면역결핍바이러스 인테그라제 억제제로서 Baicalein과 Baicalin

• 영문명: Baicalein iud Baicalin as Inhibitors of HIV-1 Integrase
• 발행기관: 대한약학회
• 저자명: 이민전(Min Jun Lee) 김미라(Mi Ra Kim) 이용섭(Yong Sup Lee) 신차균(Cha Gyun Shin)
• 간행물 정보: 『약학회지』제47권 제1호 (2003년), 46~51쪽, 전체 6쪽
• 주제분류: 의약학 > 기타의약학
• 파일형태: PDF
• 발행일자: 2003.02.28

영문 초록

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.

키워드

HIV-1 integrase baicalein baicalin.