Abstract | BACKGROUND: PURPOSE AND METHODS: Danshen extracts and its constituents were tested for sEH inhibition using its physiological substrate, 8,9-EET, based on a LC-MS/MS assay in this study. RESULTS: Among the tested 15 compounds, tanshinone IIA and cryptotanshinone were found to be the potent (Ki = 0.87 μM) and medium (Ki = 6.7 μM) mixed-type inhibitors of sEH, respectively. Salvianolic acid C (Ki = 8.6 μM) was proved to be a moderate noncompetitive sEH inhibitor. In consistent with the inhibition results of the pure compounds, the 75% ethanol extract of Danshen (EE, IC50 = 86.5 μg/ml) which contained more tanshinone IIA and cryptotanshinone exhibited more potent inhibition on sEH than the water extract (WE, IC50 > 200 μg/ml) or 1 M NaHCO3 (BE, IC50 > 200 μg/ml) extract. CONCLUSION: These data indicated that using the ethanol fraction of Danshen and increasing the amounts of tanshinone IIA, cryptotanshinone and salvianolic acid C, especially the contents of tanshinone IIA in Danshen extract or preparations to enhance the inhibitory effects on sEH might be efficient ways to improve its cardiovascular protective and anti-inflammatory effects, and that herbal medicines could be an untapped reservoir for sEH-inhibition agents and developing sEH inhibitors from the cardiovascular protective and anti-inflammatory herbs is a promising approach.
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Authors | Meijuan Xu, Haiping Hao, Lifeng Jiang, Fang Long, Yidan Wei, Hui Ji, Bingting Sun, Ying Peng, Guangji Wang, Wenzheng Ju, Ping Li |
Journal | Phytomedicine : international journal of phytotherapy and phytopharmacology
(Phytomedicine)
Vol. 22
Issue 4
Pg. 444-51
(Apr 15 2015)
ISSN: 1618-095X [Electronic] Germany |
PMID | 25925966
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Copyright | Copyright © 2015 Elsevier GmbH. All rights reserved. |
Chemical References |
- Abietanes
- Alkenes
- Drugs, Chinese Herbal
- Phenanthrenes
- Plant Extracts
- Polyphenols
- tanshinone
- dan-shen root extract
- Ethanol
- cryptotanshinone
- Epoxide Hydrolases
- salvianolic acid C
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Topics |
- Abietanes
(pharmacology)
- Alkenes
(pharmacology)
- Drugs, Chinese Herbal
(pharmacology)
- Epoxide Hydrolases
(antagonists & inhibitors)
- Ethanol
- Humans
- Phenanthrenes
(pharmacology)
- Plant Extracts
(pharmacology)
- Polyphenols
(pharmacology)
- Salvia miltiorrhiza
(chemistry)
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