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Published on: September 16, 2011
Preparation and anti-inflammatory activities of diarylheptanoid and diarylheptylamine analogs
Su-Lin Lee1, Wei-Jan Huang, Wan Wan Lin
1School of Pharmacy, College of Medicine, National Taiwan University, Taipei 100, Taiwan, ROC.
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 microM.
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