Preparation and anti-inflammatory activities of diarylheptanoid and diarylheptylamine analogs
Journal
Bioorganic and Medicinal Chemistry
Journal Volume
13
Journal Issue
22
Pages
6175-6181
Date Issued
2005
Author(s)
Abstract
Seven diarylheptylamine (12a-g) and four diarylheptanoid analogs (3-5, 9), structurally related to the natural anti-inflammatory agent oregonin (1), have been prepared from curcumin (2) for evaluation of their activity against the expression of iNOS and COX-2. Diarylheptylamine 12b and diarylheptanoid analogs can inhibit iNOS and COX-2 responses of LPS, although less potently than 1. These compounds, however, possess stronger potency than 1 against COX-2-derived PGE2 formation, of which hexahydrocurcumin (4) is the most potent one with an IC50 value of 0.7 μM. © 2005 Elsevier Ltd. All rights reserved.
SDGs
Type
journal article