Document Detail


Synthesis and structure-activity relationship study of deoxybenzoins on relaxing effects of porcine coronary artery.
MedLine Citation:
PMID:  20799703     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Deoxybenzoins are potent antioxidants and tyrosinase inhibitors with potential to be developed as food preservatives and cosmetic ingredients. To explore the potential in cardiovascular protection, 25 polyphenolic deoxybenzoins were synthesized and evaluated for inhibitory effects on KCl-induced porcine coronary arterial contraction. The results revealed deoxybenzoins are significant inhibitors of KCl-induced arterial contraction. Among those synthesized, two-thirds of the deoxybenzoins exhibited moderate to good efficacy on relaxing contracted artery including 2,4-dihydroxydeoxybenzoin with EC50=3.30 μM (Emax=100%, n=7) and 2,4-dihydroxy-4'-methoxydeoxybenzoin EC50=3.70 μM (Emax=100%, n=5). Deoxybenzoins displayed an endothelium-dependent relaxing manner on the contracted artery; the contractile responses of neither endothelium denuded nor L-NAME deactivated rings were inhibited. The structure-activity relationships of deoxybenzoin on arterial relaxing effects concluded that the 2,4-dihydroxylated deoxybenzoins presented a potential vascular relaxing pharmacophore, with favoring substitution on ring B in the order of H≥p-OMe>p-OH>o-OMe>m,p-diOMe≥m-OMe.
Authors:
Tzy-Ming Lu; Daih-Huang Kuo; Horng-Huey Ko; Lean-Teik Ng
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Publication Detail:
Type:  In Vitro; Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Journal of agricultural and food chemistry     Volume:  58     ISSN:  1520-5118     ISO Abbreviation:  J. Agric. Food Chem.     Publication Date:  2010 Sep 
Date Detail:
Created Date:  2010-09-15     Completed Date:  2011-01-14     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  0374755     Medline TA:  J Agric Food Chem     Country:  United States    
Other Details:
Languages:  eng     Pagination:  10027-32     Citation Subset:  IM    
Affiliation:
Department of Pharmacy, Tajen University, Pingtung 907, Taiwan. cmlu@mail.tajen.edu.tw
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MeSH Terms
Descriptor/Qualifier:
Animals
Benzoin / analogs & derivatives*,  chemical synthesis,  chemistry,  pharmacology
Coronary Vessels / drug effects*,  physiology
Flavonoids / chemical synthesis,  chemistry,  pharmacology
Phenols / chemical synthesis,  chemistry,  pharmacology
Structure-Activity Relationship
Sus scrofa
Vasodilation / drug effects*
Vasodilator Agents / chemical synthesis*,  chemistry,  pharmacology*
Chemical
Reg. No./Substance:
0/Flavonoids; 0/Phenols; 0/Vasodilator Agents; 0/deoxybenzoin; 0/polyphenols; 119-53-9/Benzoin

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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