra Kim ) 이용섭 (Yong Sup Lee ) 신차균 (Cha Gyun Shin )
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Abstract
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Baicalein and baicalin are flavonoid compounds isolated from medicinal herb Scutellaria baicalensis Georgi (Labiatae) and have been known to possess antiviral acti vities. 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.
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