Dihydrotanshinone l is an Inhibitor of Farmesy-Protein Transferase

Farmesy-Protein Transferase의 저해제 Dihydrotanshinone l.

  • 이동선 (경북대학교 미생물학과) ;
  • 이상한 (경북대학교 미생물학과) ;
  • 하상철 (경북대학교 미생물학과) ;
  • 김종국 (경북대학교 미생물학과) ;
  • 서영배 (경북대학교 미생물학과) ;
  • 홍순덕 (경북대학교 미생물학과)
  • Published : 1998.04.01

Abstract

An inhibitor of farnesy-protein transferae is known to be a fgood candidate for antitumor agent that block the oncogenic activity of Ras protein . We recently isolated and characterized dihydrotanshinone I from Salvia miltiorrhiza Bunge (Danshen), an oriental herb, which has an inhibitory activity of toposimerase I to some cancer cell lines. In order to examine the molecular mechanism of dihydrotanshinone I, we studied the farmesy-Protein Transferase activity by dihydrotanshinone I. As a result, we found that result, we found that dihydrotanshinone I showed inhibitory effect on farnesyl-protein transferase with $IC_{50}$ value of 15 ug/ml. This result suggest that dihydrotanshinone I may be an useful anticancer agent with the inhibitory activity of farnesyl-protein transferase.

Farmesy-Protein Transferase의 저해제는 Ras단백질의 발암활성을 차잔하는 항암제의 후보로서 알려져있다. 우리는 최근에 topoisomerase I에 대하여 저해활성을 갖는 dihydrotanshinone I을 약용식물인 Salvia miltorhiza Bunge(Danshen)으로부터 분리하였다. Dihydrotanshinone Iml 작용기작의 해석을 위한 시도에서 farmesy-Protein Transferase에 대한 저해능($IC_{50}$치= 15ug/ml)을 관찰하였으며, 이것은 유용한 항암제로서의 가능성을 제시한 결과로 본다.

Keywords

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