Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 20, Issue 16, Pages 4855-4857Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.06.095
Keywords
Morroniside; 7-O-Cinnamoylmorroniside; Anti-inflammatory activity
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Funding
- Grants-in-Aid for Scientific Research [21659436, 22390354] Funding Source: KAKEN
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A morroniside cinnamic acid conjugate was prepared and evaluated on E-selectin mediated cell-cell adhesion as an important role in inflammatory processes. 7-O-Cinnamoylmorroniside exhibited excellent anti-inflammatory activity (IC(50) = 49.3 mu M) by inhibiting the expression of E-selectin; further, it was more active than another cinnamic-acid-conjugated iridoid glycoside (harpagoside; IC(50) = 88.2 mu M), 7-O-methylmorroniside, and morroniside itself. As a result, 7-O-cinnamoylmorroniside was observed to be a potent inhibitor of TNF-alpha-induced E-selectin expression. (c) 2010 Elsevier Ltd. All rights reserved.
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