약학회지 (YAKHAK HOEJI)

  • 제47권1호
  • /
  • Pages.46-51
  • /
  • 2003
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  • 0377-9556(pISSN)
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  • 2383-9457(eISSN)
대한약학회 (The Pharmaceutical Society of Korea)
권호 표지

면역결핍바이러스 인테그라제 억제제로서 Baicalein과 Baicalin

Baicalein and Baicalin as Inhibitors of HIV-1 Integrase

  • 이민전 (중앙대학교 산업과학대학 생명공학과) ;
  • 김미라 (중앙대학교 산업과학대학 생명공학과) ;
  • 이용섭 (한국과학기술연구원 생체과학 연구부) ;
  • 신차균 (중앙대학교 산업과학대학 생명공학과)
  • 발행 : 2003.02.01
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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 immunodeficiency 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$\pm$3.3 and 25.9$\pm$4.0$\mu$M, respectively. 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

참고문헌

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