Biomolecules & Therapeutics

The Korean Society of Applied Pharmacology (한국응용약물학회)
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Inhibitory Effects of Epigallocatechin-3-Gallate on Microsomal Cyclooxygenase-1 Activity in Platelets

  • Lee, Dong-Ha (Department of Biomedical Laboratory Science, College of Biomedical Science and Engineering and Regional Research Center, Inje University) ;
  • Kim, Yun-Jung (Department of Biomedical Laboratory Science, College of Biomedical Science and Engineering and Regional Research Center, Inje University) ;
  • Kim, Hyun-Hong (Department of Biomedical Laboratory Science, College of Biomedical Science and Engineering and Regional Research Center, Inje University) ;
  • Cho, Hyun-Jeong (Department of Biomedical Laboratory Science, College of Medical Science, Konyang University) ;
  • Ryu, Jin-Hyeob (Department of Biomedical Laboratory Science, College of Biomedical Science and Engineering and Regional Research Center, Inje University) ;
  • Rhee, Man Hee (Laboratory of Veterinary Physiology & Signaling, College of Veterinary Medicine, Kyungpook National University) ;
  • Park, Hwa-Jin (Department of Biomedical Laboratory Science, College of Biomedical Science and Engineering and Regional Research Center, Inje University)
  • Received : 2012.09.21
  • Accepted : 2013.01.09
  • Published : 2013.01.31
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Abstract

In this study, we investigated the effect of (-)-epigallocatechin-3-gallate (EGCG), a major component of green tea catechins from green tea leaves, on activities of cyclooxygenase (COX)-1 and thromboxane synthase (TXAS), thromboxane $A_2$ ($TXA_2$) production associated microsomal enzymes. EGCG inhibited COX-1 activity to 96.9%, and TXAS activity to 20% in platelet microsomal fraction having cytochrome c reductase (an endoplasmic reticulum marker enzyme) activity and expressing COX-1 (70 kDa) and TXAS (58 kDa) proteins. The inhibitory ratio of COX-1 to TXAS by EGCG was 4.8. These results mean that EGCG has a stronger selectivity in COX-1 inhibition than TXAS inhibition. In special, a nonsteroid anti-inflammatory drug aspirin, a COX-1 inhibitor, inhibited COX-1 activity by 11.3% at the same concentration ($50{\mu}M$) as EGCG that inhibited COX-1 activity to 96.9% as compared with that of control. This suggests that EGCG has a stronger effect than that of aspirin on inhibition of COX-1 activity. Accordingly, we demonstrate that EGCG might be used as a crucial tool for a strong negative regulator of COX-1/$TXA_2$ signaling pathway to inhibit thrombotic disease-associated platelet aggregation.

Keywords

References

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