Preparation and anti-inflammatory activities of diarylheptanoid and diarylheptylamine analogs

Su Lin Lee, Wei Jan Huang, Wan Wan Lin, Shoei Sheng Lee, Chung Hsiung Chen

Research output: Contribution to journalArticle

67 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)6175-6181
Number of pages7
JournalBioorganic and Medicinal Chemistry
Volume13
Issue number22
DOIs
Publication statusPublished - Nov 15 2005
Externally publishedYes

Keywords

  • Anti-inflammatory activity
  • Curcumin
  • Diarylheptanoid
  • Diarylheptylamine
  • Preparation

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science

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