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Inhibitory Effects of Epigallocatechin-3-Gallate on Microsomal Cyclooxygenase-1 Activity in Platelets
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 inhibi...
Autores principales: | , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
The Korean Society of Applied Pharmacology
2013
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3762306/ https://www.ncbi.nlm.nih.gov/pubmed/24009859 http://dx.doi.org/10.4062/biomolther.2012.075 |
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author | Lee, Dong-Ha Kim, Yun-Jung Kim, Hyun-Hong Cho, Hyun-Jeong Ryu, Jin-Hyeob Rhee, Man Hee Park, Hwa-Jin |
author_facet | Lee, Dong-Ha Kim, Yun-Jung Kim, Hyun-Hong Cho, Hyun-Jeong Ryu, Jin-Hyeob Rhee, Man Hee Park, Hwa-Jin |
author_sort | Lee, Dong-Ha |
collection | PubMed |
description | 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 μM) 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. |
format | Online Article Text |
id | pubmed-3762306 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2013 |
publisher | The Korean Society of Applied Pharmacology |
record_format | MEDLINE/PubMed |
spelling | pubmed-37623062013-09-05 Inhibitory Effects of Epigallocatechin-3-Gallate on Microsomal Cyclooxygenase-1 Activity in Platelets Lee, Dong-Ha Kim, Yun-Jung Kim, Hyun-Hong Cho, Hyun-Jeong Ryu, Jin-Hyeob Rhee, Man Hee Park, Hwa-Jin Biomol Ther (Seoul) Articles 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 μM) 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. The Korean Society of Applied Pharmacology 2013-01 /pmc/articles/PMC3762306/ /pubmed/24009859 http://dx.doi.org/10.4062/biomolther.2012.075 Text en Copyright ©2013, The Korean Society of Applied Pharmacology http://creativecommons.org/licenses/by/3.0/ This is an Open Access article distributed under the terms of the Creative Commons Attribution Non-Commercial License (http://creativecommons.org/licenses/by-nc/3.0/) which permits unrestricted non-commercial use, distribution, and reproduction in any medium, provided the original work is properly cited. |
spellingShingle | Articles Lee, Dong-Ha Kim, Yun-Jung Kim, Hyun-Hong Cho, Hyun-Jeong Ryu, Jin-Hyeob Rhee, Man Hee Park, Hwa-Jin Inhibitory Effects of Epigallocatechin-3-Gallate on Microsomal Cyclooxygenase-1 Activity in Platelets |
title | Inhibitory Effects of Epigallocatechin-3-Gallate on Microsomal Cyclooxygenase-1 Activity in Platelets |
title_full | Inhibitory Effects of Epigallocatechin-3-Gallate on Microsomal Cyclooxygenase-1 Activity in Platelets |
title_fullStr | Inhibitory Effects of Epigallocatechin-3-Gallate on Microsomal Cyclooxygenase-1 Activity in Platelets |
title_full_unstemmed | Inhibitory Effects of Epigallocatechin-3-Gallate on Microsomal Cyclooxygenase-1 Activity in Platelets |
title_short | Inhibitory Effects of Epigallocatechin-3-Gallate on Microsomal Cyclooxygenase-1 Activity in Platelets |
title_sort | inhibitory effects of epigallocatechin-3-gallate on microsomal cyclooxygenase-1 activity in platelets |
topic | Articles |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3762306/ https://www.ncbi.nlm.nih.gov/pubmed/24009859 http://dx.doi.org/10.4062/biomolther.2012.075 |
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