DMNQ S64 exerts antitumor activity on A549 cells via COX-2 inhibition

  • Park, Jeong-Ran (Department of Oncology, Graduate School of East-West Medical Science, Kyunghee University) ;
  • Lim, Eu-Soo (Department of Oncology, Graduate School of East-West Medical Science, Kyunghee University) ;
  • Lee, Seong-Deok (Department of Oncology, Graduate School of East-West Medical Science, Kyunghee University) ;
  • Kim, Sung-Hoon (Department of Oncology, Graduate School of East-West Medical Science, Kyunghee University)
  • Published : 2003.10.01

Abstract

We synthesized naphthazarin derivatives from shikonin, a major compound from Lithospermum erythrorhion Sieb et ZUCC. Of derivatives, DMNQ S64, 2-or 6-(l-hydroxyiminoalkyl) effectively showed antitumor activity on A549, human lung cancer cells (IC$\sub$50/= 30 ${\mu}$M). It significantly inhibited prostaglandin E$_2$(IC$\sub$50/= 10 ${\mu}$M). We also confirmed it selectively downregulated the expression of cyclooxygenase 2(COX-2), while it didn't affect COX-1. The induction of apoptosis by DMNQ S64 is underway.

Keywords